High-Throughput Discovery of <i>Mycobacterium tuberculosis</i> Protein Tyrosine Phosphatase B (MptpB) Inhibitors Using Click Chemistry
Lay Pheng Tan(National University of Singapore), Hao Wu(National University of Singapore), Pengyu Yang(National University of Singapore), Karunakaran Kalesh(National University of Singapore), Xiao‐Hua Zhang(National University of Singapore), Mingyu Hu(National University of Singapore), Rajavel Srinivasan(National University of Singapore), Shao Q. Yao(National University of Singapore)
Cited by 69
Abstract
A approximately 3500-member library of bidentate inhibitors against protein tyrosine phosphatases (PTPs) was rapidly assembled using click chemistry. Subsequent high-throughput screening had led to the discovery of highly potent (K(i) as low as 150 nM) and selective MptpB inhibitors, some of which represent the most potent MptpB inhibitors developed to date.
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