Sesquiterpene lactones are potent and irreversible inhibitors of the antibacterial target enzyme MurA
Sesquiterpene lactones are potent and irreversible inhibitors of the antibacterial target enzyme MurA
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DOI：
10.1016/j.bmcl.2006.08.021
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发表时间：
2006-11-01
影响因子：
2.7
通讯作者：
Klein, Christian D.
中科院分区：
文献类型：
--
作者：
Bachelier, Anke;Mayer, Ralf;Klein, Christian D.
我们报告了倍半萜内酯、金雀异黄素和野百合苦苷是细菌酶Mura的有效的、不可逆转的抑制物。它们与Cys115的硫醇基团共价结合。根据构效关系，我们得出结论，不饱和酯侧链对抑制Mura具有特别重要的作用。这些结果证明Mura是SLS的靶蛋白，可能与其已知的抗菌作用有很高的相关性。(C)2006爱思唯尔有限公司。保留所有权利。
We report the identification of the sesquiterpene lactones cnicin and cynaropicrin as potent, irreversible inhibitors of the bacterial enzyme MurA. They covalently bind to the thiol group of Cys115. Judging from the structure-activity relationships, we conclude that the unsaturated ester side chain of cynaropicrin and cnicin is of particular importance for the inhibition of MurA. These results provide evidence that MurA is a target protein of SLs with a probably high relevance for their known antibacterial effect. (c) 2006 Elsevier Ltd. All rights reserved.