کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1376507 981959 2006 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Sesquiterpene lactones are potent and irreversible inhibitors of the antibacterial target enzyme MurA
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Sesquiterpene lactones are potent and irreversible inhibitors of the antibacterial target enzyme MurA
چکیده انگلیسی

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.

Certain sesquiterpene lactones are potent inhibitors of the antibacterial target enzyme MurA. We present structure–activity relationships and discuss biological implications.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 21, 1 November 2006, Pages 5605–5609
نویسندگان
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