Literature DB >> 24376907

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

Phumvadee Wangtrakuldee1, Matthew S Byrd2, Cristine G Campos2, Michael W Henderson2, Zheng Zhang1, Michael Clare3, Ali Masoudi1, Peter J Myler1, James R Horn1, Peggy A Cotter2, Timothy J Hagen1.   

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.

Entities:  

Keywords:  BpMetAP1; Burkholderia pseudomallei; melioidosis; methionine aminopeptidase inhibitor

Year:  2013        PMID： 24376907      PMCID： PMC3871185          DOI： 10.1021/ml400034m

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  19 in total

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