| 李胜,白波,陈京.G蛋白偶联受体脱敏內吞和复敏调控机制进展[J].济宁医学院学报,2016,39(2):123-127,132 |
| G蛋白偶联受体脱敏內吞和复敏调控机制进展 |
| Regulatory mechanisms of G protein coupled receptor about desensitization, endocytosis and resensitization |
| 投稿时间：2016-02-09 |
| DOI：10.3969/j.issn.1000-9760.2016.02.013 |
| 中文关键词: G蛋白偶联受体;信号转导;脱敏;內吞;复敏;网格蛋白 |
| 英文关键词: G protein-coupled receptor;signal transduction;desensitization;endocytosis;resensitization;clathrin |
| 基金项目:国家自然科学基金项目(3097108;31271243;81070961); 山东省自然科学基金项目(ZR2011CM027;2012GSF11806);山东省高校科技计划项目(JY2015KJ004) |
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| 中文摘要: |
| G蛋白偶联受体是哺乳动物细胞表面最大的膜受体家族,目前人类研发的药物中,近一半的药物都直接或间接的作用于G蛋白偶联受体信号通路。脱敏、内吞以及复敏是G蛋白偶联受体在时间和空间方面调控信号传导的关键,网格蛋白、衔接蛋白等在受体內吞过程中发挥着重要作用。本文简要阐述了G蛋白偶联受体的信号转导通路和激动剂的过刺激所导致的受体脱敏、內吞的负反馈调控机制,以及受体复敏的再循环途径,并探讨了网格蛋白抑制剂在临床中的药理作用,从而为相关疾病的治疗提供理论依据。 |
| 英文摘要: |
| G protein coupled receptor (GPCR) is one of the biggest mammal cell surface membrane receptor family,in the research and development of human medicine,nearly half of drugs have direct or indirect effects on GPCR signaling pathways.Desensitization,endocytosis and the resensitization are the key processes of GPCR regulation of signal transduction in terms of time and space.Both clathrin and AP2 play important roles in the process of endocytosis.In this paper we aimed to describe the signal transduction pathway of GPCR,summarize the negative feedback regulation of desensitization and endocytosis caused by continuous stimulation of agonist.Recycling pathway of receptor resensitization and discuss the pharmacological function of clathrin inhibitors in clinical practice so as to provide theoretical basis for the pathogenesis of related diseases. |
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