Overview of the Development of DprE1 Inhibitors for Combating the Menace of Tuberculosis

Chikhale, Rupesh V., Barmade, Mahesh A., Murumkar, Prashant R. and Yadav, Mange Ram (2018) Overview of the Development of DprE1 Inhibitors for Combating the Menace of Tuberculosis. Journal of Medicinal Chemistry, 61 (19). 8563–8593. ISSN 0022-2623

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Abstract

Decaprenylphosphoryl-β-d-ribose 2′-epimerase (DprE1), a vital enzyme for cell wall synthesis, plays a crucial role in the formation of lipoarabinomannan and arabinogalactan. It was first reported as a druggable target on the basis of inhibitors discovered in high throughput screening of a drug library. Since then, inhibitors with different types of chemical scaffolds have been reported for their activity against this enzyme. Formation of a covalent or noncovalent bond by the interacting ligand with the enzyme causes loss of its catalytic activity which ultimately leads to the death of the mycobacterium. This Perspective describes various DprE1 inhibitors as anti-TB agents reported to date.

Item Type: Article
Faculty \ School: Faculty of Science > School of Pharmacy
Depositing User: LivePure Connector
Date Deposited: 17 Aug 2020 23:54
Last Modified: 17 Aug 2020 23:54
URI: https://ueaeprints.uea.ac.uk/id/eprint/76460
DOI: 10.1021/acs.jmedchem.8b00281

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