MurD enzymes from different bacteria: evaluation of inhibitors
Barreteau, Hélène (Author), Sosič, Izidor (Author), Turk, Samo (Author), Humljan, Jan (Author), Tomašič, Tihomir (Author), Zidar, Nace (Author), Hervé, Mireille (Author), Boniface, Audrey (Author), Peterlin-Mašič, Lucija (Author), Kikelj, Danijel (Author), Mengin-Lecreulx, Dominique (Author), Gobec, Stanislav (Author), Blanot, Didier (Author)

URLURL - Presentation file, Visit http://www.sciencedirect.com/science/article/pii/S0006295212004042 This link opens in a new window

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 ŽM.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.

Keywords:D-Glutamic acid-adding enzymes, MurD ligase active sites, MurD ligase inhibitors, pathogenic bacteria, peptidoglycan biosynthesis
Work type:Not categorized (r6)
Tipology:1.01 - Original Scientific Article
Organization:FFA - Faculty of Pharmacy
Number of pages:str. 625-632
Numbering:Vol. 85, issue 5
ISSN on article:0006-2952
DOI:10.1016/j.bcp.2012.06.006 Link is opened in a new window
COBISS.SI-ID:3274609 Link is opened in a new window
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Record is a part of a journal

Title:Biochemical pharmacology
Shortened title:Biochem. pharmacol.
Publisher:Pergamon Press
COBISS.SI-ID:276759 This link opens in a new window

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