"VSports最新版本" The making of I-BET762, a BET bromodomain inhibitor now in clinical development
- PMID: 24107192
- DOI: 10.1021/jm4014407 (VSports app下载)
The making of I-BET762, a BET bromodomain inhibitor now in clinical development (V体育官网入口)
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 VSports手机版. 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. .
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"V体育官网" Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains.J Med Chem. 2013 Oct 10;56(19):7501-15. doi: 10.1021/jm401088k. Epub 2013 Sep 25. J Med Chem. 2013. PMID: 24015967
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