第4章-以酶为靶点的药物设计综述.pptVIP

Chapter 4. Drug Design based on Enzyme as Targets ; Section 1. Basic Knowledge of Enzyme;I. kinetics of enzyme-catalyzed reactions ;II. Interaction of E-I complex;Activation and Inhibition of Enzyme ;II. Inhibition of Enzyme;竞争性抑制 非竞争性抑制 反竞争性抑制;Type of reversible inhibitors;I. Enzyme Inhibitor Drugs;II. Dsign Principles Enzyme Inhibitors;（一）基于非共价结合的酶抑制剂的合理设计：;2. multisubstrate analog inhibitors 酶催化反应：活性位点同时结合两个或多个底物，底物有特殊的空间趋向并彼此接近。 多底物类似物模拟同时结合在酶的活性位点的两个或多个底物的结构，通过共价键把两个或多个底物或底物类似物结合在一起。 优点：与靶酶结合力大大增强，并且特异性更高。;3. transition-state analog inhibitors 底物——产