aspergillomarasmine A，一种细菌金属β-内酰胺酶抑制剂，赋予 blaNDM 和 blaVIM 耐药性。
Aspergillomarasmine A, an inhibitor of bacterial metallo-β-lactamases conferring blaNDM and blaVIM resistance.
机构信息
Global Drug Discovery, Bayer HealthCare.
出版信息
Angew Chem Int Ed Engl. 2014 Oct 27;53(44):11696-8. doi: 10.1002/anie.201407921. Epub 2014 Sep 24.
PMID:25256630
Abstract
Silencing the deadly "bla-bla" of superbugs: The natural product aspergillomarasmine A (AMA) showed in vivo efficacy against Enterobacteriaceae, conferring broad β-lactam resistance blaNDM-1 (NDM-1: New Delhi Metallo-β-lactamase 1). In rodents, the natural product restored efficacy of the gold standard meropenem by inhibition of the Zn-containing active site in NDM-1.
摘要
沉默的致命的“bla-bla”超级细菌：天然产物aspergillomarasmine A (AMA) 表现出对肠杆菌科的体内疗效，赋予广泛的β-内酰胺耐药 blaNDM-1 (NDM-1: 新德里金属β-内酰胺酶 1)。在啮齿动物中，该天然产物通过抑制 NDM-1 中含锌的活性位点，恢复了金标准美罗培南的疗效。
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