Center for Translational Medicine, Lewis Katz School of Medicine, Temple University, Philadelphia, Pennsylvania.
Am J Physiol Cell Physiol. 2022 Aug 1;323(2):C640-C647. doi: 10.1152/ajpcell.00445.2021. Epub 2022 Jul 18.
G protein-coupled receptors (GPCRs) represent one of the most targeted drug classes in the human genome, accounting for greater than 40% of all Food and Drug Administration-approved drugs. However, the second-largest family of GPCRs, known as adhesion GPCRs (aGPCR), have yet to serve as a clinical target despite increasing evidence of their physiological and pathological functions, which suggests an opportunity toward the development of novel therapeutics. To date, the pathophysiological function of aGPCRs is associated with a plethora of diseases including cancer, central nervous system disorders, immunity and inflammation, and others. To highlight their potential as pharmacological targets, we will review three distinct aGPCR members (ADGRG1, ADGRE5, and ADGRF5), highlighting their molecular mechanisms of action and contributions to the development of pathophysiology.
G 蛋白偶联受体（GPCRs）是人类基因组中靶向药物治疗的最大靶点之一，占所有美国食品和药物管理局批准药物的 40%以上。然而，被称为黏附 GPCRs（aGPCR）的第二大 GPCR 家族，尽管有越来越多的生理和病理功能的证据，但尚未作为临床靶点，这表明有机会开发新的治疗方法。迄今为止，aGPCRs 的病理生理学功能与包括癌症、中枢神经系统疾病、免疫和炎症等在内的多种疾病有关。为了强调它们作为药物靶点的潜力，我们将回顾三个不同的 aGPCR 成员（ADGRG1、ADGRE5 和 ADGRF5），强调它们的作用机制及其对病理生理学发展的贡献。
