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Class II G protein-coupled receptors for VIP and PACAP: structure, models of activation and pharmacology.

机译:VIP和PACAP的II类G蛋白偶联受体:结构,激活模型和药理学。

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摘要

VIP and PACAP impact strongly on human pathophysiology. Their receptors are very promising targets for developing new drugs in the treatment of inflammatory and neurodegenerative diseases. This article reviews the present knowledge regarding VIP and PACAP receptors, i.e. VPAC1, VPAC2 and PAC1. This includes: (I) a critical review of instrumental peptide agonists and antagonists; (II) a survey of recent data regarding the structure of VPAC1 receptor and the docking of VIP in the receptor binding domain. Structural models for the VPAC2 and PAC1 receptor N-terminal ectodomains are also described; (III) A critical description of the two models of VPAC1 receptor activation in the general context of class II/family B G protein-coupled receptors.
机译:VIP和PACAP对人体病理生理有很大影响。它们的受体是开发用于治疗炎性和神经退行性疾病的新药的非常有希望的靶标。本文回顾了有关VIP和PACAP受体(即VPAC1,VPAC2和PAC1)的现有知识。这包括:(I)对工具性肽激动剂和拮抗剂的严格审查; (II)关于VPAC1受体的结构和VIP结合在受体结合域中的最新数据的调查。还描述了VPAC2和PAC1受体N端胞外域的结构模型; (III)在II类/家族B G蛋白偶联受体的一般情况下,对VPAC1受体激活的两种模型的关键描述。

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