Fengcai Zhang

Dual‐Site Covalent Targeting Enables BD2‐Selective BET Inhibition With Potent Antitumor Activity in Mice

ABSTRACT Bromodomain and extra‐terminal (BET) proteins are validated therapeutic targets for cancer, but clinical translation of pan‐BET inhibitors is limited by dose‐limiting toxicities from non‐selective inhibition of BD1/BD2 domains. Herein, we report the first‐ever domain‐sel...