Research Progress in Nuclear Translocation of G Protein-Coupled Receptors

GPCR (G-protein coupled receptor) are superfamilies of cell surface receptors that regulate a variety of cellular functions by responding to corresponding ligands. GPCRs signaling was long believed to involve activation of receptor exclusively at the cell surface, followed by its binding to heterotrimeric G-proteins and arrestins to trigger various intracellular signaling cascades, and termination of signaling by internalization or other ways of the receptor. From the end of the twentieth century to the present, about 30 kinds of GPCRs have been detected in the nucleus (upper or inner). Studies have shown that GPCR located in the nucleus (upper or inner) plays a different biological function from GPCR located on the cell membrane, and GPCR-mediated signal transduction pathway in the nucleus (upper or inner) is different from the traditional G protein and downstream second messengerdependent signal transduction pathway, but closely related to some transcription factors. GPCRs are important drug targets, so understanding the physiological function and pathological significance of nuclear (upper or inner) GPCR and analyzing the transport mechanism of GPCR nuclear translocation to help to develop drug strategies that successfully target them. Here, we will review the induction conditions of GPCR nuclear translocation, the mechanism of GPCR nuclear translocation, and the latest research results of signal transduction pathway mediated by GPCR nuclear translocation, which will provide reference for the research of new targeted nuclear GPCR drugs.

CSTR: 32200.14.cjcb.2019.12.0018