受体与细胞功能调控 2015研究生受体第三次.pptVIP

Chapter 5 G-protein coupled seven TMS (transmembranous segment) receptor（GPCR） and post-receptor signal transduction;;（ G蛋白的分类 ：Subtypes of G? (% of homology) ;1. Fundamental structure of G-protein Heterotrimer: ?(39~52KDa)、?(35~36)、?(6~10) Function of G?：Coupling to receptor, signal transduction Functional domains of G?： ;Receptor - G protein;G蛋白（主要起信号转导）; Native cell membrane/G-proteins, using Site directed antibodies to block G-protein activation Cholera toxin (CTx) to inhibit certain Gi Antisense oligonucleotides to block normal G-protein sysnthesis ;3. Receptor agonist dependent G-protein activation;3. Receptor agonist dependent G-protein activation;3. Receptor agonist dependent G-protein activation;3. Receptor agonist dependent G-protein activation;3. Receptor agonist dependent G-protein activation;3. Receptor agonist dependent G-protein activation;3. Receptor agonist dependent G-protein activation;4. Endogenous GTPase de-activate G-protein;5. Function of ?? dimer (not extensively studied);受体特点：激活G蛋白（一种与三磷酸鸟苷结合的膜蛋 白质）、细胞内产生第二信使 改变 其他酶活性七跨膜型受体 G蛋白特点：介导的信号转导反应是一种慢速的过程， 经历时间长，但是敏感性高，灵活性大。 第二信使：cAMP、Ca++、IP3(肌醇1,4,5-三磷酸)、 DAG（二酯酰甘油）等。 ; cAMP pathway Phosphatidylinositol pathway G?s、G?i、G?12 G?q Adenylate cyclase (AC) Phospholipase C (PLC) Protein kinase A (PKA) Hydrolysis of 4,5-diphospho- Intracellular cAMP phosphatidyl inositol (PIP2) Protein phosphorylation IP3（Ca2+）+ DAG Biological effect Biological effect ;与G蛋白相互作用的效应蛋白;Second Messenger (Sutherland, 1972 Nobel Prize);1.Cyclic AMP pathway of G-protein signal transduction ;2. Activate Protein kinase A, PKA ;3. Action of cAMP: