A facile hydroxyindole carboxylic acid based focused library approach for potent and selective inhibitors of Mycobacterium protein tyrosine phosphatase B.
A facile hydroxyindole carboxylic acid based focused library approach for potent and selective inhibitors of Mycobacterium protein tyrosine phosphatase B.
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DOI：
10.1002/cmdc.201300115
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发表时间：
2013-06
期刊：
影响因子：
3.4
通讯作者：
Zhang, Zhong-Yin
中科院分区：
文献类型：
--
作者：
Zeng, Li-Fan;Xu, Jie;He, Yantao;He, Rongjun;Wu, Li;Gunawan, Andrea M.;Zhang, Zhong-Yin
A facile hydroxyindole carboxylic acid-based focused amide library approach was designed to target both the PTP active site and a unique nearby pocket for enhanced affinity and selectivity. High throughput screening of the focused library let to the identification of a highly potent (Ki=50 nM) and selective (>100-fold against a large panel of PTPs) inhibitor 11a for mPTPB, an essential virulence factor for Mycobacterium tuberculosis. Importantly, 11a displayed highly efficacious cellular activity and was capable of reversing the altered immune responses induced by mPTPB in macrophages.
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影响因子：
15
作者：
Soellner, Matthew B.;Rawls, Katherine A.;Ellman, Jonathan A.
通讯作者：
Ellman, Jonathan A.
影响因子：
4.8
作者：
Liang, FB;Huang, ZH;Zhang, ZY
通讯作者：
Zhang, ZY
DOI：
10.1073/pnas.0909133107
发表时间：
2010-03-09
影响因子：
11.1
作者：
Zhou, Bo;He, Yantao;Zhang, Zhong-Yin
通讯作者：
Zhang, Zhong-Yin
影响因子：
4.1
作者：
Correa, Ivan R., Jr.;Noeren-Mueller, Andrea;Waldmann, Herbert
通讯作者：
Waldmann, Herbert
影响因子：
2.7
作者：
Weide, T;Arve, L;Kessler, H
通讯作者：
Kessler, H