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

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

Olivier Mirguet, Romain Gosmini, Jérôme Toum, Catherine A Clément, Mélanie Barnathan, Jean-Marie Brusq, Jacqueline E Mordaunt, Richard M Grimes, Miriam Crowe, Olivier Pineau, Myriam Ajakane, Alain Daugan, etc.

J Med Chem. 2013 Oct 10;56(19):7501-15.

PMID: 24015967

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 disrupt the function of the BET family of bromodomains (BRD2, BRD3, and BRD4). This work has yielded a potent, selective compound I-BET762 that is now under evaluation in a phase I/II clinical trial for nuclear protein in testis (NUT) midline carcinoma and other cancers.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP1260907172	I-BET762		1260907-17-2	Price

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