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BET inhibition disrupts transcription but retains enhancer-promoter contact.
Crump NT, Ballabio E, Godfrey L, Thorne R, Repapi E, Kerry J, Tapia M, Hua P, Lagerholm C, Filippakopoulos P, Davies JOJ, Milne TA. Crump NT, et al. Among authors: filippakopoulos p. Nat Commun. 2021 Jan 11;12(1):223. doi: 10.1038/s41467-020-20400-z. Nat Commun. 2021. PMID: 33431820 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. Nature. 2010 Dec 23;468(7327):1067-73. doi: 10.1038/nature09504. Epub 2010 Sep 24. Nature. 2010. PMID: 20871596 Free PMC article.
Epigenetic targeting of bromodomain protein BRD4 counteracts cancer cachexia and prolongs survival.
Segatto M, Fittipaldi R, Pin F, Sartori R, Dae Ko K, Zare H, Fenizia C, Zanchettin G, Pierobon ES, Hatakeyama S, Sperti C, Merigliano S, Sandri M, Filippakopoulos P, Costelli P, Sartorelli V, Caretti G. Segatto M, et al. Among authors: filippakopoulos p. Nat Commun. 2017 Nov 22;8(1):1707. doi: 10.1038/s41467-017-01645-7. Nat Commun. 2017. PMID: 29167426 Free PMC article.
A chemical toolbox for the study of bromodomains and epigenetic signaling.
Wu Q, Heidenreich D, Zhou S, Ackloo S, Krämer A, Nakka K, Lima-Fernandes E, Deblois G, Duan S, Vellanki RN, Li F, Vedadi M, Dilworth J, Lupien M, Brennan PE, Arrowsmith CH, Müller S, Fedorov O, Filippakopoulos P, Knapp S. Wu Q, et al. Among authors: filippakopoulos p. Nat Commun. 2019 Apr 23;10(1):1915. doi: 10.1038/s41467-019-09672-2. Nat Commun. 2019. PMID: 31015424 Free PMC article.
Acetylation reprograms MITF target selectivity and residence time.
Louphrasitthiphol P, Loffreda A, Pogenberg V, Picaud S, Schepsky A, Friedrichsen H, Zeng Z, Lashgari A, Thomas B, Patton EE, Wilmanns M, Filippakopoulos P, Lambert JP, Steingrímsson E, Mazza D, Goding CR. Louphrasitthiphol P, et al. Among authors: filippakopoulos p. Nat Commun. 2023 Sep 28;14(1):6051. doi: 10.1038/s41467-023-41793-7. Nat Commun. 2023. PMID: 37770430 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: filippakopoulos p. 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: filippakopoulos p. 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.
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. Ciceri P, et al. Among authors: filippakopoulos p. Nat Chem Biol. 2014 Apr;10(4):305-12. doi: 10.1038/nchembio.1471. Epub 2014 Mar 2. Nat Chem Biol. 2014. PMID: 24584101 Free PMC article.
96 results