کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
2513150 1118397 2012 8 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
MurD enzymes from different bacteria: Evaluation of inhibitors
موضوعات مرتبط
علوم پزشکی و سلامت داروسازی، سم شناسی و علوم دارویی داروشناسی
پیش نمایش صفحه اول مقاله
MurD enzymes from different bacteria: Evaluation of inhibitors
چکیده انگلیسی

d-Glutamic acid-adding enzyme (MurD ligase) catalyses the addition of d-glutamic acid to UDP-N-acetylmuramoyl-l-alanine, an essential cytoplasmic step in the pathway for bacterial cell-wall peptidoglycan synthesis. As such, it represents an important antibacterial drug-discovery target enzyme. Recently, several series of compounds have been synthesised and found to inhibit MurD from Escherichia coli, the best one having an IC50 value of 8 μM. In the present work, we have tested 20 of these compounds against the MurD enzymes from Staphylococcus aureus, Streptococcus pneumoniae, Borrelia burgdorferi and Mycobacterium tuberculosis. Most of the E. coli MurD inhibitors appeared less efficient against the four other orthologues. This divergent result can be explained by the differences in amino acid sequences and topologies of the active sites of the MurD ligases studied.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Biochemical Pharmacology - Volume 84, Issue 5, 1 September 2012, Pages 625–632
نویسندگان
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