金黄色葡萄球菌中质粒介导的甲氧苄啶耐药性。首例革兰氏阳性质粒二氢叶酸还原酶（S1型）的特性分析。
Plasmid-mediated trimethoprim-resistance in Staphylococcus aureus. Characterization of the first gram-positive plasmid dihydrofolate reductase (type S1).
作者信息
Young H K, Skurray R A, Amyes S G
出版信息
Biochem J. 1987 Apr 1;243(1):309-12. doi: 10.1042/bj2430309.
Abstract
The trimethoprim-resistance gene located on plasmid pSK1, originally identified in a multi-resistant Staphylococcus aureus from Australia, encodes the production of a dihydrofolate reductase (type S1), which confers a high degree of resistance to its host and is quite unlike any plasmid-encoded dihydrofolate reductase hitherto described. It has a low Mr (19,700) and has a higher specific activity than the constitutive Gram-negative plasmid dihydrofolate reductases. The type S1 enzyme is heat-stable and has a relatively low affinity for the substrate, dihydrofolate (Km 10.8 microM). It is moderately resistant to trimethoprim, and is competitively inhibited by this drug with an inhibitor-binding constant of 11.6 microM. This is the first identification and characterization of a plasmid-encoded trimethoprim-resistant dihydrofolate reductase derived from a Gram-positive species.
摘要
位于质粒pSK1上的甲氧苄啶抗性基因最初是在一株来自澳大利亚的多重耐药金黄色葡萄球菌中鉴定出来的，它编码一种二氢叶酸还原酶（S1型）的产生，这种酶赋予宿主高度抗性，并且与迄今描述的任何质粒编码的二氢叶酸还原酶都截然不同。它的分子量较低（19,700），比组成型革兰氏阴性质粒二氢叶酸还原酶具有更高的比活性。S1型酶耐热，对底物二氢叶酸的亲和力相对较低（Km为10.8微摩尔）。它对甲氧苄啶具有中等抗性，并且被这种药物竞争性抑制，抑制剂结合常数为11.6微摩尔。这是首次对源自革兰氏阳性菌的质粒编码的甲氧苄啶抗性二氢叶酸还原酶进行鉴定和表征。
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