比阿培南与活性位点丝氨酸和金属β-内酰胺酶的相互作用。
Interactions of biapenem with active-site serine and metallo-beta-lactamases.
作者信息
Felici A, Perilli M, Segatore B, Franceschini N, Setacci D, Oratore A, Stefani S, Galleni M, Amicosante G
机构信息
Dipartimento di Scienze e Tecnologie Biomediche e di Biometria, Università degli Studi dell'Aquila, Italy.
出版信息
Antimicrob Agents Chemother. 1995 Jun;39(6):1300-5. doi: 10.1128/AAC.39.6.1300.
Abstract
Biapenem, formerly LJC 10,627 or L-627, a carbapenem antibiotic, was studied in its interactions with 12 beta-lactamases belonging to the four molecular classes proposed by R. P. Ambler (Philos. Trans. R. Soc. Lond. Biol. Sci. 289:321-331, 1980). Kinetic parameters were determined. Biapenem was readily inactivated by metallo-beta-lactamases but behaved as a transient inhibitor of the active-site serine enzymes tested, although with different acylation efficiency values. Class A and class D beta-lactamases were unable to confer in vitro resistance toward this carbapenem antibiotic. Surprisingly, the same situation was found in the case of class B enzymes from Aeromonas hydrophila AE036 and Bacillus cereus 5/B/6 when expressed in Escherichia coli strains.
摘要
比阿培南，曾用名LJC 10,627或L - 627，是一种碳青霉烯类抗生素，对其与属于R. P. 安布勒提出的四个分子类别的12种β-内酰胺酶的相互作用进行了研究（《英国皇家学会会报B辑：生物科学》289:321 - 331, 1980）。测定了动力学参数。比阿培南很容易被金属β-内酰胺酶灭活，但对所测试的活性位点丝氨酸酶表现为瞬时抑制剂，不过酰化效率值不同。A类和D类β-内酰胺酶不能赋予对这种碳青霉烯类抗生素的体外抗性。令人惊讶的是，当嗜水气单胞菌AE036和蜡样芽孢杆菌5/B/6的B类酶在大肠杆菌菌株中表达时，也出现了同样的情况。
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