Oleg Fedorov

Group Leader – Screening

University of Oxford
+44(0) 1865-612931

Oleg Fedorov obtained PhD from Institute of Theoretical and Experimental Biophysics in Russia and worked in University of Washington, University of Texas and University of Manchester before joining SGC Oxford.

Research Areas

Molecular Biophysics and Biochemistry group in SGC/TDI Oxford specialises on chemical probe discovery projects, especially in the field of Epigenetics. Main target areas are currently acetyl-lysine reader domains and histone demethylases. The group supports the wide variety of screening assays developed for most of the targets. The in-depth characterization of chemical probe candidates relies on a series of biophysical techniques established for accurate measurements of thermodynamics of and kinetic parameters of binding. The group also supports and extend the focused libraries of small molecular weight ligands for proteins of interest.

Group Members

  • Octovia Monteiro
  • James Bennett
  • Thomas Christott
  • Charline Giroud

Publications

CBP/p300 Bromodomains Regulate Amyloid-like Protein Aggregation upon Aberrant Lysine Acetylation.
Olzscha, H; Fedorov, O; Kessler, BM; Knapp, S; La Thangue, NB;
Cell Chemical Biology. 2017 24:9-23. doi: 10.1016/j.chembiol.2016.11.009
PMID: 27989401

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

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

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

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

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

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

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:

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

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

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

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

2017

Benzoisoquinolinediones as Potent and Selective Inhibitors of BRPF2 and TAF1/TAF1L Bromodomains.
Bouché, L; Christ, CD; Siegel, S; Fernández-Montalván, AE; Holton, SJ; Fedorov, O; Ter Laak, A; Sugawara, T; Stöckigt, D; Tallant, C; Bennett, J; Monteiro, O; Díaz-Sáez, L; Siejka, P; Meier, J; Pütter, V; Weiske, J; Müller, S; Huber, KVM; Hartung, IV; Haendler, B;
Journal of Medicinal Chemistry. 2017 60:4002-4022. doi: 10.1021/acs.jmedchem.7b00306
PMID: 28402630

Development of a monoclonal anti-ADAMTS-5 antibody that specifically blocks the interaction with LRP1.
Santamaria, S; Fedorov, O; McCafferty, J; Murphy, G; Dudhia, J; Nagase, H; Yamamoto, K;
mAbs. 2017 :0-0. doi: 10.1080/19420862.2017.1304341
PMID: 28306378

Potent and Selective KDM5 Inhibitor Stops Cellular Demethylation of H3K4me3 at Transcription Start Sites and Proliferation of MM1S Myeloma Cells.
Tumber, A; Nuzzi, A; Hookway, ES; Hatch, SB; Velupillai, S; Johansson, C; Kawamura, A; Savitsky, P; Yapp, C; Szykowska, A; Wu, N; Bountra, C; Strain-Damerell, C; Burgess-Brown, NA; Ruda, GF; Fedorov, O; Munro, S; England, KS; Nowak, RP; Schofield, CJ; La Thangue, NB; Pawlyn, C; Davies, F; Morgan, G; Athanasou, N; Müller, S; Oppermann, U; Brennan, PE;
Cell Chemical Biology. 2017 24:371-380. doi: 10.1016/j.chembiol.2017.02.006
PMID: 28262558

Assessing histone demethylase inhibitors in cells: lessons learned.
Hatch, SB; Yapp, C; Montenegro, RC; Savitsky, P; Gamble, V; Tumber, A; Ruda, GF; Bavetsias, V; Fedorov, O; Atrash, B; Raynaud, F; Lanigan, R; Carmichael, L; Tomlin, K; Burke, R; Westaway, SM; Brown, JA; Prinjha, RK; Martinez, ED; Oppermann, U; Schofield, CJ; Bountra, C; Kawamura, A; Blagg, J; Brennan, PE; Rossanese, O; Müller, S;
Epigenetics and Chromatin. 2017 10:9-. doi: 10.1186/s13072-017-0116-6
PMID: 28265301

Thiazolidine derivatives as potent and selective inhibitors of the PIM kinase family.
Bataille, CJ; Brennan, MB; Byrne, S; Davies, SG; Durbin, M; Fedorov, O; Huber, KV; Jones, AM; Knapp, S; Liu, G; Nadali, A; Quevedo, CE; Russell, AJ; Walker, RG; Westwood, R; Wynne, GM;
Bioorganic and Medicinal Chemistry. 2017 25:2657-2665. doi: 10.1016/j.bmc.2017.02.056
PMID: 28341403

Design of a Biased Potent Small Molecule Inhibitor of the Bromodomain and PHD Finger-Containing (BRPF) Proteins Suitable for Cellular and in Vivo Studies.
Igoe, N; Bayle, ED; Fedorov, O; Tallant, C; Savitsky, P; Rogers, C; Owen, DR; Deb, G; Somervaille, TC; Andrews, DM; Jones, N; Cheasty, A; Ryder, H; Brennan, PE; Müller, S; Knapp, S; Fish, PV;
Journal of Medicinal Chemistry. 2017 60:668-680. doi: 10.1021/acs.jmedchem.6b01583
PMID: 28068087

CBP/p300 Bromodomains Regulate Amyloid-like Protein Aggregation upon Aberrant Lysine Acetylation.
Olzscha, H; Fedorov, O; Kessler, BM; Knapp, S; La Thangue, NB;
Cell Chemical Biology. 2017 24:9-23. doi: 10.1016/j.chembiol.2016.11.009
PMID: 27989401

2016

Discovery of a PCAF Bromodomain Chemical Probe.
Moustakim M, Clark PG, Trulli L, Fuentes de Arriba AL, Ehebauer MT, Chaikuad A, Murphy EJ, Mendez-Johnson J, Daniels D, Hou CD, Lin YH, Walker JR, Hui R, Yang H, Dorrell L, Rogers CM, Monteiro OP, Fedorov O, Huber KV, Knapp S, Heer J, Dixon DJ, Brennan PE
Angew. Chem. Int. Ed. Engl.. 2016 . doi: 10.1002/anie.201610816
PMID: 27966810

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

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

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

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

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

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

A poised fragment library enables rapid synthetic expansion yielding the first reported inhibitors of PHIP(2), an atypical bromodomain
Cox, OB; Krojer, T; Collins, P; Monteiro, O; Talon, R; Bradley, A; Fedorov, O; Amin, J; Marsden, BD; Spencer, J; von Delft, F; Brennan, PE;
Chemical Science. 2016 7:2322-2330. doi: 10.1039/c5sc03115j
PMID:

Identification of a small-molecule ligand of the epigenetic reader protein Spindlin1 via a versatile screening platform.
Wagner, T; Greschik, H; Burgahn, T; Schmidtkunz, K; Schott, AK; McMillan, J; Baranauskienė, L; Xiong, Y; Fedorov, O; Jin, J; Oppermann, U; Matulis, D; Schüle, R; Jung, M;
Nucleic Acids Research. 2016 44:e88-. doi:
PMID: 26893353

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

8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors.
Bavetsias, V; Lanigan, RM; Ruda, GF; Atrash, B; McLaughlin, MG; Tumber, A; Mok, NY; Le Bihan, YV; Dempster, S; Boxall, KJ; Jeganathan, F; Hatch, SB; Savitsky, P; Velupillai, S; Krojer, T; England, KS; Sejberg, J; Thai, C; Donovan, A; Pal, A; Scozzafava, G; Bennett, JM; Kawamura, A; Johansson, C; Szykowska, A; Gileadi, C; Burgess-Brown, NA; von Delft, F; Oppermann, U; Walters, Z; Shipley, J; Raynaud, FI; Westaway, SM; Prinjha, RK; Fedorov, O; Burke, R; Schofield, CJ; Westwood, IM; Bountra, C; Müller, S; van Montfort, RL; Brennan, PE; Blagg, J;
Journal of Medicinal Chemistry. 2016 59:1388-1409. doi:
PMID: 26741168

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

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

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

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:

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

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

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

2014

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:

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:

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:

Sulfated glycosaminoglycans control the extracellular trafficking and the activity of the metalloprotease inhibitor TIMP-3.
Troeberg, L; Lazenbatt, C; Anower-E-Khuda, MF; Freeman, C; Federov, O; Habuchi, H; Habuchi, O; Kimata, K; Nagase, H;
Chemistry and Biology. 2014 21:1300-1309. doi:
PMID: 25176127

Lysine methylation-dependent binding of 53BP1 to the pRb tumor suppressor.
Carr, SM; Munro, S; Zalmas, LP; Fedorov, O; Johansson, C; Krojer, T; Sagum, CA; Bedford, MT; Oppermann, U; La Thangue, NB;
Proceedings of the National Academy of Sciences of USA. 2014 111:11341-11346. doi:
PMID: 25049398

Corrigendum: 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 10:692-. doi: 10.1038/nchembio0814-692d
PMID: 25036311

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

What is the future of bromodomains in targeted drug development?
F, O; e, ; d, ; o, ; r, ; o, ; v, ;
Future Medicinal Chemistry. 2014 6:1101-1103. doi:
PMID: 25078130

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

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

[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

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

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

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

Arginine methylation-dependent reader-writer interplay governs growth control by E2F-1.
Zheng, S; Moehlenbrink, J; Lu, YC; Zalmas, LP; Sagum, CA; Carr, S; McGouran, JF; Alexander, L; Fedorov, O; Munro, S; Kessler, B; Bedford, MT; Yu, Q; La Thangue, NB;
Molecular Cell. 2013 52:37-51. doi:
PMID: 24076217

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

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

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

Stimulation of Hepatic Apolipoprotein A-I Production by Novel Thieno-Triazolodiazepines: Roles of the Classical Benzodiazepine Receptor, PAF Receptor, and Bromodomain Binding.
Kempen, HJ; Bellus, D; Fedorov, O; Nicklisch, S; Filippakopoulos, P; Picaud, S; Knapp, S;
Lipid Insights. 2013 6:47-54. doi:
PMID: 25278768

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 plasticity of histones H3-H4 facilitates their allosteric exchange between RbAp48 and ASF1.
Zhang, W; Tyl, M; Ward, R; Sobott, F; Maman, J; Murthy, AS; Watson, AA; Fedorov, O; Bowman, A; Owen-Hughes, T; El Mkami, H; Murzina, NV; Norman, DG; Laue, ED;
Nature Structural and Molecular Biology. 2013 20:29-35. doi:
PMID: 23178455

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

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:

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:

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:

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

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

2011

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

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

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:

2010

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

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:

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

2009

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

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:
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

2008

RhoB can adopt a Mg2+ free conformation prior to GEF binding.
Soundararajan, M; Turnbull, A; Fedorov, O; Johansson, C; Doyle, DA;
Proteins: Structure, Function, and Bioinformatics. 2008 72:498-505. doi:
PMID: 18393397

Structural diversity in the RGS domain and its interaction with heterotrimeric G protein alpha-subunits.
Soundararajan, M; Willard, FS; Kimple, AJ; Turnbull, AP; Ball, LJ; Schoch, GA; Gileadi, C; Fedorov, OY; Dowler, EF; Higman, VA; Hutsell, SQ; Sundström, M; Doyle, DA; Siderovski, DP;
Proceedings of the National Academy of Sciences of USA. 2008 105:6457-6462. doi:
PMID: 18434541

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

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

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

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

Resonance assignment of the RGS domain of human RGS10.
Fedorov, OY; Higman, VA; Schmieder, P; Leidert, M; Diehl, A; Elkins, J; Soundararajan, M; Oschkinat, H; Ball, LJ;
Journal of Biomolecular NMR. 2007 38:191-. doi:
PMID: 17180548

2005

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

2004

The structure and dynamics of tandem WW domains in a negative regulator of notch signaling, Suppressor of deltex.
Fedoroff, OY; Townson, SA; Golovanov, AP; Baron, M; Avis, JM;
Journal of Biological Chemistry. 2004 279:34991-35000. doi:
PMID: 15173166

2001

Design and synthesis of fluoroquinophenoxazines that interact with human telomeric G-quadruplexes and their biological effects.
Duan, W; Rangan, A; Vankayalapati, H; Kim, MY; Zeng, Q; Sun, D; Han, H; Fedoroff, OY; Nishioka, D; Rha, SY; Izbicka, E; Von Hoff, DD; Hurley, LH;
Molecular Cancer Therapeutics. 2001 1:103-120. doi:
PMID: 12467228

Induction of duplex to G-quadruplex transition in the c-myc promoter region by a small molecule.
Rangan, A; Fedoroff, OY; Hurley, LH;
Journal of Biological Chemistry. 2001 276:4640-4646. doi:
PMID: 11035006

2000

Cationic porphyrins promote the formation of i-motif DNA and bind peripherally by a nonintercalative mechanism.
Fedoroff, OY; Rangan, A; Chemeris, VV; Hurley, LH;
Biochemistry. 2000 39:15083-15090. doi:
PMID: 11106486

G-quadruplexes as targets for drug design.
Hurley, LH; Wheelhouse, RT; Sun, D; Kerwin, SM; Salazar, M; Fedoroff, OY; Han, FX; Han, H; Izbicka, E; Von Hoff, DD;
Pharmacology and Therapeutics. 2000 85:141-158. doi:
PMID: 10739869

1998

NMR-Based model of a telomerase-inhibiting compound bound to G-quadruplex DNA.
Fedoroff, OY; Salazar, M; Han, H; Chemeris, VV; Kerwin, SM; Hurley, LH;
Biochemistry. 1998 37:12367-12374. doi:
PMID: 9730808

A common 40 amino acid motif in eukaryotic RNases H1 and caulimovirus ORF VI proteins binds to duplex RNAs.
Cerritelli, SM; Fedoroff, OY; Reid, BR; Crouch, RJ;
Nucleic Acids Research. 1998 26:1834-1840. doi:
PMID: 9512560

1997

Solution structure of r(gaggacug):d(CAGTCCTC) hybrid: implications for the initiation of HIV-1 (+)-strand synthesis.
Fedoroff, OY; Ge, Y; Reid, BR;
Journal of Molecular Biology. 1997 269:225-239. doi:
PMID: 9191067

1996

1994

The solution structure of the r(gcg)d(TATACCC):d(GGGTATACGC) Okazaki fragment contains two distinct duplex morphologies connected by a junction.
Salazar, M; Fedoroff OYu, ; Zhu, L; Reid, BR;
Journal of Molecular Biology. 1994 241:440-455. doi:
PMID: 8064857

DNA sequence GCGAATGAGC containing the human centromere core sequence GAAT forms a self-complementary duplex with sheared G.A pairs in solution.
Chou, SH; Cheng, JW; Fedoroff, O; Reid, BR;
Journal of Molecular Biology. 1994 241:467-479. doi:
PMID: 8064859

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