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GPCR/G Protein

G Protein Coupled Receptors (GPCRs) perceive many extracellular signals and transduce them to heterotrimeric G proteins, which further transduce these signals intracellular to appropriate downstream effectors and thereby play an important role in various signaling pathways. G proteins are specialized proteins with the ability to bind the nucleotides guanosine triphosphate (GTP) and guanosine diphosphate (GDP). In unstimulated cells, the state of G alpha is defined by its interaction with GDP, G beta-gamma, and a GPCR. Upon receptor stimulation by a ligand, G alpha dissociates from the receptor and G beta-gamma, and GTP is exchanged for the bound GDP, which leads to G alpha activation. G alpha then goes on to activate other molecules in the cell. These effects include activating the MAPK and PI3K pathways, as well as inhibition of the Na+/H+ exchanger in the plasma membrane, and the lowering of intracellular Ca2+ levels.

Most human GPCRs can be grouped into five main families named; Glutamate, Rhodopsin, Adhesion, Frizzled/Taste2, and Secretin, forming the GRAFS classification system.

A series of studies showed that aberrant GPCR Signaling including those for GPCR-PCa, PSGR2, CaSR, GPR30, and GPR39 are associated with tumorigenesis or metastasis, thus interfering with these receptors and their downstream targets might provide an opportunity for the development of new strategies for cancer diagnosis, prevention and treatment. At present, modulators of GPCRs form a key area for the pharmaceutical industry, representing approximately 27% of all FDA-approved drugs.

GPCR/G Protein 相关靶点
Adenylate Cyclase Amylin Receptor Androgen Receptor Arrestin Bradykinin Receptor CRFR G Protein-coupled Receptor Kinase (GRK) G protein-coupled Bile Acid Receptor 1 GCGR GLP Receptor Glutaminase GPR88 GPR68 GPR52 GPR6 GPR4 GPR139 Macrophage migration inhibitory factor (MIF) MRGPR MCHR1 (GPR24) Mitophagy nAChR NEDD8-activating Enzyme P2Y Receptor Serotonin Transporter Succinate Receptor 1 TAAR Apelin Receptor (APJ) Bombesin Receptor Chemerin Receptor CGRP Receptor Taste Receptor PTHR ICMT Antiangiogenics OX Receptor RAS Opioid Receptor GPR40 Cannabinoid Receptor Adiponectin Receptor 5-HT Receptor Adrenergic Receptor Neurokinin Receptor P2Y受体 Endothelin Receptor Angiotensin Receptor mAChR GPR119 Leukotriene Receptor Prostaglandin Receptor CXCR 组胺受体 PDGFR LPL Receptor Adenosine Receptor mGluR LPA Receptor Adenosine Kinase EP1 Receptor GHSR NOP Receptor CaSR Adenosine Deaminase RGS Protein Calcimimetic Agent Vasopressin Receptor ERRγ Glucocorticoid Receptor GPR120 Free Fatty Acid Receptors CCR2 PGD2 Receptor EP4 Receptor GPR109A 17,20-lyase S1P receptor S1P receptor inhibitor GLUT1 NK3 Receptor Oxytocin Receptors Motilin Receptor Sigma Receptor GPR44 CysLT1 receptor Somatostatin Receptor Bombesin Receptors CCK1 Receptors GPCR19 FFAR1(GPR40) PAF Receptors Melatonin Receptors GPR84 Non-selective CRF Apelin Receptor GPR55 Galanin Receptors ETA Receptors NPY Receptors Urotensin-II Receptor CRF1 Receptors NK Receptor NK2 Receptors Protease-Activated Receptors Melanin-concentrating Hormone Receptors Orexin EBI2/GPR183 CCKB Melanocortin (MC) Receptors C3aR Hydroxycarboxylic Acid Receptors CysLT2 receptor Calcitonin and Related Receptors Neurotensin Receptors CCK2 Receptors Acetylcholine Ghrelin Receptors GPR81 Orphan 7-TM Receptors Chemokine Receptors TSH Receptor Peptide Receptors GPR35 Formyl Peptide Receptors GIP Receptor Adrenergic Transporters VIP Receptors ETB Receptors CRF2 Receptors Neuropeptide FF/AF Receptors Gonadotropin-Releasing Hormone Receptors Kisspeptin Receptor Secretin Receptors Neuromedin U Receptors PACAP Receptors Sensory Neuron-Specific Receptors P2X7 receptor