期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 1, 期 7, 页码 355-359出版社
AMER CHEMICAL SOC
DOI: 10.1021/ml1001135
关键词
Mycobacterium tuberculosis; mPTPB inhibitors; anti-TB agents; high throughput screening; protein tyrosine phosphatase
资金
- National Institutes of Health [CA69202, CA126937]
Mycobacterium protein tyrosine phosphatase B (mPTPB) is an essential virulence factor required for Mycobacterium tuberculosis (Mtb) survival in host macrophages. Consequently mPTPB represents an exciting new with a completely novel mechanism of action. We screened a library of 7500 compounds against mPTPB and identified several 2-oxo-1,2-dihydrobenzo[cd]indole-6-sulfon-amide and piperazinyl-thiophenyl-ethyl-oxalamide derivatives as two distinct classes of mPTPB inhibitors. We showed that both classes of inhibitors are capable of blocking the mPTPB-mediated ERK1/2 inactivation. We further demonstrated that both classes of mPTPB inhibitors are effective in inhibiting the growth of Mtb in macrophages. Thus, improvement of the lead compounds may produce a novel class of anti-TB agents.
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