Structural and functional characterization of the endogenous agonist for orphan receptor GPR3

作者：Geng Chen, Nico Staffen, Zhangsong Wu, Xinyu Xu, Jinheng Pan, Asuka Inoue, Tingyi Shi, Peter Gmeiner, Yang Du, Jun Xu · 发表于：Cell Research · 年份：2024 · DOI：10.1038/s41422-023-00919-8 · 被引用次数：23 · 研究领域：Receptor Mechanisms and Signaling、Neuropeptides and Animal Physiology、Neuroscience and Neuropharmacology Research

GPR3 is a class A orphan G protein-coupled receptor (GPCR) exhibiting broad expression across various brain regions including the hypothalamus, hippocampus, and cortex, as well as in peripheral tissues such as liver and ovary. 1 , 2 Previous studies have highlighted the critical roles of GPR3 in regulating a diversity of physiological functions, including neurite outgrowth/neuronal survival, neuropathic pain, and oocyte maturation. 2 Intriguingly, in vivo studies using Alzheimer’s disease (AD) mouse models provide evidence showing that GPR3 can regulate the activity of γ-secretase and mediate the amyloidogenic proteolysis of the amyloid precursor protein (APP). 3 This finding positions GPR3 as a potential therapeutic target for the treatment of AD.