Abstract: The G protein-coupled receptor (GPCR) family is the largest and most diverse family of membrane proteins in eukaryotes. It has seven α-helix transmembrane domains and a wide range of biological functions. In recent years, more and more studies have shown that the disorders of GPCRs are related to cancer, which may be involved in the development and progression of tumors as proto-oncogenes or tumor suppressor genes, and GPCR has a diverse signaling mechanism. This paper briefly summarizes the diverse signaling mechanism of GPCRs, and recent research progress of a number of GPCRs in the development and progression of tumor.