Robberecht P, Gourlet P
Laboratoire de Chimie Biologique et de la Nutrition Faculté de Médecine, Université Libre de Bruxelles, Belgique.
J Pharm Belg. 1996 May-Jun;51(3):165-9.
VIP and PACAP are structurally related neuropeptides. They interact with multiple classes of receptors that have been cloned recently. These receptors may be divided into two main classes: the PACAP type I receptors with a high affinity for PACAP and a low affinity for VIP and the PACAP type II receptors (with a high affinity for PACAP and VIP). Five different forms of the PACAP type I receptors are described and result from an alternative splicing of the messenger. Two distinct forms (VIP1 and VIP2 receptors) of the PACAP type II receptors are described. Considering this high number of variants and the coexistence of several variants in the same cell, the development of cell lines expressing a single type of receptor was required for the testing of selective agonists and antagonists. However, limits in the interpretation of the results obtained in the cell lines expressing the recombinant receptors were obvious: discovery of unusual receptor states and unusual coupling of cellular effectors when a high number of receptors was expressed.
血管活性肠肽(VIP)和垂体腺苷酸环化酶激活肽(PACAP)是结构相关的神经肽。它们与最近克隆的多种受体相互作用。这些受体可分为两大类:对PACAP具有高亲和力而对VIP具有低亲和力的PACAP I型受体和(对PACAP和VIP均具有高亲和力的)PACAP II型受体。已描述了PACAP I型受体的五种不同形式,它们是由信使核糖核酸的可变剪接产生的。已描述了PACAP II型受体的两种不同形式(VIP1和VIP2受体)。考虑到变体数量众多且同一细胞中存在多种变体,为了测试选择性激动剂和拮抗剂,需要开发表达单一类型受体的细胞系。然而,在表达重组受体的细胞系中获得的结果的解释存在明显局限性:当表达大量受体时,会发现异常的受体状态和细胞效应器的异常偶联。