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The relevance of adhesion G protein-coupled receptors in metabolic functions
Biological Chemistry ( IF 3.7 ) Pub Date : 2021-07-04 , DOI: 10.1515/hsz-2021-0146
Isabell Kaczmarek 1 , Tomáš Suchý 1 , Simone Prömel 1, 2 , Torsten Schöneberg 1 , Ines Liebscher 1 , Doreen Thor 1
Affiliation  

G protein-coupled receptors (GPCRs) modulate a variety of physiological functions and have been proven to be outstanding drug targets. However, approximately one-third of all non-olfactory GPCRs are still orphans in respect to their signal transduction and physiological functions. Receptors of the class of Adhesion GPCRs (aGPCRs) are among these orphan receptors. They are characterized by unique features in their structure and tissue-specific expression, which yields them interesting candidates for deorphanization and testing as potential therapeutic targets. Capable of G-protein coupling and non-G protein-mediated function, aGPCRs may extend our repertoire of influencing physiological function. Besides their described significance in the immune and central nervous systems, growing evidence indicates a high importance of these receptors in metabolic tissue. RNAseq analyses revealed high expression of several aGPCRs in pancreatic islets, adipose tissue, liver, and intestine but also in neurons governing food intake. In this review, we focus on aGPCRs and their function in regulating metabolic pathways. Based on current knowledge, this receptor class represents high potential for future pharmacological approaches addressing obesity and other metabolic diseases.

中文翻译:

粘附 G 蛋白偶联受体在代谢功能中的相关性

G 蛋白偶联受体 (GPCR) 调节多种生理功能,并已被证明是出色的药物靶点。然而,就其信号转导和生理功能而言,大约三分之一的非嗅觉 GPCR 仍然是孤儿。粘附 GPCR (aGPCR) 类的受体属于这些孤儿受体。它们的特征在于其结构和组织特异性表达的独特特征,这使它们成为有趣的候选者,可用于去孤儿化和作为潜在治疗靶点的测试。能够 G 蛋白偶联和非 G 蛋白介导的功能,aGPCR 可以扩展我们影响生理功能的全部内容。除了它们在免疫和中枢神经系统中的描述意义外,越来越多的证据表明这些受体在代谢组织中的重要性很高。RNAseq 分析揭示了几种 aGPCR 在胰岛、脂肪组织、肝脏和肠道以及控制食物摄入的神经元中的高表达。在这篇综述中,我们关注 aGPCR 及其在调节代谢途径中的功能。根据目前的知识,这种受体类别代表了未来解决肥胖和其他代谢疾病的药理学方法的巨大潜力。
更新日期:2021-07-04
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