Abstract: G protein-coupled receptor kinases 2 (GRK2), which belongs to the serine/threonine protein kinase family, is widely distributed in a variety of tissues.With its specificity, it can enable activated G protein-coupled receptors (GPCRs) to be phosphorylated and desensitized, thus terminating the signal transduction pathways mediated by GPCRs.GRK2 can modulate GPCRs and non-GPCRs, but its own activity and expression may also be subject to the regulation of a number of factors. GRK2 has a variety of physiological and pathological effects, and many signaling pathways involved are closely related to the occurrence and development of malignant tumors.

Key words: G protein coupled receptors, G protein coupled receptor kinase 2, activity regulation, expression regulation, malignant tumor