VIP和PACAP的VPAC受体。

Receptors & channels Pub Date : 2002-01-01
M Laburthe, A Couvineau, J C Marie
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引用次数: 0

摘要

VIP和PACAP是两个重要的神经肽,它们有两个共同的G蛋白偶联受体VPAC1和VPAC2,而PACAP有一个额外的特异性受体PAC1。本文综述了目前关于VPAC受体的各个方面的知识,包括:1)受体对天然vip相关肽的特异性和合成激动剂或拮抗剂的药理学;2)基因组组织与染色体定位;3)与G蛋白或辅助蛋白(如RAMPs或含pdz的蛋白)的信号传导和已建立或推测的相互作用;4)通过位点定向诱变、受体嵌合体构建和结构建模确定配体-受体相互作用的分子基础;5)组成型活性受体突变体;6)短期(脱敏、内化、磷酸化)和长期(转录)调控及转基因模型;7)受体多态性。
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VPAC receptors for VIP and PACAP.

VIP and PACAP are two prominent neuropeptides that share two common G protein-coupled receptors, VPAC1 and VPAC2, while PACAP has an additional specific receptor, PAC1. This article reviews the present knowledge regarding various aspects of VPAC receptors including: 1) receptor specificity toward natural VIP-related peptides and pharmacology of synthetic agonists or antagonists; 2) genomic organization and chromosomal localization; 3) signaling and established or putative interactions with G proteins or accessory proteins such as RAMPs or PDZ-containing proteins; 4) molecular basis of ligand-receptor interaction as determined by site-directed mutagenesis, construction of receptor chimeras, and structural modeling; 5) constitutively active receptor mutants; 6) short-term (desensitization, internalization, phosphorylation) and long-term (transcription) regulations and transgenic models; 7) receptor polymorphisms.

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