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

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 op...

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Veröffentlicht in:	Journal of medicinal chemistry 2013-10, Vol.56 (19), p.7498-7500
Hauptverfasser:	Zhao, Yujun, Yang, Chao-Yie, Wang, Shaomeng
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antineoplastic Agents - pharmacology Benzodiazepines - pharmacology Humans Nuclear Proteins - antagonists & inhibitors Transcription Factors - antagonists & inhibitors
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Beschreibung
Zusammenfassung:	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.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm4014407