Development and Characterization of New Peptidomimetic Inhibitors of the West Nile Virus NS2B-NS3 Protease
Development and Characterization of New Peptidomimetic Inhibitors of the West Nile Virus NS2B-NS3 Protease
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DOI：
10.1002/cmdc.201200497
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发表时间：
2013-02-01
期刊：
影响因子：
3.4
通讯作者：
Steinmetzer, Torsten
中科院分区：
文献类型：
--
作者：
Hammamy, M. Zouhir;Haase, Caroline;Steinmetzer, Torsten
开发了一系列新的 WNV NS2BNS3 蛋白酶底物类似物抑制剂，其中 P1 位含有脱羧精氨酸模拟物。在各种类似物中，反式-(4-胍基)环己基甲基酰胺(GCMA)被确定为最合适的P1残基。与 P4 位上的二氯取代的苯乙酰基组合，三种抑制剂的抑制常数为
A series of new substrate analogue inhibitors of the WNV NS2BNS3 protease containing decarboxylated arginine mimetics at the P1 position was developed. Among the various analogues, trans-(4-guanidino)cyclohexylmethylamide (GCMA) was identified as the most suitable P1 residue. In combination with dichloro-substituted phenylacetyl groups at the P4 position, three inhibitors with inhibition constants of