期刊
AMERICAN JOURNAL OF PHYSIOLOGY-CELL PHYSIOLOGY
卷 323, 期 2, 页码 C640-C647出版社
AMER PHYSIOLOGICAL SOC
DOI: 10.1152/ajpcell.00445.2021
关键词
GPCR; pathophysiology; signaling
资金
- NIH [P01 HL147841, R01 HL139522]
- American Heart Association Predoctoral Fellowship [834906]
Adhesion GPCRs, as the second-largest family of GPCRs, have not yet been targeted for clinical treatment despite increasing evidence of their physiological and pathological functions. They are associated with a variety of diseases, including cancer, central nervous system disorders, immunity, and inflammation.
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 pathologi-cal 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.
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