调查isoprenylation的功能要求的人类环前列腺素受体。
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Miggin SM, Lawler OA, Kinsella BT
调查isoprenylation的功能要求的人类环前列腺素受体。
3月。2002欧元;269(6):1714 - 25所示。
- PubMed ID
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11895442 (在PubMed]
- 文摘
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在当前的研究中,我们建立了人类(h)环前列腺素受体(IP)是isoprenylated在整个细胞。通过网站直接诱变和代isoprenylation缺陷hIPSSLC,成立,虽然isoprenylation臀部不影响配体结合,是义务的受体激动剂激活腺苷酸环化酶和营地的一代。过度的GalphaS显著增强营hIPSSLC臀部而不是一代的。此外,GalphaS co-immunoprecipitated与臀部受体激动剂激活后但没有co-immunoprecipitate hIPSSLC。而臀部介导浓度激活磷脂酶C (PLC);PLC激活的程度由hIPSSLC受损而时髦。Co-expression Galphaq显著augmentated胞内钙动员臀部而不是hIPSSLC。此外,而Galphaq co-immunoprecipitated臀部,未能与hIPSSLC co-immunoprecipitate。在臀部和hIPSSLC接受agonist-induced内化,hIPSSLC内化的动力学和程度受损而时髦。改变CAAX臀部的主题通过(-CSLC) geranylgeranyl (-CSLL)异戊二烯受体,产生hIPCSLL,并不影响配体结合,产生了一个受体,它表现出相同的信号通过Gs和Gq-coupled效应器的臀部。 Thus, whereas isoprenylation of hIP does not influence ligand binding, it is functionally imperative in regulating post-receptor events including agonist-activation of adenylyl cyclase, for efficient activation of PLC and for receptor internalization. Though the nature of the isoprenoid attached to hIP does not act as a major determinant, the presence of an isoprenoid group, for example farnesyl or geranylgeranyl, is required for functional receptor-G protein interaction and coupling and for efficient agonist- induced receptor internalization.