动物褪黑激素受体的分子表征和药理学研究

E. Cecon, J. Boutin, R. Jockers
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引用次数: 1

摘要

褪黑素是一种黑暗激素,在夜间分泌的量很小,在白天几乎检测不到。褪黑素主要作用于高亲和力的G蛋白偶联受体。本文将从褪黑激素受体的克隆、表达、纯化到近年来放射性和荧光示踪剂的发展历程进行综述。然后,我们将报告褪黑激素受体功能特性的最新进展,包括受体相关蛋白和受体异构体引起的配体偏倚和系统偏倚。目前可获得的针对褪黑激素受体的抗体将首次在这里进行严格审查。该综述将以发现变构配体和一系列褪黑激素受体相关信号复合物的体内验证来改善未来的药物开发为结束。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Molecular Characterization and Pharmacology of Melatonin Receptors in Animals
Melatonin, the hormone of darkness, is secreted in minute amounts during the night and is virtually undetectable during the day. Melatonin mainly acts on high-affinity G protein-coupled receptors. The present review will trace the path of the discovery of melatonin receptors from their cloning, expression and purification to the development of recent radioactive and fluorescent tracers. We will then report on the state-of-the-art of melatonin receptor functional properties, including ligand bias and system bias due to receptor-associated proteins and receptor heteromers. Currently available antibodies raised against melatonin receptors will be critically reviewed here for the first time. The review will close with future perspectives in terms of the discovery of allosteric ligands and the in vivo validation of a range of melatonin receptor-associated signaling complexes to improve future drug development.
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