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Page 1
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. Hatch SB, et al. Among authors: fedorov o. Epigenetics Chromatin. 2017 Mar 1;10:9. doi: 10.1186/s13072-017-0116-6. eCollection 2017. Epigenetics Chromatin. 2017. PMID: 28265301 Free PMC article.
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. Bunkoczi G, et al. Among authors: fedorov o. Structure. 2007 Oct;15(10):1215-26. doi: 10.1016/j.str.2007.08.011. Structure. 2007. PMID: 17937911 Free PMC article.
The (un)targeted cancer kinome.
Fedorov O, Müller S, Knapp S. Fedorov O, et al. Nat Chem Biol. 2010 Mar;6(3):166-169. doi: 10.1038/nchembio.297. Nat Chem Biol. 2010. PMID: 20154661 No abstract available.
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. Hewings DS, et al. Among authors: fedorov o. J Med Chem. 2013 Apr 25;56(8):3217-27. doi: 10.1021/jm301588r. Epub 2013 Apr 5. J Med Chem. 2013. PMID: 23517011 Free PMC article.
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. Picaud S, et al. Among authors: fedorov o, o sullivan b. Cancer Res. 2013 Jun 1;73(11):3336-46. doi: 10.1158/0008-5472.CAN-12-3292. Epub 2013 Apr 10. Cancer Res. 2013. PMID: 23576556 Free PMC article.
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. Picaud S, et al. Among authors: fedorov o. Proc Natl Acad Sci U S A. 2013 Dec 3;110(49):19754-9. doi: 10.1073/pnas.1310658110. Epub 2013 Nov 18. Proc Natl Acad Sci U S A. 2013. PMID: 24248379 Free PMC article.
[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. Fedorov O, et al. J Med Chem. 2014 Jan 23;57(2):462-76. doi: 10.1021/jm401568s. Epub 2013 Dec 30. J Med Chem. 2014. PMID: 24313754 Free PMC article.
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. Rooney TP, et al. Among authors: fedorov o. Angew Chem Int Ed Engl. 2014 Jun 10;53(24):6126-30. doi: 10.1002/anie.201402750. Epub 2014 May 12. Angew Chem Int Ed Engl. 2014. PMID: 24821300 Free PMC article.
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. Hay DA, et al. Among authors: fedorov o. J Am Chem Soc. 2014 Jul 2;136(26):9308-19. doi: 10.1021/ja412434f. Epub 2014 Jun 19. J Am Chem Soc. 2014. PMID: 24946055 Free PMC article.
157 results