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Article

Antituberculosis thiophenes define a requirement for Pks13 in mycolic acid biosynthesis.

Nature chemical biology - 1 Aug 2013

Wilson Regina, Kumar Pradeep, Parashar Vijay, Vilchèze Catherine, Veyron-Churlet Romain, Freundlich Joel S, Barnes S Whitney, Walker John R, Szymonifka Michael J, Marchiano Emily, Shenai Shubhada, Colangeli Roberto, Jacobs William R, Neiditch Matthew B, Kremer Laurent, Alland David

Abstract excerpt

We report a new class of thiophene (TP) compounds that kill Mycobacterium tuberculosis by the previously uncharacterized mechanism of Pks13 inhibition. An F79S mutation near the catalytic Ser55 site in Pks13 conferred TP resistance in M. tuberculosis. Overexpression of wild-type Pks13 resulted in TP resistance, and overexpression of the Pks13(F79S) mutant conferred high resistance. In vitro, TP inhibited fatty...

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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

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Identifiers

PMID: 23770708
DOI: 10.1038/nchembio.1277
PMCID: PMC3720791

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