1qsg

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spinqualitylabelsall models 1qsg, resolution 1.75Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image

CRYSTAL STRUCTURE OF ENOYL REDUCTASE INHIBITION BY TRICLOSAN

Overview

The enoyl-acyl carrier protein reductase (ENR) is involved in bacterial, fatty acid biosynthesis and is the target of the antibacterial diazaborine, compounds and the front-line antituberculosis drug isoniazid. Recent, studies suggest that ENR is also the target for the broad-spectrum biocide, triclosan. The 1.75 A crystal structure of EnvM, the ENR from Escherichia, coli, in complex with triclosan and NADH reveals that triclosan binds, specifically to EnvM. These data provide a molecular mechanism for the, antibacterial activity of triclosan and substantiate the hypothesis that, its activity results from inhibition of a specific cellular target rather, than non-specific disruption of the bacterial cell membrane. This has, important implications for the emergence of drug-resistant bacteria, since, triclosan is an additive in many personal care products such as, toothpastes, mouthwashes and soaps. Based on this structure, rational, design of triclosan derivatives is possible which might be effective, against recently identified triclosan-resistant bacterial strains.

About this Structure

1QSG is a Single protein structure of sequence from Escherichia coli with GLC, NAD and TCL as ligands. Active as [acyl-carrier-protein_reductase_(NADH) Enoyl-[acyl-carrier-protein] reductase (NADH)], with EC number 1.3.1.9 Full crystallographic information is available from OCA.

Reference

Structural basis and mechanism of enoyl reductase inhibition by triclosan., Stewart MJ, Parikh S, Xiao G, Tonge PJ, Kisker C, J Mol Biol. 1999 Jul 23;290(4):859-65. PMID:10398587 [[Category: Enoyl-[acyl-carrier-protein] reductase (NADH)]]

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