具有抗菌活性的甲硫氨酸氨肽酶抑制剂的发现。
Discovery of Inhibitors of Methionine Aminopeptidase with Antibacterial Activity.
作者信息
Wangtrakuldee Phumvadee, Byrd Matthew S, Campos Cristine G, Henderson Michael W, Zhang Zheng, Clare Michael, Masoudi Ali, Myler Peter J, Horn James R, Cotter Peggy A, Hagen Timothy J
机构信息
Department of Chemistry and Biochemistry, Northern Illinois University, 1425 West Lincoln Highway, DeKalb, Illinois 60115-2828, United States.
Department of Microbiology and Immunology, University of North Carolina, 116 Manning Drive, Chapel Hill, North Carolina 27599, United States.
出版信息
ACS Med Chem Lett. 2013 Jul 1;4(8):699-703. doi: 10.1021/ml400034m.
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 IC of 30 nM, and inhibit the growth of B. pseudomallei and B. thailandensis at concentrations ≥ 31 μM.
摘要
在体外酶活性测定中对一系列甲硫氨酸氨肽酶（MetAP）抑制剂进行评估，首次鉴定出了对类鼻疽伯克霍尔德菌具有显著生长抑制作用的强效分子。硝氧喹啉类似物在BpMetAP1酶活性测定中显示出优异的抑制效力，最低半数抑制浓度（IC）为30 nM，并在浓度≥31 μM时抑制类鼻疽伯克霍尔德菌和泰国伯克霍尔德菌的生长。
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