变性作用 (denaturation):变性剂没有选择性

抑制作用 (inhibition):使酶活力下降或丧失但并不引起酶蛋白变性。抑制剂有不同程度的选择性。

研究抑制剂对酶的作用有重大的意义:

(1)药物作用机理和抑制剂型药物的设计与开发; (2)了解生物体的代谢途径,进行人为调控或代谢控制发酵; . (3)通过抑制剂试验研究酶活性中心的构象及其化学功能基团,不仅可以设计药物,而且也是酶工程和化学修饰酶、酶工业的基础。

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可逆,不可逆抑制剂的区别

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EDTA 羧基 - - 螯合金属离子

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抑制 叶酸的合成→核酸合成受抑制→细菌生长受抑

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典型的竞争性抑制剂:磺胺类药物,掌握其抗菌机理。

磺胺药物的作用机理为:磺胺类药物的结构母体为对氨基苯磺酰胺,该物质与细菌生长所必 需的对氨基苯甲酸(PABA)结构相似;二氢叶酸合成酶的作用是催化 PABA 合成二氢叶酸,磺胺药物以其结构的相似性可以竞争性抑制二氢叶酸合成酶 的活性及二氢叶酸的生物合成。二氢叶酸的产物四氢叶酸是一碳单位载体, 在碱基及核酸合成中都有重要作用,因此磺胺类药物会抑制微生物的生长繁 殖,而人体作为微生物的宿主,可以从食物中摄取四氢叶酸,不影响人体的正常代谢