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本文引用的文献

1
Targeting mycobacterium protein tyrosine phosphatase B for antituberculosis agents.针对结核分枝杆菌蛋白酪氨酸磷酸酶 B 的抗结核药物研究。
Proc Natl Acad Sci U S A. 2010 Mar 9;107(10):4573-8. doi: 10.1073/pnas.0909133107. Epub 2010 Feb 18.
2
High-throughput discovery of Mycobacterium tuberculosis protein tyrosine phosphatase B (MptpB) inhibitors using click chemistry.利用点击化学高通量发现结核分枝杆菌蛋白酪氨酸磷酸酶 B（MptpB）抑制剂。
Org Lett. 2009 Nov 19;11(22):5102-5. doi: 10.1021/ol9023419.
3
Inhibition of MptpB phosphatase from Mycobacterium tuberculosis impairs mycobacterial survival in macrophages.抑制结核分枝杆菌的MptpB磷酸酶会损害分枝杆菌在巨噬细胞中的存活。
J Antimicrob Chemother. 2009 May;63(5):928-36. doi: 10.1093/jac/dkp031. Epub 2009 Feb 24.
4
Targeting virulence: a new paradigm for antimicrobial therapy.靶向毒力：抗菌治疗的新范式
Nat Chem Biol. 2007 Sep;3(9):541-8. doi: 10.1038/nchembio.2007.24.
5
Fragment-based substrate activity screening method for the identification of potent inhibitors of the Mycobacterium tuberculosis phosphatase PtpB.基于片段的底物活性筛选方法用于鉴定结核分枝杆菌磷酸酶PtpB的有效抑制剂。
J Am Chem Soc. 2007 Aug 8;129(31):9613-5. doi: 10.1021/ja0727520. Epub 2007 Jul 18.
6
PTP1B as a drug target: recent developments in PTP1B inhibitor discovery.蛋白酪氨酸磷酸酶1B作为药物靶点：蛋白酪氨酸磷酸酶1B抑制剂发现的最新进展
Drug Discov Today. 2007 May;12(9-10):373-81. doi: 10.1016/j.drudis.2007.03.011. Epub 2007 Apr 6.
7
Structural basis for selective inhibition of Mycobacterium tuberculosis protein tyrosine phosphatase PtpB.结核分枝杆菌蛋白酪氨酸磷酸酶PtpB选择性抑制的结构基础
Structure. 2007 Apr;15(4):499-509. doi: 10.1016/j.str.2007.03.003.
8
Brunsvicamides A-C: sponge-related cyanobacterial peptides with Mycobacterium tuberculosis protein tyrosine phosphatase inhibitory activity.布伦斯维酰胺A - C：具有结核分枝杆菌蛋白酪氨酸磷酸酶抑制活性的与海绵相关的蓝细菌肽。
J Med Chem. 2006 Aug 10;49(16):4871-8. doi: 10.1021/jm060327w.
9
Discovery of protein phosphatase inhibitor classes by biology-oriented synthesis.通过生物导向合成发现蛋白质磷酸酶抑制剂类别。
Proc Natl Acad Sci U S A. 2006 Jul 11;103(28):10606-11. doi: 10.1073/pnas.0601490103. Epub 2006 Jun 29.
10
The magic bullets and tuberculosis drug targets.神奇子弹与抗结核药物靶点。
Annu Rev Pharmacol Toxicol. 2005;45:529-64. doi: 10.1146/annurev.pharmtox.45.120403.100120.

结核分枝杆菌中一种必需的毒性磷酸酶——mPTPB新型抑制剂的鉴定与表征

Identification and characterization of novel inhibitors of mPTPB, an essential virulent phosphatase from Mycobacterium tuberculosis.

作者信息

Chen Lan, Zhou Bo, Zhang Sheng, Wu Li, Wang Yuehong, Franzblau Scott G, Zhang Zhong-Yin

机构信息

Chemical Genomics Core Facility, Indiana University School of Medicine, 635 Barnhill Drive, Indianapolis, Indiana 46202.

出版信息

ACS Med Chem Lett. 2010 Oct 14;1(7):355-359. doi: 10.1021/ml1001135.

DOI:10.1021/ml1001135
PMID:21116447
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2992434/
Abstract

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 target with a completely novel mechanism of action. We screened a library of 7,500 compounds against mPTPB and identified several 2-oxo-1,2-dihydrobenzo[cd]indole-6-sulfonamide 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.

摘要

分枝杆菌蛋白酪氨酸磷酸酶B（mPTPB）是结核分枝杆菌（Mtb）在宿主巨噬细胞中存活所必需的一种关键毒力因子。因此，mPTPB代表了一个具有全新作用机制的令人兴奋的新靶点。我们针对mPTPB筛选了一个包含7500种化合物的文库，并鉴定出几种2-氧代-1,2-二氢苯并[cd]吲哚-6-磺酰胺和哌嗪基-硫苯基-乙基-草酰胺衍生物作为两类不同的mPTPB抑制剂。我们表明这两类抑制剂都能够阻断mPTPB介导的ERK1/2失活。我们进一步证明这两类mPTPB抑制剂在抑制巨噬细胞中Mtb的生长方面是有效的。因此，先导化合物的改进可能会产生一类新型抗结核药物。