Identification of bostrycin derivatives as potential inhibitors of mycobacterium tuberculosis protein tyrosine phosphatase (MptpB)
Chen Dongni Chen Hong She Zhigang Lu Yongjun · 2016
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期刊名称:
Medicinal Chemistry   2016 年 12 卷 3 期
发表日期:
2016.05.01
摘要:
Background: As a virulence factor secreted into host cells, the Mycobacterium tuberculosis protein tyrosine phosphatase (MptpB) mediates the intracellular survival of M. tuberculosis. MptpB has become an attractive target for the development of new anti-tuberculosis drugs. Objective: In the present study, we assessed the inhibitory activity of marine fungus-derived bostrycin and its derivatives against MptpB in vitro. Method: The compounds were tested for their inhibitory effects on MptpB in vitro and the inhibition mode. The binding characteristics of inhibitors and MptpB were determined by microscale thermophoresis (MST). Results: Our data showed that one of the derivatives, compound 25 (IC
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