Shao Qin Yao

Discovery of Arginine-Reactive Covalent Kinase Inhibitors Overcoming Clinical Drug Resistance

Abstract Covalent kinase inhibitors (CKIs) serve as potent therapeutics, yet their development largely depends on conserved cysteine residues. Many kinases lack accessible cysteines or develop resistance mutations at these sites, limiting clinical utility. To diversify targetable...

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...