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目的 1:一种具有机制灵活性的抗生素降解金属水解酶。

AIM-1: An Antibiotic-Degrading Metallohydrolase That Displays Mechanistic Flexibility.

机构信息

School of Chemistry and Molecular Biosciences, The University of Queensland, St. Lucia, Queensland, 4072, Australia.

Department of Chemistry and Biochemistry, Middlebury College, Middlebury, Vermont, 05753, USA.

出版信息

Chemistry. 2016 Dec 5;22(49):17704-17714. doi: 10.1002/chem.201602762. Epub 2016 Oct 25.

Abstract

Antibiotic resistance has emerged as a major threat to global health care. This is largely due to the fact that many pathogens have developed strategies to acquire resistance to antibiotics. Metallo-β-lactamases (MBL) have evolved to inactivate most of the commonly used β-lactam antibiotics. AIM-1 is one of only a few MBLs from the B3 subgroup that is encoded on a mobile genetic element in a major human pathogen. Here, its mechanism of action was characterised with a combination of spectroscopic and kinetic techniques and compared to that of other MBLs. Unlike other MBLs it appears that AIM-1 has two avenues available for the turnover of the substrate nitrocefin, distinguished by the identity of the rate-limiting step. This observation may be relevant with respect to inhibitor design for this group of enzymes as it demonstrates that at least some MBLs are very flexible in terms of interactions with substrates and possibly inhibitors.

摘要

抗生素耐药性已成为全球医疗保健的主要威胁。这主要是因为许多病原体已经发展出对抗生素产生耐药性的策略。金属β-内酰胺酶(MBL)已经进化到可以使大多数常用的β-内酰胺类抗生素失活。AIM-1 是 B3 亚组中仅有的几种 MBL 之一,它编码在一种主要人类病原体的移动遗传元件上。在这里,我们使用光谱和动力学技术相结合的方法来研究其作用机制,并与其他 MBL 进行了比较。与其他 MBL 不同,AIM-1 似乎有两种途径可用于底物硝基头孢菌素的转化,这两种途径的限速步骤不同。这一观察结果可能与该酶组抑制剂的设计有关,因为它表明至少一些 MBL 在与底物和可能的抑制剂相互作用方面非常灵活。

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