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ID: ALA2406976

Journal: ACS Med Chem Lett

Title: Discovery of Inhibitors of Burkholderia pseudomallei Methionine Aminopeptidase with Antibacterial Activity.

Authors: Wangtrakuldee P, Byrd MS, Campos CG, Henderson MW, Zhang Z, Clare M, Masoudi A, Myler PJ, Horn JR, Cotter PA, Hagen TJ.

Abstract: Evaluation of a series of MetAP inhibitors in an in vitro enzyme activity assay led to the first identification of potent molecules that show significant growth inhibition against Burkholderia pseudomallei. Nitroxoline analogs show excellent inhibition potency in the BpMetAP1 enzyme activity assay with the lowest IC50 of 30 nM, and inhibit the growth of B. pseudomallei and B. thailandensis at concentrations ≥ 31 μM.

CiteXplore: 24376907

DOI: 10.1021/ml400034m