Tumor Targeting Group, Department of Hepatology and Gastroenterology, Charité-Universitätsmedizin Berlin, Corporate Member of Freie Universität Berlin and Humboldt-Universität zu Berlin, 13353 Berlin, Germany.
Institute of Chemistry and Biochemistry, Freie Universität Berlin, 14195 Berlin, Germany.
Int J Mol Sci. 2023 Oct 12;24(20):15117. doi: 10.3390/ijms242015117.
G protein-coupled receptor 83 (GPR83) is a class A G protein-coupled receptor with predominant expression in the cerebellum and proposed function in the regulation of food intake and in anxiety-like behavior. The neuropeptide PEN has been suggested as a specific GPR83 ligand. However, conflicting reports exist about whether PEN is indeed able to bind and activate GPR83. This study was initiated to evaluate PEN as a potential ligand of GPR83. Employing several second messenger and other GPCR activation assays as well as a radioligand binding assay, and using multiple GPR83 plasmids and PEN peptides from different sources, no experimental evidence was found to support a role of PEN as a GPR83 ligand.
G 蛋白偶联受体 83（GPR83）是 A 类 G 蛋白偶联受体，在小脑中有较高表达，被认为在调节摄食和焦虑样行为方面具有作用。神经肽 PEN 被认为是 GPR83 的特异性配体。然而，关于 PEN 是否确实能够结合和激活 GPR83 存在相互矛盾的报道。本研究旨在评估 PEN 是否可能作为 GPR83 的配体。通过使用几种第二信使和其他 GPCR 激活测定法以及放射性配体结合测定法，以及使用来自不同来源的多个 GPR83 质粒和 PEN 肽，没有实验证据支持 PEN 作为 GPR83 配体的作用。
