Author

Shao Q. Yao

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Sep 2026

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

This work expands the CKI toolbox to include arginine-targeting warheads and provides a modular framework to overcome point mutation-driven resistance, and provides a modular framework to overcome point mutation-driven resistance.

Zu-Qin Wang, Xuan Wang, Hong Zhang et al. · Journal of Medicinal Chemist... · 0 citations

#protein folding Open access Sep 2026

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

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-selective covalent inhibitor, named ipAE1, of BET BD...

Ji-Bo Kang, Xuan Wang, Hong Zhang et al. · Angewandte Chemie · 0 citations