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GPR137 family belonging to the seven-transmembrane G protein-coupled receptor superfamily The GPR137 family includes GPR137A, GPR137B, and GPR137C, which are all orphan G protein-coupled receptors (GPCRs). GPR137A, also called GPR137 or transmembrane 7 superfamily member 1-like 1 protein (TM7SF1L1), is expressed in the central nervous system (CNS), endocrine gland, thymus, and lung. It is associated with different cancers including gastric cancer, pancreatic cancer, colon cancer, and malignant glioma. GPR137B, also called transmembrane 7 superfamily member 1 (TM7SF1), is a lysosome integral membrane protein that is strongly expressed in the heart, liver, kidney, and brain. It is associated with M2 macrophage polarization, and has been shown to perform a regulatory function in controlling dynamic Rag and mTORC1 localization and activity, as well as lysosome morphology. GPR137C, also called transmembrane 7 superfamily member 1-like 2 protein (TM7SF1L2), may be a key player in the prognosis of small cell lung cancer. GPCRs transmit physiological signals from the outside of the cell to the inside via G proteins. All GPCRs share a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. |
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