C类β-内酰胺酶动力学参数的研究。头孢菌素及其他β-内酰胺类化合物。
A survey of the kinetic parameters of class C beta-lactamases. Cephalosporins and other beta-lactam compounds.
作者信息
Galleni M, Amicosante G, Frère J M
机构信息
Laboratoire d'Enzymologie, Université de Liège, Sart Tilman, Belgium.
出版信息
Biochem J. 1988 Oct 1;255(1):123-9. doi: 10.1042/bj2550123.
Abstract
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.
摘要
研究了多种头孢菌素、头孢西丁、拉氧头孢、亚胺培南和氨曲南作为六种C类β-内酰胺酶的底物情况。硝基头孢菌素、头孢噻啶、头孢唑林、头孢噻吩和头孢氨苄是良好的底物，其kcat.值范围为27至5000 s-1。头孢呋辛、头孢噻肟和头孢西丁表现出较低的kcat.值（0.010 - 1.7 s-1）和较低的Km值，这表明存在限速脱酰基作用。亚胺培南和氨曲南是更差的底物（kcat.为2×10(-4) - 3×10(-2) s-1），并且在存在报告底物的情况下，表现为瞬时失活剂。对于拉氧头孢，观察到双相动力学，表明酰基酶可能发生重排。
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