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Drug Discov Today. 2001 May 1;6(10):537-544.

Bacterial fatty-acid biosynthesis: a genomics-driven target for antibacterial drug discovery.

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1
Antimicrobials and Host Defence, 1250 South Collegeville Road, 19426, Collegeville, PA, USA

Abstract

In this review we demonstrate how the interplay of genomics, bioinformatics and genomic technologies has enabled an in-depth analysis of the component enzymes of the bacterial fatty-acid biosynthesis pathway as a source of novel antibacterial targets. This evaluation has revealed that many of the enzymes are potentially selective, broad-spectrum antibacterial targets. We also illustrate the suitability of some of these targets for HTS. Furthermore, we discuss how the availability of a robust selectivity assay, mode-of-action assays and numerous crystal structures provide an excellent set of tools with which to initiate integrated programs of research to identify novel antibiotics targeted at these enzymes.

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