褪黑激素受体的结构和功能。

R Jockers, L Petit, L Brydon, P de Coppet, A D Strosberg
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引用次数: 0

摘要

褪黑素受体属于G蛋白偶联受体超家族。它们调节大量的生理功能,包括调节昼夜节律和季节性繁殖。药理学证据表明表达两种类型的受体,称为Mel1和Mel2。迄今为止,仅克隆了Mel1受体,并将其分为三种亚型(Mel1A, Mel1B, Mel1C)。Mel1受体在大脑、视网膜和其他一些外周组织中表达。所有Mel1亚型表现出类似的药理学特征,包括抑制腺苷酸环化酶。非洲爪蟾Mel1受体的两个等位基因异构体的克隆和表达揭示了另一种信号通路,即通过可溶性胍基环化酶途径抑制cGMP水平。这两种异构体与cAMP和cGMP途径的耦合不同,表明褪黑激素受体之间存在功能差异。未来的研究方向将包括Mel2受体的克隆、受体调控和褪黑激素受体在外周组织中的功能阐明。
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[Structure and function of melatonin receptors].

Melatonin receptors belong to the super-family of G protein-coupled receptors. They modulate a large spectrum of physiological functions including regulation of circadian rhythms and seasonal reproduction. Pharmacological evidence suggests the expression of two types of receptors, called Mel1 and Mel2. So far, only Mel1 receptors have been cloned and classified into three subtypes (Mel1A, Mel1B, Mel1C). Mel1 receptors are expressed in the brain, the retina and several other peripheral tissues. All Mel1 subtypes show comparable pharmacological profiles including inhibition of adenylyl cyclase. Cloning and expression of two allelic isoforms of the Mel1 receptor from Xenopus laevis has revealed another signalling pathway, inhibition of cGMP levels via the soluble guanylyl cyclase pathway. The two isoforms are differentially coupled to the cAMP and cGMP pathways indicating the existence of functional differences between melatonin receptors. Future research topics will include cloning of the Mel2 receptor, receptor regulation and the elucidation of melatonin receptor's function in peripheral tissues.

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