G protein-coupled receptors (GPCRs) are a class of receptor proteins widely present on the cell membrane in the human body, including many subtypes such as α, β, and γ. Their basic structure consists of a seven-transmembrane domain and a cytoplasmic C-terminus. GPCRs are located on the cell membrane and serve as key components in signal transduction, participating in various biological processes such as cell signaling, cell polarization, and metabolic regulation. Activation of GPCRs initiates multiple signaling pathways, such as the cAMP signaling pathway and calcium ion signaling pathway, regulating the levels of intracellular signaling molecules. GPCR genes are expressed in various tissues and cells, with their expression and activity regulated by various factors. Specific expression and mutations are associated with a variety of diseases, such as cancer, neurological disorders, and cardiovascular diseases.