Covalent inhibitors of nicotinamide N-methyltransferase (NNMT) provide evidence for target engagement challenges in situ.

Hsin-Yu Lee,Radu M Suciu,Benjamin D Horning,Ekaterina V Vinogradova,Olesya A Ulanovskaya,Benjamin F Cravatt

Bioorganic & Medicinal Chemistry Letters（2018）

引用 22|浏览25

暂无评分

摘要

•α-Chloroacetamides (αCAs) serve as irreversible inhibitors of NNMT.•αCA inhibitors show good proteomic selectivity for NNMT in vitro.•The potency of αCA inhibitors of NNMT is greatly reduced in cells.

查看译文

关键词

Nicotinamide N-methyltransferase,Activity-based profiling,Proteomics,Inhibitor,Cysteine,Covalent

AI 理解论文

溯源树

样例

生成溯源树，研究论文发展脉络

Chat Paper

正在生成论文摘要