title: Discovery of Inhibitors ofBurkholderia pseudomalleiMethionine Aminopeptidase with Antibacterial Activity.
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 IC50of 30 nM, and inhibit the growth of B. pseudomallei and B. thailandensis at concentrations ≥ 31 μM.
authors.affiliation: Department of Chemistry and Biochemistry, Northern Illinois University, 1425 West Lincoln Highway, DeKalb, Illinois 60115-2828, United States.
authors.forename: Phumvadee
authors.initials: P
authors.lastname: Wangtrakuldee
authors.affiliation: Department of Microbiology and Immunology, University of North Carolina, 116 Manning Drive, Chapel Hill, North Carolina 27599, United States.
authors.forename: Matthew S
authors.initials: MS
authors.lastname: Byrd
authors.affiliation: Department of Microbiology and Immunology, University of North Carolina, 116 Manning Drive, Chapel Hill, North Carolina 27599, United States.
authors.forename: Cristine G
authors.initials: CG
authors.lastname: Campos
authors.affiliation: Department of Microbiology and Immunology, University of North Carolina, 116 Manning Drive, Chapel Hill, North Carolina 27599, United States.
authors.forename: Michael W
authors.initials: MW
authors.lastname: Henderson
authors.affiliation: Department of Chemistry and Biochemistry, Northern Illinois University, 1425 West Lincoln Highway, DeKalb, Illinois 60115-2828, United States.
authors.forename: Zheng
authors.initials: Z
authors.lastname: Zhang
authors.affiliation: Clare Associates LLC, 5154 West Brown Street, Skokie, Illinois 60077, United States.
authors.forename: Michael
authors.initials: M
authors.lastname: Clare
authors.affiliation: Department of Chemistry and Biochemistry, Northern Illinois University, 1425 West Lincoln Highway, DeKalb, Illinois 60115-2828, United States.
authors.forename: Ali
authors.initials: A
authors.lastname: Masoudi
authors.affiliation: Department of Chemistry and Biochemistry, Northern Illinois University, 1425 West Lincoln Highway, DeKalb, Illinois 60115-2828, United States.
authors.forename: Peter J
authors.initials: PJ
authors.lastname: Myler
authors.affiliation: Department of Chemistry and Biochemistry, Northern Illinois University, 1425 West Lincoln Highway, DeKalb, Illinois 60115-2828, United States.
authors.forename: James R
authors.initials: JR
authors.lastname: Horn
authors.affiliation: Department of Microbiology and Immunology, University of North Carolina, 116 Manning Drive, Chapel Hill, North Carolina 27599, United States.
authors.forename: Peggy A
authors.initials: PA
authors.lastname: Cotter
authors.affiliation: Department of Chemistry and Biochemistry, Northern Illinois University, 1425 West Lincoln Highway, DeKalb, Illinois 60115-2828, United States.
authors.forename: Timothy J
authors.initials: TJ
authors.lastname: Hagen
keywords: BpMetAP1; Burkholderia pseudomallei; melioidosis; methionine aminopeptidase inhibitor