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G蛋白偶联受体失敏的分子机制 被引量:3

Molecular Mechanism of G Protein-coupled Receptors Desensitization
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摘要 G蛋白偶联受体(GPCRs)受到激动剂持续刺激时易发生失敏.受体内化是GPCRs失敏重要分子机制.GPCRs在G蛋白偶联受体激酶(GRKs)、第二信使调节激酶等作用下发生磷酸化,磷酸化的GPCRs与抑制蛋白(arrestins)结合后导致受体与G蛋白失偶联,并通过胞吞由细胞膜表面向膜内转移,从而因GPCRs的内化而表现为失敏. Desensitization may occur in G proteincoupled receptors(GPCRs) when agonists exist continuously.Internalization is an important mechanism of GPCRs desensitization.Phosphorylation of GPCRs happens under the action of G proteincoupled receptor kinases(GRKs) or the second messenger dependent kinases.The combination of phosphorylated GRCPs and arrestins leads to the decoupling of GRCPs with G protein,then GRCPs transfer to the internal surface of cell membrane and thus desensitization of GRCPs occurs.
出处 《生命科学研究》 CAS CSCD 2003年第1期15-19,共5页 Life Science Research
基金 国家自然科学基金资助项目(30070334) 国家自然科学基金资助项目(39730210)
关键词 失敏 G蛋白偶联受体 磷酸化 内化 胞吞 desensitazation G protein-coupled receptor phosphorylization internalization endocytosis
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参考文献15

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同被引文献31

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