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β-内酰胺酶诱导的重要性。

Importance of beta-lactamase induction.

作者信息

Phillips I, Shannon K

机构信息

Department of Microbiology, United Medical School, St. Thomas' Hospital, London, UK.

出版信息

Eur J Clin Microbiol Infect Dis. 1993;12 Suppl 1:S19-26. doi: 10.1007/BF02389873.

Abstract

Induction of an enzyme is a temporary phenomenon in which the rate of enzyme synthesis is greatly increased in response to the presence of an inducer in the environment. Induction of beta-lactamase synthesis is important for the resistance of staphylococci to penicillins since the drug both induces synthesis of the enzyme and is hydrolysed by it. Similarly, some compounds both strongly induce and are hydrolysed by the chromosomally-determined beta-lactamases of gram-negative bacilli (e.g. amoxicillin and cefoxitin for Enterobacter cloacae). Other compounds (e.g. piperacillin and cefotaxime) although labile are poor inducers, so that in the case of these drugs the phenomenon of induction is not important but the presence of the enzyme is, since resistant mutants with genetically derepressed synthesis of the enzyme can emerge. Induction can also be important when a strong inducer is present with a poor inducer and antagonises the activity of the latter.

摘要

酶的诱导是一种暂时现象,在此现象中,由于环境中存在诱导剂,酶的合成速率大幅增加。β-内酰胺酶合成的诱导对于葡萄球菌对青霉素的耐药性很重要,因为药物既诱导该酶的合成,又会被它水解。同样,一些化合物既能强烈诱导革兰氏阴性杆菌的染色体决定的β-内酰胺酶(例如阴沟肠杆菌的阿莫西林和头孢西丁),又会被其水解。其他化合物(例如哌拉西林和头孢噻肟)虽然不稳定,但诱导能力较差,因此对于这些药物而言,诱导现象并不重要,但酶的存在很重要,因为可能会出现具有该酶基因去阻遏合成的耐药突变体。当强诱导剂与弱诱导剂同时存在并拮抗后者的活性时,诱导也可能很重要。

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