Mechanism-based inhibitors of MenE, an acyl-CoA synthetase involved in bacterial menaquinone biosynthesis Journal Article

   

Authors:	Lu, X.; Zhang, H.; Tonge, P. J.; Tan, D. S.
Article Title:	Mechanism-based inhibitors of MenE, an acyl-CoA synthetase involved in bacterial menaquinone biosynthesis
Abstract:	Menaquinone (vitamin K2) is an essential component of the electron transfer chain in many pathogens, including Mycobacterium tuberculosis and Staphylococcus aureus, and menaquinone biosynthesis is a potential target for antibiotic drug discovery. We report herein a series of mechanism-based inhibitors of MenE, an acyl-CoA synthetase that catalyzes adenylation and thioesterification of o-succinylbenzoic acid (OSB) during menaquinone biosynthesis. The most potent compound inhibits MenE with an IC50 value of 5.7 μM. © 2008 Elsevier Ltd. All rights reserved.
Keywords:	unclassified drug; enzyme inhibition; enzyme inhibitor; bacteria (microorganisms); mycobacterium tuberculosis; anti-bacterial agents; esterification; molecular structure; staphylococcus aureus; ic 50; inhibitory concentration 50; benzoic acid derivative; adenylation; antibiotic; respiratory chain; long chain fatty acid coenzyme a ligase; coenzyme a ligases; acyl-coa synthetase; mechanism-based inhibitor; 2 succinylbenzoic acid; menaquinone; protein mene; sulfamic acid derivative; sulfamide derivative; vinyl sulfonamide derivative; vitamin k 2; mene
Journal Title:	Bioorganic & Medicinal Chemistry Letters
Volume:	18
Issue:	22
ISSN:	0960-894X
Publisher:	Pergamon-Elsevier Science Ltd
Date Published:	2008-11-15
Start Page:	5963
End Page:	5966
Language:	English
DOI:	10.1016/j.bmcl.2008.07.130
PUBMED:	18762421
PROVIDER:	scopus
PMCID:	PMC2628629
DOI/URL:	http://www.scopus.com/inward/record.url?eid=2-s2.0-55249100482&partnerID=40&md5=cb1e9f51518bc3af5677f594faf809c9
Notes:	--- - "Cited By (since 1996): 9" - "Export Date: 17 November 2011" - "CODEN: BMCLE" - "Source: Scopus"

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