Activating NRAS mutations occur in approximately 20% of melanomas but remain largely undruggable due to the lack of effective targeted therapies. We previously identified casein kinase 1δ (CK1δ) as a critical upstream regulator that stabilizes oncogenic NRAS mutants. However, no selective CK1δ inhibitors have advance...
Chang-Fa Zhang, Ya-Lei Wen, Jian-Qiao Yi et al.· Journal of Medicinal Chemist...· 0 citations
Drug-resistant Mycobacterium tuberculosis (Mtb) poses a growing threat, necessitating new therapeutic strategies. The cytochrome bcc-aa3 oxidase (Cyt-bcc) is an attractive target, yet single-agent inhibition fails owing to compensation by the alternative cytochrome bd terminal oxidase (Cyt-bd). Herein, we describe a...
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
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
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