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Assay development and inhibition of the Mt-DprE2 essential reductase from Mycobacterium tuberculosis

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By Beatriz L. Rodriguez, Beatriz Rodríguez Verified, Sarah M. Batt, Szilvi Toth, Katherine A. Abrahams
| Microbiology Research
DprE2 is an essential enzyme in the synthesis of decaprenylphosphoryl-β-d-arabinofuranose (DPA) and subsequently arabinogalactan, and is a significant new drug target for M. tuberculosis . Two compounds from the GSK-177 box set, GSK301A and GSK032A, were identified through Mt-DprE2-target overexpression studies. The Mt-DprE1-DprE2 complex was co-purified and a new in vitro DprE2 assay developed, based on the oxidation of the reduced nicotinamide adenine dinucleotide cofactor of DprE2 (NADH/NADPH).
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