Stefan Knapp studied Chemistry at Marburg University (Germany) and the University of Illinois (USA). He did his PhD at Prof. Ladensteins laboratory at the Karolinska Institute (Stockholm, Sweden) where he also remains as a postdoctoral scientist. In 1999 he joined Pharmacia (Nerviano, Italy) and stayed there until 2004. Since 2004 he works as a principal investigator at the SGC, University of Oxford. In 2015 he joined the Department of Pharmaceutical Chemistry at the Goethe University in Frankfurt as well as the Buchmann Institute for Life Sciences (BMLS). He is a visiting Professor at the Nuffield Department of Clinical Medicine and the SGC where is still maintains a research group.

Research Areas

My laboratory is interested in understanding molecular mechanisms that regulate protein function of key signalling molecules and how these mechanisms can be utilized for the development of highly selective and potent inhibitors (chemical probes). As a basis for this work we have generated a comprehensive set of high resolution crystal structures that cover most members of the protein family of interest. We are particularly interested in protein interactions module of the bromodomain family that specifically recognize ε-N-lysine acetylation motifs, a key event in the reading process of epigenetic marks. This effort generated several highly selective chemical probes targeting bromodomains. A second research focus is on protein kinases. Our laboratory has solved a comprehensive set of crystal structure of this large protein family offering the opportunity to understand molecular mechanisms of their regulation and developing new strategies for their selective targeting. We developed for example a number of highly selective inhibitors by exploring unusual binding modes and allosteric binding sites. A particular focus of the laboratory is also to understand structural mechanisms leading to slow binding kinetics as part of the K4DD consortium.

Group Members

  • Sebastian Mathea
  • Apirat Chaikuad
  • Jing Wang
  • Kamal Abdul Azeez
  • Eidarus Salah
  • Clara Redondo
  • Fiona Sorrell
  • Marion Schuller
  • Martin Frejno
  • Matteo Aldeghi

Publications

Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit.
Fish, PV; Filippakopoulos, P; Bish, G; Brennan, PE; Bunnage, ME; Cook, AS; Federov, O; Gerstenberger, BS; Jones, H; Knapp, S; Marsden, B; Nocka, K; Owen, DR; Philpott, M; Picaud, S; Primiano, MJ; Ralph, MJ; Sciammetta, N; Trzupek, JD;
Journal of Medicinal Chemistry. 2012 55:9831-9837. doi:
PMID: 23095041

Histone recognition and large-scale structural analysis of the human bromodomain family.
Filippakopoulos P, Picaud S, Mangos M, Keates T, Lambert JP, Barsyte-Lovejoy D, Felletar I, Volkmer R, Müller S, Pawson T, Gingras AC, Arrowsmith CH, Knapp S
Cell. 2012 149(1):214-31. doi: 10.1016/j.cell.2012.02.013
PMID: 22464331

Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function.
Kwiatkowski, N; Jelluma, N; Filippakopoulos, P; Soundararajan, M; Manak, MS; Kwon, M; Choi, HG; Sim, T; Deveraux, QL; Rottmann, S; Pellman, D; Shah, JV; Kops, GJ; Knapp, S; Gray, NS;
Nature Chemical Biology. 2010 6:359-368. doi: 10.1038/nchembio.345
PMID: 20383151

Structure of the CaMKIIdelta/calmodulin complex reveals the molecular mechanism of CaMKII kinase activation.
Rellos, P; Pike, AC; Niesen, FH; Salah, E; Lee, WH; von Delft, F; Knapp, S;
PLoS Biology. 2010 8:e1000426-. doi: 10.1371/journal.pbio.1000426
PMID: 20668654

Selective inhibition of BET bromodomains.
Filippakopoulos, P; Qi, J; Picaud, S; Shen, Y; Smith, WB; Fedorov, O; Morse, EM; Keates, T; Hickman, TT; Felletar, I; Philpott, M; Munro, S; McKeown, MR; Wang, Y; Christie, AL; West, N; Cameron, MJ; Schwartz, B; Heightman, TD; La Thangue, N; French, CA; Wiest, O; Kung, AL; Knapp, S; Bradner, JE;
Nature. 2010 468:1067-1073. doi:
PMID: 20871596

The (un)targeted cancer kinome.
Fedorov, O; Müller, S; Knapp, S;
Nature Chemical Biology. 2010 6:166-169. doi:
PMID: 20154661

Structure and functional characterization of the atypical human kinase haspin.
Eswaran, J; Patnaik, D; Filippakopoulos, P; Wang, F; Stein, RL; Murray, JW; Higgins, JM; Knapp, S;
Proceedings of the National Academy of Sciences of USA. 2009 106:20198-20203. doi: 10.1073/pnas.0901989106
PMID: 19918057

Large-scale structural analysis of the classical human protein tyrosine phosphatome.
Barr, AJ; Ugochukwu, E; Lee, WH; King, ON; Filippakopoulos, P; Alfano, I; Savitsky, P; Burgess-Brown, NA; Müller, S; Knapp, S;
Cell. 2009 136:352-363. doi: 10.1016/j.cell.2008.11.038
PMID: 19167335

Structural coupling of SH2-kinase domains links Fes and Abl substrate recognition and kinase activation.
Filippakopoulos, P; Kofler, M; Hantschel, O; Gish, GD; Grebien, F; Salah, E; Neudecker, P; Kay, LE; Turk, BE; Superti-Furga, G; Pawson, T; Knapp, S;
Cell. 2008 134:793-803. doi: 10.1016/j.cell.2008.07.047
PMID: 18775312

UnPAKing the class differences among p21-activated kinases.
Eswaran, J; Soundararajan, M; Kumar, R; Knapp, S;
Trends in Biochemical Sciences. 2008 33:394-403. doi: 10.1016/j.tibs.2008.06.002
PMID: 18639460

A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
Fedorov, O; Marsden, B; Pogacic, V; Rellos, P; Müller, S; Bullock, AN; Schwaller, J; Sundström, M; Knapp, S;
Proceedings of the National Academy of Sciences of USA. 2007 104:20523-20528. doi:
PMID: 18077363

2016

Mechanism of TAp73 inhibition by ΔNp63 and structural basis of p63/p73 hetero-tetramerization.
Gebel, J; Luh, LM; Coutandin, D; Osterburg, C; Löhr, F; Schäfer, B; Frombach, AS; Sumyk, M; Buchner, L; Krojer, T; Salah, E; Mathea, S; Güntert, P; Knapp, S; Dötsch, V;
Cell Death and Differentiation. 2016 23:1930-1940. doi: 10.1038/cdd.2016.83
PMID: 27716744

Promiscuous targeting of bromodomains by bromosporine identifies BET proteins as master regulators of primary transcription response in leukemia.
Picaud, S; Leonards, K; Lambert, JP; Dovey, O; Wells, C; Fedorov, O; Monteiro, O; Fujisawa, T; Wang, CY; Lingard, H; Tallant, C; Nikbin, N; Guetzoyan, L; Ingham, R; Ley, SV; Brennan, P; Muller, S; Samsonova, A; Gingras, AC; Schwaller, J; Vassiliou, G; Knapp, S; Filippakopoulos, P;
Science Advances. 2016 2:e1600760-. doi: 10.1126/sciadv.1600760
PMID: 27757418

Development of Selective CBP/P300 Benzoxazepine Bromodomain Inhibitors.
Popp, TA; Tallant, C; Rogers, C; Fedorov, O; Brennan, PE; Müller, S; Knapp, S; Bracher, F;
Journal of Medicinal Chemistry. 2016 :-. doi:
PMID: 27673482

The MAPK pathway regulates intrinsic resistance to BET inhibitors in colorectal cancer.
Ma, Y; Wang, L; Neitzel, LR; Loganathan, S; Tang, N; Qin, L; Emily, CE; Guo, Y; Knapp, S; Beauchamp, RD; Lee, E; Wang, J;
Clinical Cancer Research. 2016 :-. doi:
PMID: 27678457

Discovery and optimization of a selective ligand for the Switch/Sucrose Non-Fermenting-related bromodomains of Polybromo protein-1 by the use of virtual screening and hydration analysis.
Myrianthopoulos, V; Gaboriaud-Kolar, N; Tallant, C; Hall, ML; Grigoriou, S; Brownlee, PM; Fedorov, O; Rogers, C; Heidenreich, D; Wanior, M; Drosos, N; Mexia, N; Savitsky, P; Bagratuni, T; Kastritis, E; Terpos, E; Filippakopoulos, P; Müller, S; Skaltsounis, AL; Downs, JA; Knapp, S; Mikros, E;
Journal of Medicinal Chemistry. 2016 :-. doi:
PMID: 27617704

Salt-Inducible Kinase 2 Couples Ovarian Cancer Cell Metabolism with Survival at the Adipocyte-Rich Metastatic Niche.
Miranda, F; Mannion, D; Liu, S; Zheng, Y; Mangala, LS; Redondo, C; Herrero-Gonzalez, S; Xu, R; Taylor, C; Chedom, DF; Karaminejadranjbar, M; Albukhari, A; Jiang, D; Pradeep, S; Rodriguez-Aguayo, C; Lopez-Berestein, G; Salah, E; Abdul Azeez, KR; Elkins, JM; Campo, L; Myers, KA; Klotz, D; Bivona, S; Dhar, S; Bast, RC; Saya, H; Choi, HG; Gray, NS; Fischer, R; Kessler, BM; Yau, C; Sood, AK; Motohara, T; Knapp, S; Ahmed, AA;
Cancer Cell. 2016 30:273-289. doi:
PMID: 27478041

Cardiac myosin light chain is phosphorylated by Ca2+/calmodulin-dependent and -independent kinase activities.
Chang, AN; Mahajan, P; Knapp, S; Barton, H; Sweeney, HL; Kamm, KE; Stull, JT;
Proceedings of the National Academy of Sciences of USA. 2016 113:E3824-E3833. doi:
PMID: 27325775

Mapping the chemical chromatin reactivation landscape identifies BRD4-TAF1 cross-talk.
Sdelci, S; Lardeau, CH; Tallant, C; Klepsch, F; Klaiber, B; Bennett, J; Rathert, P; Schuster, M; Penz, T; Fedorov, O; Superti-Furga, G; Bock, C; Zuber, J; Huber, KV; Knapp, S; Müller, S; Kubicek, S;
Nature Chemical Biology. 2016 12:504-510. doi:
PMID: 27159579

The BET inhibitor JQ1 selectively impairs tumour response to hypoxia and downregulates CA9 and angiogenesis in triple negative breast cancer.
da Motta, LL; Ledaki, I; Purshouse, K; Haider, S; De Bastiani, MA; Baban, D; Morotti, M; Steers, G; Wigfield, S; Bridges, E; Li, JL; Knapp, S; Ebner, D; Klamt, F; Harris, AL; McIntyre, A;
Oncogene. 2016 :-. doi:
PMID: 27292261

BET inhibition as a new strategy for the treatment of gastric cancer.
Montenegro, RC; Clark, PG; Howarth, A; Wan, X; Ceroni, A; Siejka, P; Nunez-Alonso, GA; Monteiro, O; Rogers, C; Gamble, V; Burbano, R; Brennan, PE; Tallant, C; Ebner, D; Fedorov, O; O'Neill, E; Knapp, S; Dixon, D; Müller, S;
Oncotarget. 2016 :-. doi:
PMID: 27259267

Protein-Protein Interaction Inhibition (2P2I)-Oriented Chemical Library Accelerates Hit Discovery.
Milhas, S; Raux, B; Betzi, S; Derviaux, C; Roche, P; Restouin, A; Basse, MJ; Rebuffet, E; Lugari, A; Badol, M; Kashyap, R; Lissitzky, JC; Eydoux, C; Hamon, V; Gourdel, ME; Combes, S; Zimmermann, P; Aurrand-Lions, M; Roux, T; Rogers, C; Müller, S; Knapp, S; Trinquet, E; Collette, Y; Guillemot, JC; Morelli, X;
ACS Chemical Biology. 2016 11:2140-2148. doi:
PMID: 27219844

Co-crystal structures of the protein kinase haspin with bisubstrate inhibitors.
Lavogina, D; Kestav, K; Chaikuad, A; Heroven, C; Knapp, S; Uri, A;
Acta Crystallographica Section F: Structural Biology Communications. 2016 72:339-345. doi:
PMID: 27139824

Identification and Development of 2,3-Dihydropyrrolo[1,2-a]quinazolin-5(1H)-one Inhibitors Targeting Bromodomains within the Switch/Sucrose Nonfermenting Complex.
Sutherell, CL; Tallant, C; Monteiro, OP; Yapp, C; Fuchs, JE; Fedorov, O; Siejka, P; Müller, S; Knapp, S; Brenton, JD; Brennan, PE; Ley, SV;
Journal of Medicinal Chemistry. 2016 59:5095-5101. doi:
PMID: 27119626

Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit.
Gerstenberger, BS; Trzupek, JD; Tallant, C; Fedorov, O; Filippakopoulos, P; Brennan, PE; Fedele, V; Martin, S; Picaud, S; Rogers, C; Parikh, M; Taylor, A; Samas, B; O'Mahony, A; Berg, E; Pallares, G; Torrey, AD; Treiber, DK; Samardjiev, IJ; Nasipak, BT; Padilla-Benavides, T; Wu, Q; Imbalzano, AN; Nickerson, JA; Bunnage, ME; Müller, S; Knapp, S; Owen, DR;
Journal of Medicinal Chemistry. 2016 59:4800-4811. doi:
PMID: 27115555

Discovery of pyrido[3,4-g]quinazoline derivatives as CMGC family protein kinase inhibitors: Design, synthesis, inhibitory potency and X-ray co-crystal structure.
Esvan, YJ; Zeinyeh, W; Boibessot, T; Nauton, L; Théry, V; Knapp, S; Chaikuad, A; Loaëc, N; Meijer, L; Anizon, F; Giraud, F; Moreau, P;
European Journal of Medicinal Chemistry. 2016 118:170-177. doi:
PMID: 27128181

Quality control in oocytes by p63 is based on a spring-loaded activation mechanism on the molecular and cellular level.
Coutandin, D; Osterburg, C; Srivastav, RK; Sumyk, M; Kehrloesser, S; Gebel, J; Tuppi, M; Hannewald, J; Schäfer, B; Salah, E; Mathea, S; Müller-Kuller, U; Doutch, J; Grez, M; Knapp, S; Dötsch, V;
eLife. 2016 5:-. doi:
PMID: 27021569

Structure of the Human Protein Kinase ZAK in Complex with Vemurafenib.
Mathea, S; Abdul Azeez, KR; Salah, E; Tallant, C; Wolfreys, F; Konietzny, R; Fischer, R; Lou, HJ; Brennan, PE; Schnapp, G; Pautsch, A; Kessler, BM; Turk, BE; Knapp, S;
ACS Chemical Biology. 2016 11:1595-1602. doi:
PMID: 26999302

Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor.
Martin, LJ; Koegl, M; Bader, G; Cockcroft, XL; Fedorov, O; Fiegen, D; Gerstberger, T; Hofmann, MH; Hohmann, AF; Kessler, D; Knapp, S; Knesl, P; Kornigg, S; Müller, S; Nar, H; Rogers, C; Rumpel, K; Schaaf, O; Steurer, S; Tallant, C; Vakoc, CR; Zeeb, M; Zoephel, A; Pearson, M; Boehmelt, G; McConnell, D;
Journal of Medicinal Chemistry. 2016 59:4462-4475. doi:
PMID: 26914985

Citrullination-acetylation interplay guides E2F-1 activity during the inflammatory response.
Ghari, F; Quirke, AM; Munro, S; Kawalkowska, J; Picaud, S; McGouran, J; Subramanian, V; Muth, A; Williams, R; Kessler, B; Thompson, PR; Fillipakopoulos, P; Knapp, S; Venables, PJ; La Thangue, NB;
Science Advances. 2016 2:e1501257-. doi:
PMID: 26989780

Family-wide Structural Analysis of Human Numb-Associated Protein Kinases.
Sorrell, FJ; Szklarz, M; Abdul Azeez, KR; Elkins, JM; Knapp, S;
Structure. 2016 24:401-411. doi:
PMID: 26853940

Epigenomic regulation of oncogenesis by chromatin remodeling.
Kumar, R; Li, DQ; Müller, S; Knapp, S;
Oncogene. 2016 35:4423-4436. doi:
PMID: 26804164

The Intersection of Structural and Chemical Biology - An Essential Synergy.
Zuercher, WJ; Elkins, JM; Knapp, S;
Cell chemical biology. 2016 23:173-182. doi:
PMID: 26933743

Structure-Based Identification of Inhibitory Fragments Targeting the p300/CBP-Associated Factor Bromodomain.
Chaikuad, A; Lang, S; Brennan, PE; Temperini, C; Fedorov, O; Hollander, J; Nachane, R; Abell, C; Müller, S; Siegal, G; Knapp, S;
Journal of Medicinal Chemistry. 2016 59:1648-1653. doi:
PMID: 26731131

Exploring Selective Inhibition of the First Bromodomain of the Human Bromodomain and Extra-terminal Domain (BET) Proteins.
Raux, B; Voitovich, Y; Derviaux, C; Lugari, A; Rebuffet, E; Milhas, S; Priet, S; Roux, T; Trinquet, E; Guillemot, JC; Knapp, S; Brunel, JM; Fedorov, AY; Collette, Y; Roche, P; Betzi, S; Combes, S; Morelli, X;
Journal of Medicinal Chemistry. 2016 59:1634-1641. doi:
PMID: 26735842

Effect of BET Missense Mutations on Bromodomain Function, Inhibitor Binding and Stability.
Lori, L; Pasquo, A; Lori, C; Petrosino, M; Chiaraluce, R; Tallant, C; Knapp, S; Consalvi, V;
PLoS One. 2016 11:e0159180-. doi:
PMID: 27403962

Comprehensive characterization of the Published Kinase Inhibitor Set.
Elkins, JM; Fedele, V; Szklarz, M; Abdul Azeez, KR; Salah, E; Mikolajczyk, J; Romanov, S; Sepetov, N; Huang, XP; Roth, BL; Al Haj Zen, A; Fourches, D; Muratov, E; Tropsha, A; Morris, J; Teicher, BA; Kunkel, M; Polley, E; Lackey, KE; Atkinson, FL; Overington, JP; Bamborough, P; Müller, S; Price, DJ; Willson, TM; Drewry, DH; Knapp, S; Zuercher, WJ;
Nature Biotechnology. 2016 34:95-103. doi:
PMID: 26501955

Novel p38α MAP kinase inhibitors identified from yoctoReactor DNA-encoded small molecule library
Petersen, LK; Blakskjær, P; Chaikuad, A; Christensen, AB; Dietvorst, J; Holmkvist, J; Knapp, S; Kořínek, M; Larsen, LK; Pedersen, AE; Röhm, S; Sløk, FA; Hansen, NJV;
MedChemComm. 2016 7:1332-1339. doi: 10.1039/c6md00241b
PMID:

Emerging Target Families: Intractable Targets.
K, S; n, ; a, ; p, ; p, ;
Handbook of Experimental Pharmacology. 2016 232:43-58. doi:
PMID: 26552403

Atad2 is a generalist facilitator of chromatin dynamics in embryonic stem cells.
Morozumi, Y; Boussouar, F; Tan, M; Chaikuad, A; Jamshidikia, M; Colak, G; He, H; Nie, L; Petosa, C; de Dieuleveult, M; Curtet, S; Vitte, AL; Rabatel, C; Debernardi, A; Cosset, FL; Verhoeyen, E; Emadali, A; Schweifer, N; Gianni, D; Gut, M; Guardiola, P; Rousseaux, S; Gérard, M; Knapp, S; Zhao, Y; Khochbin, S;
Journal of Molecular Cell Biology. 2016 8:349-362. doi:
PMID: 26459632

Discovery of a Chemical Tool Inhibitor Targeting the Bromodomains of TRIM24 and BRPF.
Bennett, J; Fedorov, O; Tallant, C; Monteiro, O; Meier, J; Gamble, V; Savitsky, P; Nunez-Alonso, GA; Haendler, B; Rogers, C; Brennan, PE; Müller, S; Knapp, S;
Journal of Medicinal Chemistry. 2016 59:1642-1647. doi:
PMID: 25974391

Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B.
Chen, P; Chaikuad, A; Bamborough, P; Bantscheff, M; Bountra, C; Chung, CW; Fedorov, O; Grandi, P; Jung, D; Lesniak, R; Lindon, M; Müller, S; Philpott, M; Prinjha, R; Rogers, C; Selenski, C; Tallant, C; Werner, T; Willson, TM; Knapp, S; Drewry, DH;
Journal of Medicinal Chemistry. 2016 59:1410-1424. doi:
PMID: 25799074

Accurate calculation of the absolute free energy of binding for drug molecules.
Aldeghi, M; Heifetz, A; Bodkin, MJ; Knapp, S; Biggin, PC;
Chemical Science. 2016 7:207-218. doi:
PMID: 26798447

2017

BRD4 localization to lineage-specific enhancers is associated with a distinct transcription factor repertoire.
Najafova, Z; Tirado-Magallanes, R; Subramaniam, M; Hossan, T; Schmidt, G; Nagarajan, S; Baumgart, SJ; Mishra, VK; Bedi, U; Hesse, E; Knapp, S; Hawse, JR; Johnsen, SA;
Nucleic Acids Research. 2017 45:127-141. doi: 10.1093/nar/gkw826
PMID: 27651452

2015

Generation of a Selective Small Molecule Inhibitor of the CBP/p300 Bromodomain for Leukemia Therapy.
Picaud, S; Fedorov, O; Thanasopoulou, A; Leonards, K; Jones, K; Meier, J; Olzscha, H; Monteiro, O; Martin, S; Philpott, M; Tumber, A; Filippakopoulos, P; Yapp, C; Wells, C; Che, KH; Bannister, A; Robson, S; Kumar, U; Parr, N; Lee, K; Lugo, D; Jeffrey, P; Taylor, S; Vecellio, ML; Bountra, C; Brennan, PE; O'Mahony, A; Velichko, S; Müller, S; Hay, D; Daniels, DL; Urh, M; La Thangue, NB; Kouzarides, T; Prinjha, R; Schwaller, J; Knapp, S;
Cancer Research. 2015 75:5106-5119. doi:
PMID: 26552700

Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance.
Fedorov, O; Castex, J; Tallant, C; Owen, DR; Martin, S; Aldeghi, M; Monteiro, O; Filippakopoulos, P; Picaud, S; Trzupek, JD; Gerstenberger, BS; Bountra, C; Willmann, D; Wells, C; Philpott, M; Rogers, C; Biggin, PC; Brennan, PE; Bunnage, ME; Schüle, R; Günther, T; Knapp, S; Müller, S;
Science Advances. 2015 1:e1500723-. doi:
PMID: 26702435

The ins and outs of selective kinase inhibitor development.
Müller, S; Chaikuad, A; Gray, NS; Knapp, S;
Nature Chemical Biology. 2015 11:818-821. doi:
PMID: 26485069

Overcoming ABCG2-mediated drug resistance with imidazo-[1,2-b]-pyridazine-based Pim1 kinase inhibitors.
Darby, RA; Unsworth, A; Knapp, S; Kerr, ID; Callaghan, R;
Cancer Chemotherapy and Pharmacology. 2015 76:853-864. doi:
PMID: 26351135

Differential Recognition Preferences of the Three Src Homology 3 (SH3) Domains from the Adaptor CD2-associated Protein (CD2AP) and Direct Association with Ras and Rab Interactor 3 (RIN3).
Rouka, E; Simister, PC; Janning, M; Kumbrink, J; Konstantinou, T; Muniz, JR; Joshi, D; O'Reilly, N; Volkmer, R; Ritter, B; Knapp, S; von Delft, F; Kirsch, KH; Feller, SM;
Journal of Biological Chemistry. 2015 290:25275-25292. doi:
PMID: 26296892

CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses.
Hammitzsch, A; Tallant, C; Fedorov, O; O'Mahony, A; Brennan, PE; Hay, DA; Martinez, FO; Al-Mossawi, MH; de Wit, J; Vecellio, M; Wells, C; Wordsworth, P; Müller, S; Knapp, S; Bowness, P;
Proceedings of the National Academy of Sciences of USA. 2015 112:10768-10773. doi:
PMID: 26261308

The salt inducible kinase 2 (SIK2) links lipid metabolism to survival of ovarian cancer metastasis
Miranda, F; Liu, S; Herrero-Gonzalez, S; Mannion, D; Knapp, S; Ahmed, AA;
Cancer Research. 2015 75:-. doi: 10.1158/1538-7445.AM2015-4111
PMID:

Defined PEG smears as an alternative approach to enhance the search for crystallization conditions and crystal-quality improvement in reduced screens.
Chaikuad, A; Knapp, S; von Delft, F;
Acta Crystallographica Section D: Biological Crystallography. 2015 71:1627-1639. doi:
PMID: 26249344

A core of kinase-regulated interactomes defines the neoplastic MDSC lineage.
Gato-Cañas, M; Martinez de Morentin, X; Blanco-Luquin, I; Fernandez-Irigoyen, J; Zudaire, I; Liechtenstein, T; Arasanz, H; Lozano, T; Casares, N; Chaikuad, A; Knapp, S; Guerrero-Setas, D; Escors, D; Kochan, G; Santamaría, E;
Oncotarget. 2015 6:27160-27175. doi:
PMID: 26320174

Type II Inhibitors Targeting CDK2.
Alexander, LT; Möbitz, H; Drueckes, P; Savitsky, P; Fedorov, O; Elkins, JM; Deane, CM; Cowan-Jacob, SW; Knapp, S;
ACS Chemical Biology. 2015 10:2116-2125. doi:
PMID: 26158339

Design and synthesis of potent and selective inhibitors of BRD7 and BRD9 bromodomains
Hay, DA; Rogers, CM; Fedorov, O; Tallant, C; Martin, S; Monteiro, OP; Mueller, S; Knapp, S; Schofield, CJ; Brennan, PE;
MedChemComm. 2015 6:1381-1386. doi: 10.1039/c5md00152h
PMID:

Pim Kinase Inhibitors Evaluated with a Single-Molecule Engineered Nanopore Sensor.
Harrington, L; Alexander, LT; Knapp, S; Bayley, H;
Angewandte Chemie International Edition. 2015 54:8154-8159. doi:
PMID: 26058458

Development of SRPK1 inhibitors as novel anti-angiogenic therapeutics for exudative age-related macular degeneration (AMD)
Batson, J; Troop, H; Rowlinson, J; Allen, C; Babaei-Jadidi, R; Zhang, J; Wearmouth, S; Knapp, S; Morris, J; Bates, D;
Investigative Ophthalmology and Visual Science. 2015 56:-. doi:
PMID:

LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor.
Clark, PG; Vieira, LC; Tallant, C; Fedorov, O; Singleton, DC; Rogers, CM; Monteiro, OP; Bennett, JM; Baronio, R; Müller, S; Daniels, DL; Méndez, J; Knapp, S; Brennan, PE; Dixon, DJ;
Angewandte Chemie International Edition. 2015 127:6315-6319. doi:
PMID: 27346896

LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor.
Clark, PG; Vieira, LC; Tallant, C; Fedorov, O; Singleton, DC; Rogers, CM; Monteiro, OP; Bennett, JM; Baronio, R; Müller, S; Daniels, DL; Méndez, J; Knapp, S; Brennan, PE; Dixon, DJ;
Angewandte Chemie International Edition. 2015 54:6217-6221. doi:
PMID: 25864491

Perspective on computational and structural aspects of kinase discovery from IPK2014.
Martin, E; Knapp, S; Engh, RA; Moebitz, H; Varin, T; Roux, B; Meiler, J; Berdini, V; Baumann, A; Vieth, M;
Biochimica et Biophysica Acta: international journal of biochemistry and biophysics. 2015 1854:1595-1604. doi:
PMID: 25861861

Selective Inhibitors of Cyclin G Associated Kinase (GAK) as Anti-Hepatitis C Agents.
Kovackova, S; Chang, L; Bekerman, E; Neveu, G; Barouch-Bentov, R; Chaikuad, A; Heroven, C; Šála, M; De Jonghe, S; Knapp, S; Einav, S; Herdewijn, P;
Journal of Medicinal Chemistry. 2015 58:3393-3410. doi:
PMID: 25822739

10-iodo-11H-indolo[3,2-c]quinoline-6-carboxylic acids are selective inhibitors of DYRK1A.
Falke, H; Chaikuad, A; Becker, A; Loaëc, N; Lozach, O; Abu Jhaisha, S; Becker, W; Jones, PG; Preu, L; Baumann, K; Knapp, S; Meijer, L; Kunick, C;
Journal of Medicinal Chemistry. 2015 58:3131-3143. doi:
PMID: 25730262

Structure enabled design of BAZ2-ICR, a chemical probe targeting the bromodomains of BAZ2A and BAZ2B.
Drouin, L; McGrath, S; Vidler, LR; Chaikuad, A; Monteiro, O; Tallant, C; Philpott, M; Rogers, C; Fedorov, O; Liu, M; Akhtar, W; Hayes, A; Raynaud, F; Müller, S; Knapp, S; Hoelder, S;
Journal of Medicinal Chemistry. 2015 58:2553-2559. doi:
PMID: 25719566

Absolute Binding Free Energy Calculations of Bromodomain Inhibitors
Aldeghi, M; Knapp, S; Heifetz, A; Barker, JJ; Bodkin, MJ; Law, RJ; Biggin, PC;
Biophysical Journal. 2015 108:357A-357A. doi:
PMID:

Perspective on computational and structural aspects of kinase discovery from IPK2014
Martin, E; Knapp, S; Engh, RA; Moebitz, H; Varin, T; Roux, B; Meiler, J; Berdini, V; Baumann, A; Vieth, M;
BBA: Proteins and Proteomics. 2015 1854:1595-1604. doi: 10.1016/j.bbapap.2015.03.014
PMID:

Bisubstrate inhibitor approach for targeting mitotic kinase Haspin.
Kestav, K; Lavogina, D; Raidaru, G; Chaikuad, A; Knapp, S; Uri, A;
Bioconjugate Chemistry. 2015 26:225-234. doi:
PMID: 25595038

Identification and structure-function analysis of subfamily selective G protein-coupled receptor kinase inhibitors.
Homan, KT; Larimore, KM; Elkins, JM; Szklarz, M; Knapp, S; Tesmer, JJ;
ACS Chemical Biology. 2015 10:310-319. doi:
PMID: 25238254

The global cancer genomics consortium’s symposium: New era of molecular medicine and epigenetic cancer medicine - Cross section of genomics and epigenetics
Toi, M; Pillai, MR; Gupta, S; Badwe, R; Carmo-Fonseca, M; Costa, L; Chow, LWC; Knapp, S; Kumar, R;
Genes and Cancer. 2015 6:1-8. doi:
PMID:

PIM kinase-responsive microsecond-lifetime photoluminescent probes based on selenium-containing heteroaromatic tricycle
Ekambaram, R; Manoharan, GB; Enkvist, E; Ligi, K; Knapp, S; Uri, A;
RSC Advances. 2015 5:96750-96757. doi: 10.1039/c5ra20777k
PMID:

Nanog requires BRD4 to maintain murine embryonic stem cell pluripotency and is suppressed by bromodomain inhibitor JQ1 together with Lefty1.
Horne, GA; Stewart, HJ; Dickson, J; Knapp, S; Ramsahoye, B; Chevassut, T;
Stem Cells and Development. 2015 24:879-891. doi:
PMID: 25393219

Molecular basis of histone tail recognition by human TIP5 PHD finger and bromodomain of the chromatin remodeling complex NoRC.
Tallant, C; Valentini, E; Fedorov, O; Overvoorde, L; Ferguson, FM; Filippakopoulos, P; Svergun, DI; Knapp, S; Ciulli, A;
Structure. 2015 23:80-92. doi:
PMID: 25533489

Identification and characterization of a small-molecule inhibitor of death-associated protein kinase 1.
Wilbek, TS; Skovgaard, T; Sorrell, FJ; Knapp, S; Berthelsen, J; Strømgaard, K;
ChemBioChem: a European journal of chemical biology. 2015 16:59-63. doi:
PMID: 25382253

2014

Crystal Structure of Sphingosine Kinase 1 with PF-543.
Wang, J; Knapp, S; Pyne, NJ; Pyne, S; Elkins, JM;
ACS Medicinal Chemistry Letters. 2014 5:1329-1333. doi:
PMID: 25516793

Targeting Aberrant Self-Renewal of Leukemic Cells with a Novel CBP/p300 Bromodomain Inhibitor
Thanasopoulou, A; Dumrese, K; Picaud, S; Fedorov, O; Knapp, S; Schwaller, J;
Blood. 2014 124:-. doi:
PMID:

Copper is required for oncogenic BRAF signaling and tumorigenesis
Brady, D; Crowe, M; Turski, M; Hobbs, A; Yao, X; Chaikuad, A; Knapp, S; Xiao, K; Campbell, S; Thiele, D; Counter, C;
Molecular Cancer Research. 2014 12:-. doi: 10.1158/1557-3125.RASONC14-IA09
PMID:

Structure-based approaches towards identification of fragments for the low-druggability ATAD2 bromodomain
Chaikuad, A; Petros, AM; Fedorov, O; Xu, J; Knapp, S;
MedChemComm. 2014 5:1843-1848. doi: 10.1039/c4md00237g
PMID:

The crystal structure of the RhoA-AKAP-Lbc DH-PH domain complex.
Abdul Azeez, KR; Knapp, S; Fernandes, JM; Klussmann, E; Elkins, JM;
Biochemical Journal. 2014 464:231-239. doi:
PMID: 25186459

Dual kinase/bromodomain inhibitors for rationally designed polypharmacology
Quinn, ER; Ciceri, P; Mueller-Knapp, S; O'Mahony, A; Fedorov, O; Filippakopoulos, P; Hunt, JP; Lasater, EA; Pallares, G; Picaud, S; Wells, C; Wodicka, LM; Shah, NP; Knapp, S; Treiber, DK;
Cancer Research. 2014 74:-. doi: 10.1158/1538-7445.AM2014-5387
PMID:

A unique inhibitor binding site in ERK1/2 is associated with slow binding kinetics.
Chaikuad, A; Tacconi, EM; Zimmer, J; Liang, Y; Gray, NS; Tarsounas, M; Knapp, S;
Nature Chemical Biology. 2014 10:853-860. doi:
PMID: 25195011

Recently targeted kinases and their inhibitors-the path to clinical trials.
Knapp, S; Sundström, M;
Current Opinion in Pharmacology. 2014 17:58-63. doi:
PMID: 25113945

Bromodomain protein BRD4 is required for estrogen receptor-dependent enhancer activation and gene transcription.
Nagarajan, S; Hossan, T; Alawi, M; Najafova, Z; Indenbirken, D; Bedi, U; Taipaleenmäki, H; Ben-Batalla, I; Scheller, M; Loges, S; Knapp, S; Hesse, E; Chiang, CM; Grundhoff, A; Johnsen, SA;
Cell Reports. 2014 8:460-469. doi:
PMID: 25017071

Exploration of type II binding mode: A privileged approach for kinase inhibitor focused drug discovery?
Zhao, Z; Wu, H; Wang, L; Liu, Y; Knapp, S; Liu, Q; Gray, NS;
ACS Chemical Biology. 2014 9:1230-1241. doi:
PMID: 24730530

Discovery and optimization of small-molecule ligands for the CBP/p300 bromodomains.
Hay, DA; Fedorov, O; Martin, S; Singleton, DC; Tallant, C; Wells, C; Picaud, S; Philpott, M; Monteiro, OP; Rogers, CM; Conway, SJ; Rooney, TP; Tumber, A; Yapp, C; Filippakopoulos, P; Bunnage, ME; Müller, S; Knapp, S; Schofield, CJ; Brennan, PE;
Journal of the American Chemical Society. 2014 136:9308-9319. doi:
PMID: 24946055

A series of potent CREBBP bromodomain ligands reveals an induced-fit pocket stabilized by a cation-π interaction.
Rooney, TP; Filippakopoulos, P; Fedorov, O; Picaud, S; Cortopassi, WA; Hay, DA; Martin, S; Tumber, A; Rogers, CM; Philpott, M; Wang, M; Thompson, AL; Heightman, TD; Pryde, DC; Cook, A; Paton, RS; Müller, S; Knapp, S; Brennan, PE; Conway, SJ;
Angewandte Chemie International Edition. 2014 53:6126-6130. doi:
PMID: 24821300

Targeting bromodomains: epigenetic readers of lysine acetylation.
Filippakopoulos, P; Knapp, S;
Nature Reviews Drug Discovery. 2014 13:337-356. doi:
PMID: 24751816

Modulation of the chromatin phosphoproteome by the Haspin protein kinase.
Maiolica, A; de Medina-Redondo, M; Schoof, EM; Chaikuad, A; Villa, F; Gatti, M; Jeganathan, S; Lou, HJ; Novy, K; Hauri, S; Toprak, UH; Herzog, F; Meraldi, P; Penengo, L; Turk, BE; Knapp, S; Linding, R; Aebersold, R;
Molecular and Cellular Proteomics. 2014 13:1724-1740. doi:
PMID: 24732914

Copper is required for oncogenic BRAF signalling and tumorigenesis.
Brady, DC; Crowe, MS; Turski, ML; Hobbs, GA; Yao, X; Chaikuad, A; Knapp, S; Xiao, K; Campbell, SL; Thiele, DJ; Counter, CM;
Nature. 2014 509:492-496. doi:
PMID: 24717435

Stereospecific targeting of MTH1 by (S)-crizotinib as an anticancer strategy.
Huber, KV; Salah, E; Radic, B; Gridling, M; Elkins, JM; Stukalov, A; Jemth, AS; Göktürk, C; Sanjiv, K; Strömberg, K; Pham, T; Berglund, UW; Colinge, J; Bennett, KL; Loizou, JI; Helleday, T; Knapp, S; Superti-Furga, G;
Nature. 2014 508:222-227. doi:
PMID: 24695225

Novel approaches for targeting kinases: allosteric inhibition, allosteric activation and pseudokinases.
Cowan-Jacob, SW; Jahnke, W; Knapp, S;
Future Medicinal Chemistry. 2014 6:541-561. doi:
PMID: 24649957

Machine-assisted synthesis of modulators of the histone reader BRD9 using flow methods of chemistry and frontal affinity chromatography
Guetzoyan, L; Ingham, RJ; Nikbin, N; Rossignol, J; Wolling, M; Baumert, M; Burgess-Brown, NA; Strain-Damerell, CM; Shrestha, L; Brennan, PE; Fedorov, O; Knapp, S; Ley, SV;
MedChemComm. 2014 5:540-546. doi: 10.1039/c4md00007b
PMID:

Dual kinase-bromodomain inhibitors for rationally designed polypharmacology.
Ciceri, P; Müller, S; O'Mahony, A; Fedorov, O; Filippakopoulos, P; Hunt, JP; Lasater, EA; Pallares, G; Picaud, S; Wells, C; Martin, S; Wodicka, LM; Shah, NP; Treiber, DK; Knapp, S;
Nature Chemical Biology. 2014 10:305-312. doi:
PMID: 24584101

A new way to interrogate PTPs
Van Ameijde, J; Overvoorde, J; Knapp, S; Den Hertog, J; Ruijtenbeek, R; Liskamp, RM;
Assay and Drug Development Technologies. 2014 12:105-106. doi: 10.1089/adt.2014.1202.lr
PMID:

Discovery of BET bromodomain inhibitors and their role in target validation
Mueller, S; Knapp, S;
MedChemComm. 2014 5:288-296. doi: 10.1039/c3md00291h
PMID:

Electrostatically Enhanced Association of a Pim Kinase Substrate Revealed by Stochastic Detection
Harrington, L; Cheley, S; Alexander, LT; Knapp, S; Bayley, H;
Biophysical Journal. 2014 106:18A-18A. doi:
PMID:

The structural basis of PI3K cancer mutations: from mechanism to therapy.
Liu, S; Knapp, S; Ahmed, AA;
Cancer Research. 2014 74:641-646. doi: 10.1158/0008-5472.CAN-13-2319
PMID: 24459181

Diverse levels of sequence selectivity and catalytic efficiency of protein-tyrosine phosphatases
Selner, NG; Luechapanichkul, R; Chen, X; Neel, BG; Zhang, ZY; Knapp, S; Bell, CE; Pei, D;
Biochemistry. 2014 53:397-412. doi: 10.1021/bi401223r
PMID: 24359314

Structure of cyclin G-associated kinase (GAK) trapped in different conformations using nanobodies.
Chaikuad, A; Keates, T; Vincke, C; Kaufholz, M; Zenn, M; Zimmermann, B; Gutiérrez, C; Zhang, RG; Hatzos-Skintges, C; Joachimiak, A; Muyldermans, S; Herberg, FW; Knapp, S; Müller, S;
Biochemical Journal. 2014 459:59-69. doi:
PMID: 24438162

A comparison of protein kinases inhibitor screening methods using both enzymatic activity and binding affinity determination.
Rudolf, AF; Skovgaard, T; Knapp, S; Jensen, LJ; Berthelsen, J;
PLoS One. 2014 9:e98800-. doi:
PMID: 24915177

The global cancer genomics consortium’s third annual symposium: From oncogenomics to cancer care
Costa, L; Casimiro, S; Gupta, S; Knapp, S; Pillai, MR; Toi, M; Badwe, R; Carmo-Fonseca, M; Kumar, R;
Genes and Cancer. 2014 5:64-70. doi:
PMID:

Benzoselenadiazole-based responsive long-lifetime photoluminescent probes for protein kinases.
Ekambaram, R; Enkvist, E; Manoharan, G; Ugandi, M; Kasari, M; Viht, K; Knapp, S; Issinger, OG; Uri, A;
Chemical Communications. 2014 50:4096-4098. doi:
PMID: 24619026

BROMODOMAIN INHIBITORS REDUCE TH17-TYPE RESPONSES IN SPONDYLOARTHRITIS IN VITRO
Hammitzsch, A; de Wit, J; Ridley, A; Al-Mossawi, MH; Knapp, S; Bowness, P;
Clinical and Experimental Rheumatology. 2014 32:810-810. doi:
PMID:

Assessing cellular efficacy of bromodomain inhibitors using fluorescence recovery after photobleaching.
Philpott, M; Rogers, CM; Yapp, C; Wells, C; Lambert, JP; Strain-Damerell, C; Burgess-Brown, NA; Gingras, AC; Knapp, S; Müller, S;
Epigenetics and Chromatin. 2014 7:14-. doi:
PMID: 25097667

Identification of a major determinant for serine-threonine kinase phosphoacceptor specificity.
Chen, C; Ha, BH; Thévenin, AF; Lou, HJ; Zhang, R; Yip, KY; Peterson, JR; Gerstein, M; Kim, PM; Filippakopoulos, P; Knapp, S; Boggon, TJ; Turk, BE;
Molecular Cell. 2014 53:140-147. doi: 10.1016/j.molcel.2013.11.013
PMID: 24374310

[1,2,4]triazolo[4,3-a]phthalazines: inhibitors of diverse bromodomains.
Fedorov, O; Lingard, H; Wells, C; Monteiro, OP; Picaud, S; Keates, T; Yapp, C; Philpott, M; Martin, SJ; Felletar, I; Marsden, BD; Filippakopoulos, P; Müller, S; Knapp, S; Brennan, PE;
Journal of Medicinal Chemistry. 2014 57:462-476. doi:
PMID: 24313754

A versatile spectrophotometric protein tyrosine phosphatase assay based on 3-nitrophosphotyrosine containing substrates.
van Ameijde, J; Overvoorde, J; Knapp, S; den Hertog, J; Ruijtenbeek, R; Liskamp, RM;
Analytical Biochemistry. 2014 448:9-13. doi: 10.1016/j.ab.2013.11.023
PMID: 24309020

2013

Targeting low-druggability bromodomains: fragment based screening and inhibitor design against the BAZ2B bromodomain.
Ferguson, FM; Fedorov, O; Chaikuad, A; Philpott, M; Muniz, JR; Felletar, I; von Delft, F; Heightman, T; Knapp, S; Abell, C; Ciulli, A;
Journal of Medicinal Chemistry. 2013 56:10183-10187. doi:
PMID: 24304323

Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones
Deng, X; Elkins, JM; Zhang, J; Yang, Q; Erazo, T; Gomez, N; Choi, HG; Wang, J; Dzamko, N; Lee, JD; Sim, T; Kim, N; Alessi, DR; Lizcano, JM; Knapp, S; Gray, NS;
European Journal of Medicinal Chemistry. 2013 70:758-767. doi: 10.1016/j.ejmech.2013.10.052
PMID: 24239623

RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain.
Picaud, S; Wells, C; Felletar, I; Brotherton, D; Martin, S; Savitsky, P; Diez-Dacal, B; Philpott, M; Bountra, C; Lingard, H; Fedorov, O; Müller, S; Brennan, PE; Knapp, S; Filippakopoulos, P;
Proceedings of the National Academy of Sciences of USA. 2013 110:19754-19759. doi:
PMID: 24248379

Highly functionalized terpyridines as competitive inhibitors of AKAP-PKA interactions
Schäfer, G; Milic̈, J; Eldahshan, A; Götz, F; Zühlke, K; Schillinger, C; Kreuchwig, A; Elkins, JM; Abdulazeez, KR; Oder, A; Moutty, MC; Masada, N; Beerbaum, M; Schlegel, B; Niquet, S; Schmieder, P; Krause, G; Vonkries, JP; Cooper, DMF; Knapp, S; Rademann, J; Rosenthal, W; Klussmann, E;
Angewandte Chemie International Edition. 2013 52:12187-12191. doi: 10.1002/anie.201304686
PMID: 24115519

Maintenance of muscle myosin levels in adult C. elegans requires both the double bromodomain protein BET-1 and sumoylation.
Fisher, K; Gee, F; Wang, S; Xue, F; Knapp, S; Philpott, M; Wells, C; Rodriguez, M; Snoek, LB; Kammenga, J; Poulin, GB;
Biology Open. 2013 2:1354-1363. doi: 10.1242/bio.20136007
PMID: 24285704

Stochastic detection of Pim protein kinases reveals electrostatically enhanced association of a peptide substrate.
Harrington, L; Cheley, S; Alexander, LT; Knapp, S; Bayley, H;
Proceedings of the National Academy of Sciences of USA. 2013 110:E4417-E4426. doi: 10.1073/pnas.1312739110
PMID: 24194548

Real-Time Monitoring of the Dephosphorylating Activity of Protein Tyrosine Phosphatases Using Microarrays with 3-Nitrophosphotyrosine Substrates
van Ameijde, J; Overvoorde, J; Knapp, S; den Hertog, J; Ruijtenbeek, R; Liskamp, RMJ;
ChemPlusChem. 2013 78:1349-1357. doi: 10.1002/cplu.201300299
PMID:

Small-molecule modulators for epigenetics targets.
Knapp, S; Weinmann, H;
ChemMedChem: chemistry enabling drug discovery. 2013 8:1885-1891. doi: 10.1002/cmdc.201300344
PMID: 24127276

Discovery of novel small-molecule inhibitors of BRD4 using structure-based virtual screening.
Vidler, LR; Filippakopoulos, P; Fedorov, O; Picaud, S; Martin, S; Tomsett, M; Woodward, H; Brown, N; Knapp, S; Hoelder, S;
Journal of Medicinal Chemistry. 2013 56:8073-8088. doi:
PMID: 24090311

Mechanism and consequence of the autoactivation of p38α mitogen-activated protein kinase promoted by TAB1
De Nicola, GF; Martin, ED; Chaikuad, A; Bassi, R; Clark, J; Martino, L; Verma, S; Sicard, P; Tata, R; Atkinson, RA; Knapp, S; Conte, MR; Marber, MS;
Nature Structural and Molecular Biology. 2013 20:1182-1192. doi: 10.1038/nsmb.2668
PMID:

Chemical probes for bromodomains outside the BET family
Brennan, PE; Martin, SJ; Monteiro, O; Fedorov, O; Knapp, S; Hay, D; Wells, C; Filippakopoulos, P; Picaud, S; Muller-Knapp, S; Keates, T; Yapp, C; Philpott, M; Schofield, C; Burgess-Brown, N; Shrestha, L; Strain-Damerell, C;
ACS National Meeting Book of Abstracts. 2013 246:-. doi:
PMID:

Topical antiangiogenic SRPK1 inhibitors reduce choroidal neovascularization in rodent models of exudative AMD.
Gammons, MV; Fedorov, O; Ivison, D; Du, C; Clark, T; Hopkins, C; Hagiwara, M; Dick, AD; Cox, R; Harper, SJ; Hancox, JC; Knapp, S; Bates, DO;
Investigative Ophthalmology and Visual Science. 2013 54:6052-6062. doi:
PMID: 23887803

BET inhibition as a single or combined therapeutic approach in primary paediatric B-precursor acute lymphoblastic leukaemia
Da Costa, D; Agathanggelou, A; Perry, T; Weston, V; Petermann, E; Zlatanou, A; Oldreive, C; Wei, W; Stewart, G; Longman, J; Smith, E; Kearns, P; Knapp, S; Stankovic, T;
Blood Cancer Journal. 2013 3:-. doi: 10.1038/bcj.2013.24
PMID: 23872705

Effect of Single Amino Acid Substitution Observed in Cancer on Pim-1 Kinase Thermodynamic Stability and Structure
Lori, C; Lantella, A; Pasquo, A; Alexander, LT; Knapp, S; Chiaraluce, R; Consalvi, V;
PLoS One. 2013 8:-. doi: 10.1371/journal.pone.0064824
PMID: 23755147

Selective Bisubstrate Inhibitors with Sub-nanomolar Affinity for Protein Kinase Pim-1
Ekambaram, R; Enkvist, E; Vaasa, A; Kasari, M; Raidaru, G; Knapp, S; Uri, A;
ChemMedChem: chemistry enabling drug discovery. 2013 8:909-913. doi: 10.1002/cmdc.201300042
PMID: 23616352

X-ray crystal structure of ERK5 (MAPK7) in complex with a specific inhibitor.
Elkins, JM; Wang, J; Deng, X; Pattison, MJ; Arthur, JS; Erazo, T; Gomez, N; Lizcano, JM; Gray, NS; Knapp, S;
Journal of Medicinal Chemistry. 2013 56:4413-4421. doi: 10.1021/jm4000837
PMID: 23656407

Restoring p53 function in human melanoma cells by inhibiting MDM2 and cyclin B1/CDK1-phosphorylated nuclear iASPP.
Lu, M; Breyssens, H; Salter, V; Zhong, S; Hu, Y; Baer, C; Ratnayaka, I; Sullivan, A; Brown, NR; Endicott, J; Knapp, S; Kessler, BM; Middleton, MR; Siebold, C; Jones, EY; Sviderskaya, EV; Cebon, J; John, T; Caballero, OL; Goding, CR; Lu, X;
Cancer Cell. 2013 23:618-633. doi: 10.1016/j.ccr.2013.03.013
PMID: 23623661

Structures of Down syndrome kinases, DYRKs, reveal mechanisms of kinase activation and substrate recognition.
Soundararajan, M; Roos, AK; Savitsky, P; Filippakopoulos, P; Kettenbach, AN; Olsen, JV; Gerber, SA; Eswaran, J; Knapp, S; Elkins, JM;
Structure. 2013 21:986-996. doi: 10.1016/j.str.2013.03.012
PMID: 23665168

PFI-1, a highly selective protein interaction inhibitor, targeting BET Bromodomains.
Picaud, S; Da Costa, D; Thanasopoulou, A; Filippakopoulos, P; Fish, PV; Philpott, M; Fedorov, O; Brennan, P; Bunnage, ME; Owen, DR; Bradner, JE; Taniere, P; O'Sullivan, B; Müller, S; Schwaller, J; Stankovic, T; Knapp, S;
Cancer Research. 2013 73:3336-3346. doi:
PMID: 23576556

Inhibition of BET Bromodomain Targets Genetically Diverse Glioblastoma
Cheng, Z; Gong, Y; Ma, Y; Lu, K; Lu, X; Pierce, LA; Thompson, RC; Muller, S; Knapp, S; Wang, J;
Clinical Cancer Research. 2013 19:1748-1759. doi: 10.1158/1078-0432.CCR-12-3066
PMID:

Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands.
Hewings, DS; Fedorov, O; Filippakopoulos, P; Martin, S; Picaud, S; Tumber, A; Wells, C; Olcina, MM; Freeman, K; Gill, A; Ritchie, AJ; Sheppard, DW; Russell, AJ; Hammond, EM; Knapp, S; Brennan, PE; Conway, SJ;
Journal of Medicinal Chemistry. 2013 56:3217-3227. doi:
PMID: 23517011

The Global Cancer Genomics Consortium's Second Annual Symposium: Genomics Medicine in Cancer Research
Kumar, R; Horvath, A; Mazumder, R; Toi, M; Sato, F; Pillai, MR; Costa, L; Carmo-Fonseca, M; Knapp, S; Dutt, A; Gupta, S; Badwe, R;
Genes and Cancer. 2013 4:196-200. doi: 10.1177/1947601913484582
PMID:

Structural basis for Cul3 protein assembly with the BTB-Kelch family of E3 ubiquitin ligases.
Canning, P; Cooper, CD; Krojer, T; Murray, JW; Pike, AC; Chaikuad, A; Keates, T; Thangaratnarajah, C; Hojzan, V; Ayinampudi, V; Marsden, BD; Gileadi, O; Knapp, S; von Delft, F; Bullock, AN;
Journal of Biological Chemistry. 2013 288:7803-7814. doi: 10.1074/jbc.M112.437996
PMID: 23349464

Novel Inverse Binding Mode of Indirubin Derivatives Yields Improved Selectivity for DYRK Kinases.
Myrianthopoulos, V; Kritsanida, M; Gaboriaud-Kolar, N; Magiatis, P; Ferandin, Y; Durieu, E; Lozach, O; Cappel, D; Soundararajan, M; Filippakopoulos, P; Sherman, W; Knapp, S; Meijer, L; Mikros, E; Skaltsounis, AL;
ACS Medicinal Chemistry Letters. 2013 4:22-26. doi: 10.1021/ml300207a
PMID: 23336033

3D Structure and Physiological Regulation of PAKs
K, S; n, ; a, ; p, ; p, ;
. 2013 :137-148. doi: 10.1016/B978-0-12-407198-8.00008-4
PMID:

The design and synthesis of 5- and 6-isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains.
Hay, D; Fedorov, O; Filippakopoulos, P; Martin, S; Philpott, M; Picaud, S; Hewings, DS; Uttakar, S; Heightman, TD; Conway, SJ; Knapp, S; Brennan, PE;
MedChemComm. 2013 4:140-144. doi:
PMID: 26682033

Structural insights into the activation of MST3 by MO25
Mehellou, Y; Alessi, DR; Macartney, TJ; Szklarz, M; Knapp, S; Elkins, JM;
Biochemical and Biophysical Research Communications. 2013 :-. doi:
PMID: 23296203

Construction of human activity-based phosphorylation networks
Newman, RH; Hu, J; Rho, HS; Xie, Z; Woodard, C; Neiswinger, J; Cooper, C; Shirley, M; Clark, HM; Hu, S; Hwang, W; Seop Jeong, J; Wu, G; Lin, J; Gao, X; Ni, Q; Goel, R; Xia, S; Ji, H; Dalby, KN; Birnbaum, MJ; Cole, PA; Knapp, S; Ryazanov, AG; Zack, DJ; Blackshaw, S; Pawson, T; Gingras, AC; Desiderio, S; Pandey, A; Turk, BE; Zhang, J; Zhu, H; Qian, J;
Molecular Systems Biology. 2013 9:-. doi: 10.1038/msb.2013.12
PMID: 23549483

2012

Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit.
Fish, PV; Filippakopoulos, P; Bish, G; Brennan, PE; Bunnage, ME; Cook, AS; Federov, O; Gerstenberger, BS; Jones, H; Knapp, S; Marsden, B; Nocka, K; Owen, DR; Philpott, M; Picaud, S; Primiano, MJ; Ralph, MJ; Sciammetta, N; Trzupek, JD;
Journal of Medicinal Chemistry. 2012 55:9831-9837. doi:
PMID: 23095041

A small-molecule inhibitor of Haspin alters the kinetochore functions of Aurora B
De Antoni, A; Maffini, S; Knapp, S; Musacchio, A; Santaguida, S;
The Journal of Cell Biology. 2012 199:269-284. doi: 10.1083/jcb.201205119
PMID: 23071153

INHIBITION OF BET BROMODOMAIN TARGETS GENETICALLY DIVERSE GLIOBLASTOMA
Cheng, Z; Gong, Y; Ma, Y; Ller-Knapp, SM; Knapp, S; Wang, J;
Clinical Cancer Research. 2012 14:28-28. doi:
PMID: 23403638

Progress in the development and application of small molecule inhibitors of bromodomain-acetyl-lysine interactions.
Hewings, DS; Rooney, TP; Jennings, LE; Hay, DA; Schofield, CJ; Brennan, PE; Knapp, S; Conway, SJ;
Journal of Medicinal Chemistry. 2012 55:9393-9413. doi: 10.1021/jm300915b
PMID: 22924434

Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B.
Tahtouh, T; Elkins, JM; Filippakopoulos, P; Soundararajan, M; Burgy, G; Durieu, E; Cochet, C; Schmid, RS; Lo, DC; Delhommel, F; Oberholzer, AE; Pearl, LH; Carreaux, F; Bazureau, JP; Knapp, S; Meijer, L;
Journal of Medicinal Chemistry. 2012 55:9312-9330. doi: 10.1021/jm301034u
PMID: 22998443

Crystal structure of human aurora B in complex with INCENP and VX-680.
Elkins, JM; Santaguida, S; Musacchio, A; Knapp, S;
Journal of Medicinal Chemistry. 2012 55:7841-7848. doi: 10.1021/jm3008954
PMID: 22920039

Structure of the bone morphogenetic protein receptor ALK2 and implications for fibrodysplasia ossificans progressiva.
Chaikuad, A; Alfano, I; Kerr, G; Sanvitale, CE; Boergermann, JH; Triffitt, JT; von Delft, F; Knapp, S; Knaus, P; Bullock, AN;
Journal of Biological Chemistry. 2012 287:36990-36998. doi: 10.1074/jbc.M112.365932
PMID: 22977237

Pharmacological inhibition of LIM kinase stabilizes microtubules and inhibits neoplastic growth.
Prudent, R; Vassal-Stermann, E; Nguyen, CH; Pillet, C; Martinez, A; Prunier, C; Barette, C; Soleilhac, E; Filhol, O; Beghin, A; Valdameri, G; Honoré, S; Aci-Sèche, S; Grierson, D; Antonipillai, J; Li, R; Di Pietro, A; Dumontet, C; Braguer, D; Florent, JC; Knapp, S; Bernard, O; Lafanechère, L;
Cancer Research. 2012 72:4429-4439. doi: 10.1158/0008-5472.CAN-11-3342
PMID: 22761334

Developing small molecule inhibitors of the CREBBP bromodomain-histone interaction
Rooney, TPC; Fedorov, O; Filippakopoulos, P; Wang, M; Philpott, M; Cook, A; Heightman, TD; Knapp, S; Pryde, D; Brennan, PE; Conway, SJ;
ACS National Meeting Book of Abstracts. 2012 244:-. doi:
PMID:

Small-molecule inhibition of BRDT for male contraception.
Matzuk, MM; McKeown, MR; Filippakopoulos, P; Li, Q; Ma, L; Agno, JE; Lemieux, ME; Picaud, S; Yu, RN; Qi, J; Knapp, S; Bradner, JE;
Cell. 2012 150:673-684. doi: 10.1016/j.cell.2012.06.045
PMID: 22901802

Leucettines, a family of pharmacological inhibitors of DYRKs & CLKs kinases derived from the marine sponge Leucettamine B
Tahtouh, T; Fedorov, O; Lozach, O; Carreaux, F; Bazureau, JP; Meunier, J; Maurice, T; Knapp, S; Meijer, L;
Planta Medica: natural products and medicinal plant research. 2012 78:1072-1072. doi:
PMID:

Versatile selective kinase inhibitors: Chemistry and biology of indirubins
Gaboriaud-Kolar, N; Magiatis, P; Brivanlou, A; Greengard, P; Knapp, S; Nam, S; Jove, R; Meijer, L; Mikros, E; Skaltsounis, AL;
Planta Medica: natural products and medicinal plant research. 2012 78:1080-1080. doi:
PMID:

Small-molecule inhibitors of the c-Fes protein-tyrosine kinase.
Hellwig, S; Miduturu, CV; Kanda, S; Zhang, J; Filippakopoulos, P; Salah, E; Deng, X; Choi, HG; Zhou, W; Hur, W; Knapp, S; Gray, NS; Smithgall, TE;
Chemistry and Biology. 2012 19:529-540. doi: 10.1016/j.chembiol.2012.01.020
PMID: 22520759

3,5-Dimethylisoxazoles inhibit the bromodomain-histone protein-protein interaction
Hewings, DS; Wang, M; Philpott, M; Fedorov, O; Uttarkar, S; Filippakopoulos, P; Picaud, S; Vuppusetty, C; Marsden, B; Heightman, TD; Knapp, S; Brennan, P; Conway, SJ;
ACS National Meeting Book of Abstracts. 2012 243:-. doi:
PMID:

Developing chemical probes for the BET bromodomains
Hewings, DS; Wang, M; Philpott, M; Fedorov, O; Uttarkar, S; Filippakopoulos, P; Picaud, S; Vuppusetty, C; Marsden, B; Heightman, TD; Knapp, S; Brennan, P; Conway, SJ;
ACS National Meeting Book of Abstracts. 2012 243:-. doi:
PMID:

The p53 cofactor Strap exhibits an unexpected TPR motif and oligonucleotide-binding (OB)-fold structure.
Adams, CJ; Pike, AC; Maniam, S; Sharpe, TD; Coutts, AS; Knapp, S; La Thangue, NB; Bullock, AN;
Proceedings of the National Academy of Sciences of USA. 2012 109:3778-3783. doi: 10.1073/pnas.1113731109
PMID: 22362889

Fragment screening of cyclin G-associated kinase by weak affinity chromatography
Meiby, E; Knapp, S; Elkins, JM; Ohlson, S;
Analytical and Bioanalytical Chemistry. 2012 :1-9. doi:
PMID: 22918538

Kinase inhibitor selectivity profiling using differential scanning fluorimetry.
Fedorov, O; Niesen, FH; Knapp, S;
Methods in Molecular Biology. 2012 795:109-118. doi:
PMID: 21960218

PIM kinases are progression markers and emerging therapeutic targets in diffuse large B-cell lymphoma
Brault, L; Menter, T; Obermann, EC; Knapp, S; Thommen, S; Schwaller, J; Tzankov, A;
British Journal of Cancer. 2012 :-. doi:
PMID: 22722314

Rapid determination of multiple linear kinase substrate motifs by mass spectrometry
Kettenbach, AN; Wang, T; Faherty, BK; Madden, DR; Knapp, S; Bailey-Kellogg, C; Gerber, SA;
Chemistry and Biology. 2012 19:608-618. doi: 10.1016/j.chembiol.2012.04.011
PMID: 22633412

Structural stability of human protein tyrosine phosphatase ρ catalytic domain: Effect of point mutations
Pasquo, A; Consalvi, V; Knapp, S; Alfano, I; Ardini, M; Stefanini, S; Chiaraluce, R;
PLoS One. 2012 7:-. doi: 10.1371/journal.pone.0032555
PMID: 22389709

The bromodomain interaction module
Filippakopoulos, P; Knapp, S;
FEBS Letters. 2012 586:2692-2704. doi: 10.1016/j.febslet.2012.04.045
PMID:

The Global Cancer Genomics Consortium: Interfacing genomics and cancer medicine
Eswaran, J; Gupta, S; Dutt, A; Toi, M; Pillai, MR; Costa, L; Knapp, S; Badwe, R; Kumar, R;
Cancer Research. 2012 72:3720-3724. doi: 10.1158/0008-5472.CAN-12-1054
PMID: 22628426

The therapeutic potential of acetyl-lysine and methyl-lysine effector domains
Brennan, P; Filippakopoulos, P; Knapp, S;
Drug Discovery Today: Therapeutic Strategies. 2012 :-. doi:
PMID:

The therapeutic potential of acetyl-lysine and methyl-lysine effector domains
Brennan, P; Filippakopoulos, P; Knapp, S;
Drug Discovery Today: Therapeutic Strategies. 2012 9:-. doi: 10.1016/j.ddstr.2012.04.001
PMID:

Bromodomain-containing protein 4 (BRD4) regulates RNA polymerase II serine 2 phosphorylation in human CD4+ T cells
Zhang, W; Prakash, C; Sum, C; Gong, Y; Li, Y; Kwok, JJT; Thiessen, N; Pettersson, S; Jones, SJM; Knapp, S; Yang, H; Chin, KC;
Journal of Biological Chemistry. 2012 287:43137-43155. doi: 10.1074/jbc.M112.413047
PMID: 23086925

Druggability analysis and structural classification of bromodomain acetyl-lysine binding sites
Vidler, LR; Brown, N; Knapp, S; Hoelder, S;
Journal of Medicinal Chemistry. 2012 55:7346-7359. doi: 10.1021/jm300346w
PMID: 22788793

7,8-dichloro-1-oxo-β-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes.
Huber, K; Brault, L; Fedorov, O; Gasser, C; Filippakopoulos, P; Bullock, AN; Fabbro, D; Trappe, J; Schwaller, J; Knapp, S; Bracher, F;
Journal of Medicinal Chemistry. 2012 55:403-413. doi:
PMID: 22136433

Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
Filippakopoulos, P; Picaud, S; Fedorov, O; Keller, M; Wrobel, M; Morgenstern, O; Bracher, F; Knapp, S;
Bioorganic and Medicinal Chemistry. 2012 20:1878-1886. doi:
PMID: 22137933

Analysis of conditions affecting auto-phosphorylation of human kinases during expression in bacteria.
Shrestha, A; Hamilton, G; O'Neill, E; Knapp, S; Elkins, JM;
Protein Expression and Purification. 2012 81:136-143. doi: 10.1016/j.pep.2011.09.012
PMID: 21985771

2011

Inhibition of BRD4 Bromodomains Is a Potent Novel Strategy to Target Apoptosis Resistance in Paediatric ALL
Da Costa, D; Weston, VJ; Wei, W; Agathanggelou, A; Petermann, E; Knapp, S; Kearns, PR; Stankovic, T;
Blood. 2011 118:37-37. doi:
PMID:

Bromodomains as therapeutic targets.
Muller, S; Filippakopoulos, P; Knapp, S;
Expert Reviews in Molecular Medicine. 2011 13:e29-. doi: 10.1017/S1462399411001992
PMID: 21933453

3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands.
Hewings, DS; Wang, M; Philpott, M; Fedorov, O; Uttarkar, S; Filippakopoulos, P; Picaud, S; Vuppusetty, C; Marsden, B; Knapp, S; Conway, SJ; Heightman, TD;
Journal of Medicinal Chemistry. 2011 54:6761-6770. doi:
PMID: 21851057

Bromodomain-peptide displacement assays for interactome mapping and inhibitor discovery.
Philpott, M; Yang, J; Tumber, T; Fedorov, O; Uttarkar, S; Filippakopoulos, P; Picaud, S; Keates, T; Felletar, I; Ciulli, A; Knapp, S; Heightman, TD;
Molecular Biosystems. 2011 7:2899-2908. doi: 10.1039/c1mb05099k
PMID: 21804994

High-throughput kinase profiling: a more efficient approach toward the discovery of new kinase inhibitors.
Miduturu, CV; Deng, X; Kwiatkowski, N; Yang, W; Brault, L; Filippakopoulos, P; Chung, E; Yang, Q; Schwaller, J; Knapp, S; King, RW; Lee, JD; Herrgard, S; Zarrinkar, P; Gray, NS;
Chemistry and Biology. 2011 18:868-879. doi: 10.1016/j.chembiol.2011.05.010
PMID: 21802008

Leucettines, a class of potent inhibitors of cdc2-like kinases and dual specificity, tyrosine phosphorylation regulated kinases derived from the marine sponge leucettamine B: modulation of alternative pre-RNA splicing.
Debdab, M; Carreaux, F; Renault, S; Soundararajan, M; Fedorov, O; Filippakopoulos, P; Lozach, O; Babault, L; Tahtouh, T; Baratte, B; Ogawa, Y; Hagiwara, M; Eisenreich, A; Rauch, U; Knapp, S; Meijer, L; Bazureau, JP;
Journal of Medicinal Chemistry. 2011 54:4172-4186. doi:
PMID: 21615147

New potent dual inhibitors of CK2 and Pim kinases: discovery and structural insights (September, pg 3175, 2010)
Lopez-Ramos, M; Prudent, R; Moucadel, V; Sautel, CF; Barette, C; Lafanechere, L; Mouawad, L; Grierson, D; Schmidt, F; Florent, J-C; Filippakopoulos, P; Bullock, AN; Knapp, S; Reiser, J-B; Cochet, C;
The FASEB Journal. 2011 25:1775-1775. doi: 10.1096/fj.09-143743err
PMID:

Crystal structures of ABL-related gene (ABL2) in complex with imatinib, tozasertib (VX-680), and a type I inhibitor of the triazole carbothioamide class.
Salah, E; Ugochukwu, E; Barr, AJ; von Delft, F; Knapp, S; Elkins, JM;
Journal of Medicinal Chemistry. 2011 54:2359-2367. doi: 10.1021/jm101506n
PMID: 21417343

Specific CLK inhibitors from a novel chemotype for regulation of alternative splicing.
Fedorov, O; Huber, K; Eisenreich, A; Filippakopoulos, P; King, O; Bullock, AN; Szklarczyk, D; Jensen, LJ; Fabbro, D; Trappe, J; Rauch, U; Bracher, F; Knapp, S;
Chemistry and Biology. 2011 18:67-76. doi:
PMID: 21276940

Bromodomain-peptide displacement assays for interactome mapping and inhibitor discovery.
Philpott, M; Yang, J; Tumber, T; Fedorov, O; Uttarkar, S; Filippakopoulos, P; Picaud, S; Keates, T; Felletar, I; Ciulli, A; Knapp, S; Heightman, TD;
Molecular Biosystems. 2011 7:2899-2908. doi:
PMID:

DNA damage in oocytes induces a switch of the quality control factor TAp63α from dimer to tetramer
Deutsch, GB; Zielonka, EM; Coutandin, D; Weber, TA; Schäfer, B; Hannewald, J; Luh, LM; Durst, FG; Ibrahim, M; Hoffmann, J; Niesen, FH; Sentürk, A; Kunkel, H; Brutschy, B; Schleiff, E; Knapp, S; Acker-Palmer, A; Grez, M; McKeon, F; Dötsch, V;
Cell. 2011 144:566-576. doi: 10.1016/j.cell.2011.01.013
PMID: 21335238

Structurally sophisticated octahedral metal complexes as highly selective protein kinase inhibitors
Feng, L; Geisselbrecht, Y; Blanck, S; Wilbuer, A; Atilla-Gokcumen, GE; Filippakopoulos, P; Kräling, K; Celik, MA; Harms, K; Maksimoska, J; Marmorstein, R; Frenking, G; Knapp, S; Essen, LO; Meggers, E;
Journal of the American Chemical Society. 2011 133:5976-5986. doi: 10.1021/ja1112996
PMID: 21446733

Structural basis for c-KIT inhibition by the suppressor of cytokine signaling 6 (SOCS6) ubiquitin ligase.
Zadjali, F; Pike, AC; Vesterlund, M; Sun, J; Wu, C; Li, SS; Rönnstrand, L; Knapp, S; Bullock, AN; Flores-Morales, A;
Journal of Biological Chemistry. 2011 286:480-490. doi: 10.1074/jbc.M110.173526
PMID: 21030588

2010

The PIM Kinase Inhibitor K00135 Sensitizes Primary Acute Lymphoblastic Leukaemia (ALL) Cells to DNA-Damaging Agents
Da Costa, D; Weston, VJ; Knapp, S; Taylor, AMR; Kearns, PR; Stankovic, T;
Blood. 2010 116:1328-1328. doi:
PMID:

Whole Kinome Profiling In Pediatric Acute Leukemia
Gombert, M; Krell, PFI; Linka, RM; Knapp, S; Borkhardt, A;
Blood. 2010 116:453-453. doi:
PMID:

Whole Kinome Profiling In Pediatric Acute Leukemia
Krell, PFI; Linka, RM; Knapp, S; Borkhardt, A;
Blood. 2010 116:453-453. doi:
PMID:

Selective inhibition of BET bromodomains.
Filippakopoulos, P; Qi, J; Picaud, S; Shen, Y; Smith, WB; Fedorov, O; Morse, EM; Keates, T; Hickman, TT; Felletar, I; Philpott, M; Munro, S; McKeown, MR; Wang, Y; Christie, AL; West, N; Cameron, MJ; Schwartz, B; Heightman, TD; La Thangue, N; French, CA; Wiest, O; Kung, AL; Knapp, S; Bradner, JE;
Nature. 2010 468:1067-1073. doi:
PMID: 20871596

Targeting kinases for the treatment of inflammatory diseases
Müller, S; Knapp, S;
Expert Opinion on Drug Discovery. 2010 5:867-881. doi: 10.1517/17460441.2010.504203
PMID: 22823261

Small-molecule bromodomain inhibitors for cancer therapy
Qi, J; Filippakopoulos, P; Picaud, S; Smith, W; Keates, T; Morse, E; Philpott, M; Shaw, K; Fedorov, O; West, N; Heightman, T; French, C; Knapp, S; Bradner, J;
ACS National Meeting Book of Abstracts. 2010 240:-. doi:
PMID:

Differential regulation of CaMKII inhibitor β protein expression after exposure to a novel context and during contextual fear memory formation
Radwańska, K; Tudor-Jones, AA; Mizuno, K; Pereira, GS; Lucchesi, W; Alfano, I; Łach, A; Kaczmarek, L; Knapp, S; Peter Giese, K;
Genes, Brain and Behavior. 2010 9:648-657. doi: 10.1111/j.1601-183X.2010.00595.x
PMID: 20487031

PIM serine/threonine kinases in the pathogenesis and therapy of hematologic malignancies and solid cancers.
Brault, L; Gasser, C; Bracher, F; Huber, K; Knapp, S; Schwaller, J;
Haematologica: the hematology journal. 2010 95:1004-1015. doi:
PMID: 20145274

Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function.
Kwiatkowski, N; Jelluma, N; Filippakopoulos, P; Soundararajan, M; Manak, MS; Kwon, M; Choi, HG; Sim, T; Deveraux, QL; Rottmann, S; Pellman, D; Shah, JV; Kops, GJ; Knapp, S; Gray, NS;
Nature Chemical Biology. 2010 6:359-368. doi: 10.1038/nchembio.345
PMID: 20383151

New potent dual inhibitors of CK2 and Pim kinases: discovery and structural insights.
López-Ramos, M; Prudent, R; Moucadel, V; Sautel, CF; Barette, C; Lafanechère, L; Mouawad, L; Grierson, D; Schmidt, F; Florent, JC; Filippakopoulos, P; Bullock, AN; Knapp, S; Reiser, JB; Cochet, C;
The FASEB Journal. 2010 24:3171-3185. doi: 10.1096/fj.09-143743
PMID: 20400536

The (un)targeted cancer kinome.
Fedorov, O; Müller, S; Knapp, S;
Nature Chemical Biology. 2010 6:166-169. doi:
PMID: 20154661

Structural comparison of human mammalian ste20-like kinases.
Record, CJ; Chaikuad, A; Rellos, P; Das, S; Pike, AC; Fedorov, O; Marsden, BD; Knapp, S; Lee, WH;
PLoS One. 2010 5:e11905-. doi:
PMID: 20730082

Structure of the CaMKIIdelta/calmodulin complex reveals the molecular mechanism of CaMKII kinase activation.
Rellos, P; Pike, AC; Niesen, FH; Salah, E; Lee, WH; von Delft, F; Knapp, S;
PLoS Biology. 2010 8:e1000426-. doi: 10.1371/journal.pbio.1000426
PMID: 20668654

Insights into protein kinase regulation and inhibition by large scale structural comparison.
Eswaran, J; Knapp, S;
Biochimica et Biophysica Acta: international journal of biochemistry and biophysics. 2010 1804:429-432. doi: 10.1016/j.bbapap.2009.10.013
PMID: 19854302

2009

Conformational stability and activity of p73 require a second helix in the tetramerization domain.
Coutandin, D; Löhr, F; Niesen, FH; Ikeya, T; Weber, TA; Schäfer, B; Zielonka, EM; Bullock, AN; Yang, A; Güntert, P; Knapp, S; McKeon, F; Ou, HD; Dötsch, V;
Cell Death and Differentiation. 2009 16:1582-1589. doi: 10.1038/cdd.2009.139
PMID: 19763140

SH2 domains: modulators of nonreceptor tyrosine kinase activity.
Filippakopoulos, P; Müller, S; Knapp, S;
Current Opinion in Structural Biology. 2009 19:643-649. doi: 10.1016/j.sbi.2009.10.001
PMID: 19926274

Structure and functional characterization of the atypical human kinase haspin.
Eswaran, J; Patnaik, D; Filippakopoulos, P; Wang, F; Stein, RL; Murray, JW; Higgins, JM; Knapp, S;
Proceedings of the National Academy of Sciences of USA. 2009 106:20198-20203. doi: 10.1073/pnas.0901989106
PMID: 19918057

Synthesis, kinase inhibitory potencies, and in vitro antiproliferative evaluation of new Pim kinase inhibitors.
Akué-Gédu, R; Rossignol, E; Azzaro, S; Knapp, S; Filippakopoulos, P; Bullock, AN; Bain, J; Cohen, P; Prudhomme, M; Anizon, F; Moreau, P;
Journal of Medicinal Chemistry. 2009 52:6369-6381. doi: 10.1021/jm901018f
PMID: 19788246

Propionate analogues of zearalenone bind to Hsp90.
Ugele, M; Sasse, F; Knapp, S; Fedorov, O; Zubriene, A; Matulis, D; Maier, ME;
ChemBioChem: a European journal of chemical biology. 2009 10:2203-2212. doi:
PMID: 19637143

Dissection of PIM serine/threonine kinases in FLT3-ITD-induced leukemogenesis reveals PIM1 as regulator of CXCL12-CXCR4-mediated homing and migration.
Grundler, R; Brault, L; Gasser, C; Bullock, AN; Dechow, T; Woetzel, S; Pogacic, V; Villa, A; Ehret, S; Berridge, G; Spoo, A; Dierks, C; Biondi, A; Knapp, S; Duyster, J; Schwaller, J;
Journal of Experimental Medicine. 2009 206:1957-1970. doi: 10.1084/jem.20082074
PMID: 19687226

Structural determinants of G-protein α subunit selectivity by regulator of G-protein signaling 2 (RGS2)
Kimple, AJ; Soundararajan, M; Hutsell, SQ; Roos, AK; Urban, DJ; Setola, V; Temple, BRS; Roth, BL; Knapp, S; Willard, FS; Siderovski, DP;
Journal of Biological Chemistry. 2009 284:19402-19411. doi: 10.1074/jbc.M109.024711
PMID: 19478087

STUDYING THE ROLE OF PIM KINASES IN FLT3-ITD-INDUCED LEUKEMIA REVEALED PIM1 AS REGULATOR OF CXCL12/CXCR4-MEDIATED HOMING AND MIGRATION
Brault, L; Grundler, R; Gasser, C; Bullock, AN; Ehret, S; Spoo, A; Dierks, C; Biondi, A; Knapp, S; Duyster, J; Schwaller, J;
Haematologica: the hematology journal. 2009 94:448-449. doi:
PMID:

Targeting group II PAKs in cancer and metastasis.
Eswaran, J; Soundararajan, M; Knapp, S;
Cancer and Metastasis Reviews. 2009 28:209-217. doi: 10.1007/s10555-008-9181-4
PMID: 19160016

Girls homozygous for an IL-2-inducible T cell kinase mutation that leads to protein deficiency develop fatal EBV-associated lymphoproliferation
Huck, K; Feyen, O; Niehues, T; Rüschendorf, F; Hübner, N; Laws, HJ; Telieps, T; Knapp, S; Wacker, HH; Meindl, A; Jumaa, H; Borkhardt, A;
Journal of Clinical Investigation. 2009 119:1350-1358. doi: 10.1172/JCI37901
PMID: 19425169

Missense mutation in the inducible T-cell kinase (ITK) leading to immunodeficiency and fatal immune dysregulation after EBV infection
Telieps, T; Huck, K; Feyen, O; Niehues, T; Rueschendorf, F; Huebner, N; Laws, HJ; Knapp, S; Wacker, HH; Meindl, A; Jumaa, H; Borkhardt, A;
Klinische Paediatrie: Zeitschrift fuer Klinik und Praxis. 2009 221:209-209. doi:
PMID:

Structure of dystrophia myotonica protein kinase.
Elkins, JM; Amos, A; Niesen, FH; Pike, AC; Fedorov, O; Knapp, S;
Protein Science. 2009 18:782-791. doi: 10.1002/pro.82
PMID: 19309729

Kinase domain insertions define distinct roles of CLK kinases in SR protein phosphorylation.
Bullock, AN; Das, S; Debreczeni, JE; Rellos, P; Fedorov, O; Niesen, FH; Guo, K; Papagrigoriou, E; Amos, AL; Cho, S; Turk, BE; Ghosh, G; Knapp, S;
Structure. 2009 17:352-362. doi:
PMID: 19278650

Identification of a novel primary immunodeficiency syndrome leading to an XLP-like phenotype in girls
Huck, K; Feyen, O; Rueschendorf, F; Knapp, S; Borkhardt, A;
European Journal of Pediatrics. 2009 168:380-380. doi:
PMID:

Large-scale structural analysis of the classical human protein tyrosine phosphatome.
Barr, AJ; Ugochukwu, E; Lee, WH; King, ON; Filippakopoulos, P; Alfano, I; Savitsky, P; Burgess-Brown, NA; Müller, S; Knapp, S;
Cell. 2009 136:352-363. doi: 10.1016/j.cell.2008.11.038
PMID: 19167335

Discovery of a potent and selective inhibitor for human carbonyl reductase 1 from propionate scanning applied to the macrolide zearalenone.
Zimmermann, TJ; Niesen, FH; Pilka, ES; Knapp, S; Oppermann, U; Maier, ME;
Bioorganic and Medicinal Chemistry. 2009 17:530-536. doi: 10.1016/j.bmc.2008.11.076
PMID: 19097799

HD-PTP is a catalytically inactive tyrosine phosphatase due to a conserved divergence in its phosphatase domain
Gingras, MC; Zhang, YL; Kharitidi, D; Barr, AJ; Knapp, S; Tremblay, ML; Pause, A;
PLoS One. 2009 4:-. doi: 10.1371/journal.pone.0005105
PMID: 19340315

Crystal structure of the PIM2 kinase in complex with an organoruthenium inhibitor.
Bullock, AN; Russo, S; Amos, A; Pagano, N; Bregman, H; Debreczeni, JE; Lee, WH; von Delft, F; Meggers, E; Knapp, S;
PLoS One. 2009 4:e7112-. doi: 10.1371/journal.pone.0007112
PMID: 19841674

2008

Extremely tight binding of a ruthenium complex to glycogen synthase kinase 3.
Atilla-Gokcumen, GE; Pagano, N; Streu, C; Maksimoska, J; Filippakopoulos, P; Knapp, S; Meggers, E;
ChemBioChem: a European journal of chemical biology. 2008 9:2933-2936. doi: 10.1002/cbic.200800489
PMID: 19035373

Dissecting Proto-Oncogenic PIM Serine/Threonine Kinases in FLT3-ITD-Induced Leukemogenesis: PIM1 Regulates CXCL12/CXCR4-Mediated Homing and Migration
Gasser, C; Grundler, R; Brault, L; Bullock, A; Dechow, T; Nawijn, M; Woetzel, S; Ehret, S; Berridge, G; Spoo, A; Dierks, C; Biondi, A; Knapp, S; Duyster, J; Schwaller, J;
Blood. 2008 112:1299-1299. doi:
PMID:

Structural coupling of SH2-kinase domains links Fes and Abl substrate recognition and kinase activation.
Filippakopoulos, P; Kofler, M; Hantschel, O; Gish, GD; Grebien, F; Salah, E; Neudecker, P; Kay, LE; Turk, BE; Superti-Furga, G; Pawson, T; Knapp, S;
Cell. 2008 134:793-803. doi: 10.1016/j.cell.2008.07.047
PMID: 18775312

Linear Motif Atlas for Phosphorylation-Dependent Signaling
Miller, ML; Jensen, LJ; Diella, F; Jorgensen, C; Tinti, M; Li, L; Hsiung, M; Parker, SA; Bordeaux, J; Sicheritz-Ponten, T; Olhovsky, M; Pasculescu, A; Alexander, J; Knapp, S; Blom, N; Bork, P; Li, S; Cesareni, G; Pawson, T; Turk, BE; Yaffe, MB; Brunak, S; Linding, R;
Science Signaling. 2008 1:-. doi: 10.1126/scisignal.1159433
PMID: 18765831

UnPAKing the class differences among p21-activated kinases.
Eswaran, J; Soundararajan, M; Kumar, R; Knapp, S;
Trends in Biochemical Sciences. 2008 33:394-403. doi: 10.1016/j.tibs.2008.06.002
PMID: 18639460

The structure of P-TEFb (CDK9/cyclin T1), its complex with flavopiridol and regulation by phosphorylation.
Baumli, S; Lolli, G; Lowe, ED; Troiani, S; Rusconi, L; Bullock, AN; Debreczeni, JE; Knapp, S; Johnson, LN;
The EMBO Journal. 2008 27:1907-1918. doi: 10.1038/emboj.2008.121
PMID: 18566585

Activation segment dimerization: a mechanism for kinase autophosphorylation of non-consensus sites.
Pike, AC; Rellos, P; Niesen, FH; Turnbull, A; Oliver, AW; Parker, SA; Turk, BE; Pearl, LH; Knapp, S;
The EMBO Journal. 2008 27:704-714. doi: 10.1038/emboj.2008.8
PMID: 18239682

Doing more than just the structure-structural genomics in kinase drug discovery.
Marsden, BD; Knapp, S;
Current Opinion in Chemical Biology. 2008 12:40-45. doi: 10.1016/j.cbpa.2008.01.042
PMID: 18267130

Thermal unfolding of the archaeal DNA and RNA binding protein Ssh10.
Wu, X; Oppermann, M; Berndt, KD; Bergman, T; Jörnvall, H; Knapp, S; Oppermann, U;
Biochemical and Biophysical Research Communications. 2008 373:482-487. doi: 10.1016/j.bbrc.2008.06.030
PMID: 18571501

Similar biological activities of two isostructural ruthenium and osmium complexes.
Maksimoska, J; Williams, DS; Atilla-Gokcumen, GE; Smalley, KS; Carroll, PJ; Webster, RD; Filippakopoulos, P; Knapp, S; Herlyn, M; Meggers, E;
Chemistry: A European Journal. 2008 14:4816-4822. doi: 10.1002/chem.200800294
PMID: 18425743

Structure of the human protein kinase MPSK1 reveals an atypical activation loop architecture.
Eswaran, J; Bernad, A; Ligos, JM; Guinea, B; Debreczeni, JE; Sobott, F; Parker, SA; Najmanovich, R; Turk, BE; Knapp, S;
Structure. 2008 16:115-124. doi: 10.1016/j.str.2007.10.026
PMID: 18184589

2007

A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
Fedorov, O; Marsden, B; Pogacic, V; Rellos, P; Müller, S; Bullock, AN; Schwaller, J; Sundström, M; Knapp, S;
Proceedings of the National Academy of Sciences of USA. 2007 104:20523-20528. doi:
PMID: 18077363

Structural and functional characterization of the human protein kinase ASK1.
Bunkoczi, G; Salah, E; Filippakopoulos, P; Fedorov, O; Müller, S; Sobott, F; Parker, SA; Zhang, H; Min, W; Turk, BE; Knapp, S;
Structure. 2007 15:1215-1226. doi:
PMID: 17937911

The scientific impact of the Structural Genomics Consortium: a protein family and ligand-centered approach to medically-relevant human proteins.
Gileadi, O; Knapp, S; Lee, WH; Marsden, BD; Müller, S; Niesen, FH; Kavanagh, KL; Ball, LJ; von Delft, F; Doyle, DA; Oppermann, UC; Sundström, M;
Journal of Structural and Functional Genomics. 2007 8:107-119. doi: 10.1007/s10969-007-9027-2
PMID: 17932789

Activation segment exchange: a common mechanism of kinase autophosphorylation?
Oliver, AW; Knapp, S; Pearl, LH;
Trends in Biochemical Sciences. 2007 32:351-356. doi: 10.1016/j.tibs.2007.06.004
PMID: 17627826

Structural analysis identifies imidazo[1,2-b]pyridazines as PIM kinase inhibitors with in vitro antileukemic activity.
Pogacic, V; Bullock, AN; Fedorov, O; Filippakopoulos, P; Gasser, C; Biondi, A; Meyer-Monard, S; Knapp, S; Schwaller, J;
Cancer Research. 2007 67:6916-6924. doi:
PMID: 17638903

Protein-protein interaction site mapping using NMR-detected mutational scanning
Baminger, B; Ludwiczek, ML; Kontaxis, G; Knapp, S; Konrat, R;
Journal of Biomolecular NMR. 2007 38:133-137. doi: 10.1007/s10858-007-9154-x
PMID: 17447011

Specificity profiling of Pak kinases allows identification of novel phosphorylation sites
Rennefahrt, UEE; Deacon, SW; Parker, SA; Devarajan, K; Beeser, A; Chernoff, J; Knapp, S; Turk, BE; Peterson, JR;
Journal of Biological Chemistry. 2007 282:15667-15678. doi: 10.1074/jbc.M700253200
PMID: 17392278

Structures of the human eIF4E homologous protein, h4EHP, in its m7GTP-bound and unliganded forms.
Rosettani, P; Knapp, S; Vismara, MG; Rusconi, L; Cameron, AD;
Journal of Molecular Biology. 2007 368:691-705. doi: 10.1016/j.jmb.2007.02.019
PMID: 17368478

Insights for the development of specific kinase inhibitors by targeted structural genomics.
Fedorov, O; Sundström, M; Marsden, B; Knapp, S;
Drug Discovery Today. 2007 12:365-372. doi:
PMID: 17467572

Structure and regulation of the human Nek2 centrosomal kinase.
Rellos, P; Ivins, FJ; Baxter, JE; Pike, A; Nott, TJ; Parkinson, DM; Das, S; Howell, S; Fedorov, O; Shen, QY; Fry, AM; Knapp, S; Smerdon, SJ;
Journal of Biological Chemistry. 2007 282:6833-6842. doi:
PMID: 17197699

Biochemical characterization of TASSELSEED 2, an essential plant short-chain dehydrogenase/reductase with broad spectrum activities.
Wu, X; Knapp, S; Stamp, A; Stammers, DK; Jörnvall, H; Dellaporta, SL; Oppermann, U;
The Federation of European Biochemical Societies (FEBS) Journal. 2007 274:1172-1182. doi: 10.1111/j.1742-4658.2007.05642.x
PMID: 17298439

Crystal Structures of the p21-activated kinases PAK4, PAK5, and PAK6 reveal catalytic domain plasticity of active group II PAKs.
Eswaran, J; Lee, WH; Debreczeni, JE; Filippakopoulos, P; Turnbull, A; Fedorov, O; Deacon, SW; Peterson, JR; Knapp, S;
Structure. 2007 15:201-213. doi:
PMID: 17292838

2006

MAPK-specific tyrosine phosphatases: new targets for drug discovery?
Barr, AJ; Knapp, S;
Trends in Pharmacological Sciences. 2006 27:525-530. doi: 10.1016/j.tips.2006.08.005
PMID: 16919785

Crystal structure of human protein tyrosine phosphatase 14 (PTPN14) at 1.65-A resolution.
Barr, AJ; Debreczeni, JE; Eswaran, J; Knapp, S;
Proteins: Structure, Function, and Bioinformatics. 2006 63:1132-1136. doi: 10.1002/prot.20958
PMID: 16534812

The crystal structure of human receptor protein tyrosine phosphatase kappa phosphatase domain 1.
Eswaran, J; Debreczeni, JE; Longman, E; Barr, AJ; Knapp, S;
Protein Science. 2006 15:1500-1505. doi: 10.1110/ps.062128706
PMID: 16672235

The molecular mechanism of nitrogen-containing bisphosphonates as antiosteoporosis drugs.
Kavanagh, KL; Guo, K; Dunford, JE; Wu, X; Knapp, S; Ebetino, FH; Rogers, MJ; Russell, RG; Oppermann, U;
Proceedings of the National Academy of Sciences of USA. 2006 103:7829-7834. doi: 10.1073/pnas.0601643103
PMID: 16684881

Crystal structures and inhibitor identification for PTPN5, PTPRR and PTPN7: a family of human MAPK-specific protein tyrosine phosphatases.
Eswaran, J; von Kries, JP; Marsden, B; Longman, E; Debreczeni, JE; Ugochukwu, E; Turnbull, A; Lee, WH; Knapp, S; Barr, AJ;
Biochemical Journal. 2006 395:483-491. doi: 10.1042/BJ20051931
PMID: 16441242

Crystal structures and molecular interactions of risedronate and zoledronate with human farnesyl diphosphate synthase
Kavanagh, KL; Guo, K; Wu, X; Knapp, S; Ebetino, FH; Dunford, JE; Rogers, MJ; Russell, RGG; Oppermann, U;
Bone. 2006 38:53-53. doi: 10.1016/j.bone.2005.12.050
PMID:

Ruthenium half-sandwich complexes bound to protein kinase Pim-1.
Debreczeni, JE; Bullock, AN; Atilla, GE; Williams, DS; Bregman, H; Knapp, S; Meggers, E;
Angewandte Chemie International Edition. 2006 45:1580-1585. doi: 10.1002/anie.200503468
PMID: 16381041

Inhibition of protein-protein interactions: The discovery of druglike β-catenin inhibitors by combining virtual and biophysical screening
Trosset, JY; Dalvit, C; Knapp, S; Fasolini, M; Veronesi, M; Mantegani, S; Gianellini, LM; Catana, C; Sundström, M; Stouten, PFW; Moll, JK;
Proteins: Structure, Function, and Bioinformatics. 2006 64:60-67. doi: 10.1002/prot.20955
PMID: 16568448

High-throughput structural characterisation of therapeutic protein targets
Marsden, BD; Sundstrom, M; Knapp, S;
Expert Opinion on Drug Discovery. 2006 1:123-136. doi: 10.1517/17460441.1.2.123
PMID:

2005

Structure and substrate specificity of the Pim-1 kinase.
Bullock, AN; Debreczeni, J; Amos, AL; Knapp, S; Turk, BE;
Journal of Biological Chemistry. 2005 280:41675-41682. doi: 10.1074/jbc.M510711200
PMID: 16227208

Structural basis of inhibitor specificity of the human protooncogene proviral insertion site in moloney murine leukemia virus (PIM-1) kinase.
Bullock, AN; Debreczeni, JE; Fedorov, OY; Nelson, A; Marsden, BD; Knapp, S;
Journal of Medicinal Chemistry. 2005 48:7604-7614. doi:
PMID: 16302800

Human farnesyl diphosphate synthase (FDFS): Crystal structure and molecular interactions with Nnitrogen-containing bisphosphonates.
Kavanagh, K; Guo, K; Wu, X; Knapp, S; Ebetino, FH; Dunford, JE; Rogers, MJ; Russell, RGG; Oppermann, U;
Journal of Bone and Mineral Research. 2005 20:S95-S96. doi:
PMID:

Regulation of the wild-type and Y1235D mutant met kinase activation
Cristiani, C; Rusconi, L; Perego, R; Schiering, N; Kalisz, HM; Knapp, S; Isacchi, A;
Biochemistry. 2005 44:14110-14119. doi: 10.1021/bi051242k
PMID: 16245927

2004

Coupling PAF signaling to dynein regulation: Structure of LIS1 in complex with PAF-acetylhydrolase
Tarricone, C; Perrina, F; Monzani, S; Massimiliano, L; Kim, MH; Derewenda, ZS; Knapp, S; Tsai, LH; Musacchio, A;
Neuron. 2004 44:809-821. doi: 10.1016/j.neuron.2004.11.019
PMID: 15572112

2003

Crystal structure of the tyrosine kinase domain of the hepatocyte growth factor receptor c-Met and its complex with the microbial alkaloid K-252a.
Schiering, N; Knapp, S; Marconi, M; Flocco, MM; Cui, J; Perego, R; Rusconi, L; Cristiani, C;
Proceedings of the National Academy of Sciences of USA. 2003 100:12654-12659. doi: 10.1073/pnas.1734128100
PMID: 14559966

Structural characterization of the GSK-3beta active site using selective and non-selective ATP-mimetic inhibitors.
Bertrand, JA; Thieffine, S; Vulpetti, A; Cristiani, C; Valsasina, B; Knapp, S; Kalisz, HM; Flocco, M;
Journal of Molecular Biology. 2003 333:393-407. doi:
PMID: 14529625

Protein stabilisation by compatible solutes: Effect of mannosylglycerate on unfolding thermodynamics and activity of ribonuclease A
Faria, TQ; Knapp, S; Ladenstein, R; Maçanita, AL; Santos, H;
ChemBioChem: a European journal of chemical biology. 2003 4:734-741. doi: 10.1002/cbic.200300574
PMID: 12898624

Inhibitor affinity chromatography: profiling the specific reactivity of the proteome with immobilized molecules.
Lolli, G; Thaler, F; Valsasina, B; Roletto, F; Knapp, S; Uggeri, M; Bachi, A; Matafora, V; Storici, P; Stewart, A; Kalisz, HM; Isacchi, A;
Proteomics. 2003 3:1287-1298. doi: 10.1002/pmic.200300431
PMID: 12872229

Hot spots in Tcf4 for the interaction with beta-catenin.
Fasolini, M; Wu, X; Flocco, M; Trosset, JY; Oppermann, U; Knapp, S;
Journal of Biological Chemistry. 2003 278:21092-21098. doi: 10.1074/jbc.M301781200
PMID: 12657632

2002

Critical residues for structure and catalysis in short-chain dehydrogenases/reductases.
Filling, C; Berndt, KD; Benach, J; Knapp, S; Prozorovski, T; Nordling, E; Ladenstein, R; Jörnvall, H; Oppermann, U;
Journal of Biological Chemistry. 2002 277:25677-25684. doi: 10.1074/jbc.M202160200
PMID: 11976334

High-throughput NMR-based screening with competition binding experiments.
Dalvit, C; Flocco, M; Knapp, S; Mostardini, M; Perego, R; Stockman, BJ; Veronesi, M; Varasi, M;
Journal of the American Chemical Society. 2002 124:7702-7709. doi:
PMID: 12083923

NMR-Based screening with competition water-ligand observed via gradient spectroscopy experiments: detection of high-affinity ligands.
Dalvit, C; Fasolini, M; Flocco, M; Knapp, S; Pevarello, P; Veronesi, M;
Journal of Medicinal Chemistry. 2002 45:2610-2614. doi:
PMID: 12036370

Crystal structure of the tetrameric Mad1-Mad2 core complex: implications of 'safety belt' binding mechanism for the spindle checkpoint
Sironi, L; Mapelli, M; Knapp, S; De Antoni, A; Jeang, KT; Musacchio, A;
The EMBO Journal. 2002 21:2496-2506. doi: 10.1093/emboj/21.10.2496
PMID: 12006501

2001

Thermodynamics of HMGB1 interaction with duplex DNA.
Müller, S; Bianchi, ME; Knapp, S;
Biochemistry. 2001 40:10254-10261. doi:
PMID: 11513603

Thermodynamics of the high-affinity interaction of TCF4 with beta-catenin.
Knapp, S; Zamai, M; Volpi, D; Nardese, V; Avanzi, N; Breton, J; Plyte, S; Flocco, M; Marconi, M; Isacchi, A; Caiolfa, VR;
Journal of Molecular Biology. 2001 306:1179-1189. doi: 10.1006/jmbi.2001.4463
PMID: 11237626

2000

Thermal unfolding and conformational stability of the recombinant domain II of glutamate dehydrogenase from the hyperthermophile Thermotoga maritima
Consalvi, V; Chiaraluce, R; Giangiacomo, L; Scandurra, R; Christova, P; Karshikoff, A; Knapp, S; Ladenstein, R;
Protein Engineering Design and Selection. 2000 13:501-507. doi: 10.1093/protein/13.7.501
PMID: 10906345

1999

The staphylococcal alpha-toxin pore has a flexible conformation.
Vécsey-Semjén, B; Knapp, S; Möllby, R; van der Goot, FG;
Biochemistry. 1999 38:4296-4302. doi: 10.1021/bi982472k
PMID: 10194347

1998

Isolation and structure of repressor-like proteins from the archaeon Sulfolobus solfataricus. Co-purification of RNase A with Sso7c.
Oppermann, UC; Knapp, S; Bonetto, V; Ladenstein, R; Jörnvall, H;
FEBS Letters. 1998 432:141-144. doi:
PMID: 9720912

Thermal unfolding of small proteins with SH3 domain folding pattern
Knapp, S; Mattson, PT; Christova, P; Berndt, KD; Karshikoff, A; Vihinen, M; Smith, CIE; Ladenstein, R;
Proteins: Structure, Function, and Bioinformatics. 1998 31:309-319. doi: 10.1002/(SICI)1097-0134(19980515)31:3<309::AID-PROT7>3.0.CO;2-D
PMID: 9593201

1996

Thermal unfolding of the DNA-binding protein Sso7d from the hyperthermophile Sulfolobus solfataricus
Knapp, S; Karshikoff, A; Berndt, KD; Christova, P; Atanasov, B; Ladenstein, R;
Journal of Molecular Biology. 1996 264:1132-1144. doi: 10.1006/jmbi.1996.0701
PMID: 9000635

1994

THE MOLECULAR CHAPERONIN TF55 FROM THE THERMOPHILIC ARCHAEON SULFOLOBUS-SOLFATARICUS - A BIOCHEMICAL AND STRUCTURAL CHARACTERIZATION
KNAPP, S; SCHMIDTKREY, I; HEBERT, H; BERGMAN, T; JORNVALL, H; LADENSTEIN, R;
Journal of Molecular Biology. 1994 242:397-407. doi:
PMID: 7932699

2 DISTINCT FACTORS BIND TO THE RABBIT UTEROGLOBIN TATA-BOX REGION AND ARE REQUIRED FOR EFFICIENT TRANSCRIPTION
KLUG, J; KNAPP, S; CASTRO, I; BEATO, M;
Molecular and Cellular Biology. 1994 14:6208-6218. doi:
PMID:

Two distinct factors bind to the rabbit uteroglobin TATA-box region and are required for efficient transcription.
Klug, J; Knapp, S; Castro, I; Beato, M;
Molecular and Cellular Biology. 1994 14:6208-6218. doi:
PMID: 8065353

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