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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. Picaud S, et al. Sci Adv. 2016 Oct 12;2(10):e1600760. doi: 10.1126/sciadv.1600760. eCollection 2016 Oct. Sci Adv. 2016. PMID: 27757418 Free PMC article.
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. Filippakopoulos P, et al. Among authors: picaud s. Nature. 2010 Dec 23;468(7327):1067-73. doi: 10.1038/nature09504. Epub 2010 Sep 24. Nature. 2010. PMID: 20871596 Free PMC article.
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. Hewings DS, et al. Among authors: picaud s. J Med Chem. 2011 Oct 13;54(19):6761-70. doi: 10.1021/jm200640v. Epub 2011 Sep 6. J Med Chem. 2011. PMID: 21851057 Free PMC article.
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. Filippakopoulos P, et al. Among authors: picaud s. Cell. 2012 Mar 30;149(1):214-31. doi: 10.1016/j.cell.2012.02.013. Cell. 2012. PMID: 22464331 Free PMC article.
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. Matzuk MM, et al. Among authors: picaud s. Cell. 2012 Aug 17;150(4):673-84. doi: 10.1016/j.cell.2012.06.045. Cell. 2012. PMID: 22901802 Free PMC article.
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. Fish PV, et al. Among authors: picaud s. J Med Chem. 2012 Nov 26;55(22):9831-7. doi: 10.1021/jm3010515. Epub 2012 Nov 8. J Med Chem. 2012. PMID: 23095041 Free PMC article.
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: picaud s. 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. 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.
299 results