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The Making of I-BET762, a BET Bromodomain Inhibitor Now in Clinical Development

Yujun Zhao, Chao-Yie Yang, Shaomeng Wang

J Med Chem. 2013 Oct 10;56(19):7498-500.

PMID: 24107192

Abstract:

Bromodomain and extra-terminal (BET) proteins belong to a class of proteins collectively called epigenetic "readers". BET bromodomains have emerged as promising drug targets for treatment of cancers, inflammatory diseases, and other medical conditions. GlaxoSmithKline scientists have successfully optimized a class of benzodiazepines as inhibitors of BET bromodomains, without any prior knowledge of identified molecular targets. It thus is possible to hit a target without aiming at it. The optimized lead compound I-BET762 is currently being evaluated in a phase I clinical trial for treatment of human cancer.

Chemicals Related in the Paper:

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