突变改变的二氢蝶酸合酶的特性及其形成含磺酰胺二氢叶酸类似物的能力。
Characterization of mutationally altered dihydropteroate synthase and its ability to form a sulfonamide-containing dihydrofolate analog.
作者信息
Swedberg G, Castensson S, Sköld O
出版信息
J Bacteriol. 1979 Jan;137(1):129-36. doi: 10.1128/jb.137.1.129-136.1979.
Abstract
Among spontaneous mutants of Escherichia coli selected for resistance against sulfonamides, thermosensitive strains were found. These were shown to possess a changed dihydropteroate synthase (EC 2.5.1.15), which had a substantially higher Km value for its normal substrate, p-aminobenzoic acid, and an about 150-fold higher Km for sulfonamides. The mutationally changed dihydropteroate synthase was found to be thermosensitive by in vitro assays. The thermosensitivity was used as an enzyme marker to demonstrate the complex formation between 2-amino-4-hydroxy-6-pyrophosphorylmethyl pteridine and sulfonamides by partially purified dihydropteroate synthase. The formation of folate from 2-amino-4-hydroxy-6-pyrophosphorylmethyl pteridine and p-aminobenzoylglutamic acid by dihydropteroate synthase was found to be very sensitive to inhibition by sulfonamides and very inefficient with the mutationally changed enzyme.
摘要
在为抗磺胺类药物而筛选出的大肠杆菌自发突变体中，发现了热敏菌株。这些菌株被证明具有一种改变的二氢蝶酸合酶（EC 2.5.1.15），它对其正常底物对氨基苯甲酸具有显著更高的Km值，而对磺胺类药物的Km值约高150倍。通过体外测定发现，突变改变的二氢蝶酸合酶是热敏的。热敏性被用作酶标记，以证明部分纯化的二氢蝶酸合酶催化2-氨基-4-羟基-6-焦磷酸甲基蝶啶与磺胺类药物之间形成复合物。发现二氢蝶酸合酶由2-氨基-4-羟基-6-焦磷酸甲基蝶啶和对氨基苯甲酰谷氨酸形成叶酸的过程对磺胺类药物的抑制非常敏感，并且使用突变改变的酶时效率非常低。
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