Discovery of Epigenetic Regulator I-BET762: Lead Optimization to Afford a Clinical Candidate Inhibitor of the BET Bromodomains

Mirguet, Olivier; Gosmini, Romain; Toum, Jérôme; A. Clément, Catherine; Barnathan, Mélanie; Brusq, Jean‐Marie; Mordaunt, J.E.; M. Grimes, Richard; C. Crowe, Miriam; Pineau, Olivier; Ajakane, Myriam; Daugan, Alain; D. Jeffrey, Philip; Cutler, Leanne; Haynes, Andrea; Smithers, Nicholas; Chung, Chun‐wa; Bamborough, Paul; Uings, Iain; J. Lewis, Antonia; Witherington, Jason; J. Parr, Nigel; K. Prinjha, Rab; Nicodème, Edwige

doi:10.1021/jm401088k

Public

Discovery of Epigenetic Regulator I-BET762: Lead Optimization to Afford a Clinical Candidate Inhibitor of the BET Bromodomains

Published in Journal of Medicinal Chemistry • Sep 9, 2013

Authors:

Olivier Mirguet

Romain Gosmini

Jérôme Toum

Abstract

The bromo and extra C-terminal domain (BET) family of bromodomains are involved in binding epigenetic marks on histone proteins, more specifically acetylated lysine residues. This paper describes the discovery and structure-activity relationships (SAR) of potent benzodiazepine inhibitors that disrup...

Subject

Bromodomain

BRD4

Epigenetics

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