首页> 美国卫生研究院文献>Biochemical Journal >A survey of the kinetic parameters of class C beta-lactamases. Cephalosporins and other beta-lactam compounds.
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A survey of the kinetic parameters of class C beta-lactamases. Cephalosporins and other beta-lactam compounds.

机译:C类β-内酰胺酶动力学参数的调查。头孢菌素和其他β-内酰胺化合物。

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摘要

Various cephalosporins, cefoxitin, moxalactam, imipenem and aztreonam were studied as substrates of six class C beta-lactamases. Nitrocefin, cephaloridine, cefazolin, cephalothin and cephalexin were good substrates, with kcat. values ranging from 27 to 5000 s-1. Cefuroxime, cefotaxime and cefoxitin exhibited low kcat. values (0.010-1.7 s-1) and low Km values, which suggested a rate-limiting deacylation. Imipenem and aztreonam were even poorer substrates (kcat. 2 x 10(-4)-3 x 10(-2) s-1) and, in the presence of a reporter substrate, behaved as transient inactivators. With moxalactam, biphasic kinetics were observed, indicating a possible rearrangement of the acyl-enzyme.
机译:研究了各种头孢菌素,头孢西丁,莫拉西坦,亚胺培南和氨曲南作为六种C类β-内酰胺酶的底物。硝苯蝶呤,头孢啶,头孢唑林,头孢菌素和头孢氨苄是良好的底物,并伴有卡卡特。值范围从27到5000 s-1。头孢呋辛,头孢噻肟和头孢西丁表现出低kcat。值(0.010-1.7 s-1)和低Km值,表明存在限速脱酰作用。亚胺培南和氨曲南是更差的底物(kcat。2 x 10(-4)-3 x 10(-2)s-1),在有报道分子底物的情况下,它们可作为瞬时灭活剂。对于莫拉西坦,观察到双相动力学,表明酰基酶可能重新排列。

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