High-Throughput Discovery of Mycobacterium tuberculosis Protein Tyrosine Phosphatase B (MptpB) Inhibitors Using Click Chemistry

Lay Pheng Tan; Hao Wu; Peng-Yu Yang; Karunakaran A. Kalesh; Xiaohua Zhang; Mingyu Hu; Rajavel Srinivasan; Shao Q. Yao

doi:10.1021/ol9023419

High-Throughput Discovery of Mycobacterium tuberculosis Protein Tyrosine Phosphatase B (MptpB) Inhibitors Using Click Chemistry

Lay Pheng Tan, Hao Wu, Peng-Yu Yang, Karunakaran A. Kalesh, Xiaohua Zhang, Mingyu Hu, Rajavel Srinivasan, Shao Q. Yao

Research output: Contribution to journal › Article › peer-review

Abstract

A ∼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 (Ki as low as 150 nM) and selective MptpB inhibitors, some of which represent the most potent MptpB inhibitors developed to date.

Original language	English
Pages (from-to)	5102–5105
Number of pages	4
Journal	Organic Letters
Volume	11
Issue number	22
Early online date	23 Oct 2009
DOIs	https://doi.org/10.1021/ol9023419
Publication status	Published - 19 Nov 2009
Externally published	Yes

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abstract = "A ∼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 (Ki as low as 150 nM) and selective MptpB inhibitors, some of which represent the most potent MptpB inhibitors developed to date.",

author = "Tan, {Lay Pheng} and Hao Wu and Peng-Yu Yang and Kalesh, {Karunakaran A.} and Xiaohua Zhang and Mingyu Hu and Rajavel Srinivasan and Yao, {Shao Q.}",

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AU - Tan, Lay Pheng

AU - Wu, Hao

AU - Yang, Peng-Yu

AU - Kalesh, Karunakaran A.

AU - Zhang, Xiaohua

AU - Hu, Mingyu

AU - Srinivasan, Rajavel

AU - Yao, Shao Q.

PY - 2009/11/19

Y1 - 2009/11/19

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AB - A ∼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 (Ki 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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High-Throughput Discovery of Mycobacterium tuberculosis Protein Tyrosine Phosphatase B (MptpB) Inhibitors Using Click Chemistry

Abstract

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