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Displaying 1 - 50 of 959

2016

Discovery of a Potent Class I Protein Arginine Methyltransferase Fragment Inhibitor.
Ferreira de Freitas R, Eram MS, Szewczyk MM, Steuber H, Smil D, Wu H, Li F, Senisterra G, Dong A, Brown PJ, Hitchcock M, Moosmayer D, Stegmann CM, Egner U, Arrowsmith C, Barsyte-Lovejoy D, Vedadi M, Schapira M
J. Med. Chem.. 29.01.2016 . doi: 10.1021/acs.jmedchem.5b01772
PMID: 26824386

A cellular chemical probe targeting the chromodomains of Polycomb repressive complex 1.
Stuckey JI, Dickson BM, Cheng N, Liu Y, Norris JL, Cholensky SH, Tempel W, Qin S, Huber KG, Sagum C, Black K, Li F, Huang XP, Roth BL, Baughman BM, Senisterra G, Pattenden SG, Vedadi M, Brown PJ, Bedford MT, Min J, Arrowsmith CH, James LI, Frye SV
Nat. Chem. Biol.. 25.01.2016 . doi: 10.1038/nchembio.2007
PMID: 26807715

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. 5.1.2016 :-. doi:
PMID: 26731131

Genome-wide profiling of histone H3 lysine 27 and lysine 4 trimethylation in multiple myeloma reveals the importance of Polycomb gene targeting and highlights EZH2 as a potential therapeutic target.
Agarwal P, Alzrigat M, Párraga AA, Enroth S, Singh U, Ungerstedt J, Österborg A, Brown PJ, Ma A, Jin J, Nilsson K, Öberg F, Kalushkova A, Jernberg-Wiklund H
Oncotarget. 07.01.2016 . doi: 10.18632/oncotarget.6843
PMID: 26755663

Profiling of Small Molecules by Chemical Proteomics.
Huber, KV; Superti-Furga, G;
Methods in Molecular Biology. 01.1.2016 1394:211-218. doi: 10.1007/978-1-4939-3341-9_15
PMID: 26700051

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. 01.1.2016 34:95-103. doi: 10.1038/nbt.3374
PMID: 26501955

2015

SMN and symmetric arginine dimethylation of RNA polymerase II C-terminal domain control termination.
Yanling Zhao D, Gish G, Braunschweig U, Li Y, Ni Z, Schmitges FW, Zhong G, Liu K, Li W, Moffat J, Vedadi M, Min J, Pawson TJ, Blencowe BJ, Greenblatt JF
Nature. 23.12.2015 . doi: 10.1038/nature16469
PMID: 26700805

A Radioactivity-Based Assay for Screening Human m6A-RNA Methyltransferase, METTL3-METTL14 Complex, and Demethylase ALKBH5.
Li F, Kennedy S, Hajian T, Gibson E, Seitova A, Xu C, Arrowsmith CH, Vedadi M
J Biomol Screen. 23.12.2015 . doi: 10.1177/1087057115623264
PMID: 26701100

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. 01.12.2015 75:5106-5119. doi: 10.1158/0008-5472.can-15-0236
PMID: 26552700

MLL5 Orchestrates a Cancer Self-Renewal State by Repressing the Histone Variant H3.3 and Globally Reorganizing Chromatin.
Gallo M, Coutinho FJ, Vanner RJ, Gayden T, Mack SC, Murison A, Remke M, Li R, Takayama N, Desai K, Lee L, Lan X, Park NI, Barsyte-Lovejoy D, Smil D, Sturm D, Kushida MM, Head R, Cusimano MD, Bernstein M, Clarke ID, Dick JE, Pfister SM, Rich JN, Arrowsmith CH, Taylor MD, Jabado N, Bazett-Jones DP, Lupien M, Dirks PB
Cancer Cell. 25.11.2015 . doi: 10.1016/j.ccell.2015.10.005
PMID: 26626085

A Potent, Selective and Cell-active Inhibitor of Human Type I Protein Arginine Methyltransferases.
Eram MS, Shen Y, Szewczyk M, Wu H, Senisterra G, Li F, Butler KV, Kaniskan HÜ, Speed BA, Dela Seña C, Dong A, Zeng H, Schapira M, Brown PJ, Arrowsmith CH, Barsyte-Lovejoy D, Liu J, Vedadi M, Jin J
ACS Chem. Biol.. 24.11.2015 . doi: 10.1021/acschembio.5b00839
PMID: 26598975

Chemical basis for the recognition of trimethyllysine by epigenetic reader proteins.
Kamps JJ, Huang J, Poater J, Xu C, Pieters BJ, Dong A, Min J, Sherman W, Beuming T, Matthias Bickelhaupt F, Li H, Mecinović J
Nat Commun. 19.11.2015 6:8911. doi: 10.1038/ncomms9911
PMID: 26578293

Design of a fluorescent ligand targeting the S-adenosylmethionine binding site of the histone methyltransferase MLL1.
Luan Y, Blazer LL, Hu H, Hajian T, Zhang J, Wu H, Houliston S, Arrowsmith CH, Vedadi M, Zheng YG
Org. Biomol. Chem.. 06.11.2015 . doi: 10.1039/c5ob01794g
PMID: 26541578

Structural basis for substrate recognition by the human N-terminal methyltransferase 1.
Dong C, Mao Y, Tempel W, Qin S, Li L, Loppnau P, Huang R, Min J
Genes Dev.. 05.11.2015 . doi: 10.1101/gad.270611.115
PMID: 26543161

Structural basis for the regulatory role of the PPxY motifs in the thioredoxin-interacting protein TXNIP.
Liu Y, Lau J, Li W, Tempel W, Li L, Dong A, Narula A, Qin S, Min J
Biochem. J.. 02.11.2015 . doi: 10.1042/BJ20150830
PMID: 26527736

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. 13.11.2015 1:e1500723-. doi: 10.1126/sciadv.1500723
PMID: 26702435

The ins and outs of selective kinase inhibitor development.
Müller, S; Chaikuad, A; Gray, NS; Knapp, S;
Nature Chemical Biology. 01.11.2015 11:818-821. doi: 10.1038/nchembio.1938
PMID: 26485069

New Insights into the RNA-Binding and E3 Ubiquitin Ligase Activities of Roquins.
Zhang Q, Fan L, Hou F, Dong A, Wang YX, Tong Y
Sci Rep. 23.10.2015 5:15660. doi: 10.1038/srep15660
PMID: 26489670

STRUCTURAL BIOLOGY. Chromatin complex, crystal clear.
Schapira M
Science. 16.10.2015 350(6258):278-9. doi: 10.1126/science.aad5203
PMID: 26472895

WDR5 supports an N-Myc transcriptional complex that drives a pro-tumorigenic gene expression signature in neuroblastoma.
Sun Y, Bell JL, Carter DR, Gherardi S, Poulos RC, Milazzo G, Wong JW, Al-Awar R, Tee AE, Liu PY, Liu B, Atmadibrata B, Wong M, Trahair T, Zhao Q, Shohet JM, Haupt Y, Schulte JH, Brown PJ, Arrowsmith CH, Vedadi M, MacKenzie KL, Huttelmaier S, Perini G, Marshall GM, Braithwaite A, Liu T
Cancer Res.. 15.10.2015 . doi: 10.1158/0008-5472.CAN-15-0423
PMID: 26471359

Targeting RIPK1,2,3 to combat inflammation.
Bullock, AN; Degterev, A;
Oncotarget. 13.10.2015 6:34057-34058. doi: 10.18632/oncotarget.6106
PMID: 26472031

Streamlining the Pipeline for Generation of Recombinant Affinity Reagents by Integrating the Affinity Maturation Step.
Huang R, Gorman KT, Vinci CR, Dobrovetsky E, Gräslund S, Kay BK
Int J Mol Sci. 06.10.2015 16(10):23587-603. doi: 10.3390/ijms161023587
PMID: 26437402

Optimizing Production of Antigens and Fabs in the Context of Generating Recombinant Antibodies to Human Proteins.
Zhong N, Loppnau P, Seitova A, Ravichandran M, Fenner M, Jain H, Bhattacharya A, Hutchinson A, Paduch M, Lu V, Olszewski M, Kossiakoff AA, Dowdell E, Koide A, Koide S, Huang H, Nadeem V, Sidhu SS, Greenblatt JF, Marcon E, Arrowsmith CH, Edwards AM, Gräslund S
PLoS ONE. 05.10.2015 10(10):e0139695. doi: 10.1371/journal.pone.0139695
PMID: 26437229

Open access chemical probes for epigenetic targets.
Brown PJ, Müller S
Future Med Chem. 23.09.2015 . doi: 10.4155/fmc.15.127
PMID: 26397018

Proteome-wide drug and metabolite interaction mapping by thermal-stability profiling.
Huber, KV; Olek, KM; Müller, AC; Tan, CS; Bennett, KL; Colinge, J; Superti-Furga, G;
Nature Methods. 01.11.2015 12:1055-1057. doi: 10.1038/nmeth.3590
PMID: 26389571

Crystal structure of human nuclear pore complex component NUP43.
Xu C, Li Z, He H, Wernimont A, Li Y, Loppnau P, Min J
FEBS Lett.. 19.09.2015 . doi: 10.1016/j.febslet.2015.09.008
PMID: 26391640

WONKA: objective novel complex analysis for ensembles of protein-ligand structures.
Bradley, AR; Wall, ID; von Delft, F; Green, DV; Deane, CM; Marsden, BD;
Journal of Computer-Aided Molecular Design. 01.10.2015 29:963-973. doi: 10.1007/s10822-015-9866-z
PMID: 26387008

Gain-of-function p53 mutants co-opt chromatin pathways to drive cancer growth.
Zhu J, Sammons MA, Donahue G, Dou Z, Vedadi M, Getlik M, Barsyte-Lovejoy D, Al-awar R, Katona BW, Shilatifard A, Huang J, Hua X, Arrowsmith CH, Berger SL
Nature. 10.09.2015 525(7568):206-11. doi: 10.1038/nature15251
PMID: 26331536

Proteomic and Biochemical Studies of Lysine Malonylation Suggest Its Malonic Aciduria-associated Regulatory Role in Mitochondrial Function and Fatty Acid Oxidation.
Colak, G; Pougovkina, O; Dai, L; Tan, M; Te Brinke, H; Huang, H; Cheng, Z; Park, J; Wan, X; Liu, X; Yue, WW; Wanders, RJ; Locasale, JW; Lombard, DB; de Boer, VC; Zhao, Y;
Molecular and Cellular Proteomics. 01.11.2015 14:3056-3071. doi: 10.1074/mcp.m115.048850
PMID: 26320211

The inhibition of human farnesyl pyrophosphate synthase by nitrogen-containing bisphosphonates. Elucidating the role of active site threonine 201 and tyrosine 204 residues using enzyme mutants.
Tsoumpra, MK; Muniz, JR; Barnett, BL; Kwaasi, AA; Pilka, ES; Kavanagh, KL; Evdokimov, A; Walter, RL; Von Delft, F; Ebetino, FH; Oppermann, U; Russell, RG; Dunford, JE;
Bone. 01.12.2015 81:478-486. doi: 10.1016/j.bone.2015.08.020
PMID: 26318908

Inflammatory Signaling by NOD-RIPK2 Is Inhibited by Clinically Relevant Type II Kinase Inhibitors.
Canning, P; Ruan, Q; Schwerd, T; Hrdinka, M; Maki, JL; Saleh, D; Suebsuwong, C; Ray, S; Brennan, PE; Cuny, GD; Uhlig, HH; Gyrd-Hansen, M; Degterev, A; Bullock, AN;
Chemistry and Biology. 01.9.2015 22:1174-1184. doi: 10.1016/j.chembiol.2015.07.017
PMID: 26320862

Dual EZH2 and EHMT2 histone methyltransferase inhibition increases biological efficacy in breast cancer cells.
Curry E, Green I, Chapman-Rothe N, Shamsaei E, Kandil S, Cherblanc FL, Payne L, Bell E, Ganesh T, Srimongkolpithak N, Caron J, Li F, Uren AG, Snyder JP, Vedadi M, Fuchter MJ, Brown R
Clin Epigenetics. 21.08.2015 7(1):84. doi: 10.1186/s13148-015-0118-9
PMID: 26300989

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. 01.10.2015 290:25275-25292. doi: 10.1074/jbc.m115.637207
PMID: 26296892

A High Through-put Platform for Recombinant Antibodies to Folded Proteins.
Hornsby M, Paduch M, Miersch S, Sääf A, Matsuguchi T, Lee B, Wypisniak K, Doak A, King D, Usatyuk S, Perry K, Lu V, Thomas W, Luke J, Goodman J, Hoey RJ, Lai D, Griffin C, Li Z, Vizeacoumar FJ, Dong D, Campbell E, Anderson S, Zhong N, Gräslund S, Koide S, Moffat J, Sidhu S, Kossiakoff A, Wells J
Mol. Cell Proteomics. 19.08.2015 . doi: 10.1074/mcp.O115.052209
PMID: 26290498

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. 10.8.2015 112:10768-10773. doi: 10.1073/pnas.1501956112
PMID: 26261308

Structure of the human MLH1 N-terminus: implications for predisposition to Lynch syndrome.
Wu H, Zeng H, Lam R, Tempel W, Kerr ID, Min J
Acta Crystallogr F Struct Biol Commun. 01.08.2015 71(Pt 8):981-5. doi: 10.1107/S2053230X15010183
PMID: 26249686

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. 01.8.2015 71:1627-1639. doi: 10.1107/s1399004715007968
PMID: 26249344

BET Inhibition Upregulates SIRT1 and Alleviates Inflammatory Responses.
Kokkola, T; Suuronen, T; Pesonen, M; Filippakopoulos, P; Salminen, A; Jarho, EM; Lahtela-Kakkonen, M;
ChemBioChem: a European journal of chemical biology. 01.9.2015 16:1997-2001. doi: 10.1002/cbic.201500272
PMID: 26212199

Crystal structure of Porphyromonas gingivalis peptidylarginine deiminase: implications for autoimmunity in rheumatoid arthritis.
Montgomery, AB; Kopec, J; Shrestha, L; Thezenas, ML; Burgess-Brown, NA; Fischer, R; Yue, WW; Venables, PJ;
Annals of the Rheumatic Diseases. 24.7.2015 :-. doi:
PMID: 26209657

Discovery of NCT-501, a Potent and Selective Theophylline-Based Inhibitor of Aldehyde Dehydrogenase 1A1 (ALDH1A1).
Yang, SM; Yasgar, A; Miller, B; Lal-Nag, M; Brimacombe, K; Hu, X; Sun, H; Wang, A; Xu, X; Nguyen, K; Oppermann, U; Ferrer, M; Vasiliou, V; Simeonov, A; Jadhav, A; Maloney, DJ;
Journal of Medicinal Chemistry. 13.8.2015 58:5967-5978. doi: 10.1021/acs.jmedchem.5b00577
PMID: 26207746

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. 01.9.2015 6:27160-27175. doi: 10.18632/oncotarget.4746
PMID: 26320174

The promise and peril of chemical probes.
Arrowsmith CH, Audia JE, Austin C, Baell J, Bennett J, Blagg J, Bountra C, Brennan PE, Brown PJ, Bunnage ME, Buser-Doepner C, Campbell RM, Carter AJ, Cohen P, Copeland RA, Cravatt B, Dahlin JL, Dhanak D, Edwards AM, Frye SV, Gray N, Grimshaw CE, Hepworth D, Howe T, Huber KV, Jin J, Knapp S, Kotz JD, Kruger RG, Lowe D, Mader MM, Marsden B, Mueller-Fahrnow A, Müller S, O'Hagan RC, Overington JP, Owen DR, Rosenberg SH, Roth B, Ross R, Schapira M, Schreiber SL, Shoichet B, Sundström M, Superti-Furga G, Taunton J, Toledo-Sherman L, Walpole C, Walters MA, Willson TM, Workman P, Young RN, Zuercher WJ
Nat. Chem. Biol.. 21.07.2015 11(8):536-41. doi: 10.1038/nchembio.1867
PMID: 26196764

Probing the epigenome.
Huston A, Arrowsmith CH, Knapp S, Schapira M
Nat. Chem. Biol.. 21.07.2015 11(8):542-5. doi: 10.1038/nchembio.1871
PMID: 26196765

Structural basis of glycogen branching enzyme deficiency and pharmacologic rescue by rational peptide design.
Froese, DS; Michaeli, A; McCorvie, TJ; Krojer, T; Sasi, M; Melaev, E; Goldblum, A; Zatsepin, M; Lossos, A; Álvarez, R; Escribá, PV; Minassian, BA; von Delft, F; Kakhlon, O; Yue, WW;
Human Molecular Genetics. 01.10.2015 24:5667-5676. doi: 10.1093/hmg/ddv280
PMID: 26199317

Pharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia.
Grebien F, Vedadi M, Getlik M, Giambruno R, Grover A, Avellino R, Skucha A, Vittori S, Kuznetsova E, Smil D, Barsyte-Lovejoy D, Li F, Poda G, Schapira M, Wu H, Dong A, Senisterra G, Stukalov A, Huber KV, Schönegger A, Marcellus R, Bilban M, Bock C, Brown PJ, Zuber J, Bennett KL, Al-Awar R, Delwel R, Nerlov C, Arrowsmith CH, Superti-Furga G
Nat. Chem. Biol.. 13.07.2015 . doi: 10.1038/nchembio.1859
PMID: 26167872

Transactivation Function-2 of Estrogen Receptor α Contains Transactivation Function-1 Regulating Element
Arao, Y.; Coons L.A.; Zuercher W.J.; Korach K.S.
J. Biol. Chem.. 07.10.2015 290(28):17611-27. doi: 10.1074/jbc.M115.638650
PMID: 26028650

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