G-protein-coupled receptors (GPCRs) mediate a wide range of physiological responses to environmental stimulants, neurotransmitters, hormones cytokines and lipid signaling molecules. As a result, GPCRs play a significant role in biological processes such as vision, olfaction, the autonomic nervous system, and behavior.
All GPCRs share a common seven trans-membrane structure. GPCRs are associated with heterotrimeric G-proteins which are GTP-binding proteins made of alpha, beta, and gamma subunits. When a ligand binds to GPCR, it activates the attached G-protein, the GDP is replaced with GTP. The activated G-protein then dissociates into an alpha and a beta-gamma complex which activates downstream signaling pathways. These intracellular signaling pathways include cAMP/PKA, calcium/NFAT, phospholipase C, protein tyrosine kinases, MAP kinases, PI-3-kinase, nitric oxide/cGMP, Rho, and JAK/STAT.
GPCRs are one of the most important therapeutic targets for various diseases, over 30% of all modern medicinal drugs target this family. Aberrant GPCR functions are involved in pathological conditions such as neurological, immunological and hormonal disorders. A large number of GPCRs have been identified, but whose ligands are not known, are classified as orphan receptors.
Items 1-10 of 1139
- UNBS 5162Catalog No. :A8886A pan-antagonist of CXCL chemokinesUNBS5162 is a pan-antagonist of CXCL chemokines.
- K-Ras(G12C) inhibitor 12Catalog No. :B4876allosteric inhibitor of K-Ras(G12C)K-Ras(G12C) inhibitor 12 is an allosteric inhibitor of K-Ras(G12C) .
- p-iodo-Clonidine (hydrochloride)Catalog No. :C5822partial agonist of the α2-adrenergic receptor
- ONO-8130Catalog No. :C5743orally bioavailable antagonist of the prostaglandin E2 (PGE2) receptor EP
- GPR120 Compound ACatalog No. :C5824orally available, high-affinity agonist of GPR120
- CarazololCatalog No. :C5802high-affinity, lipophilic, non-selective ligand of the β-adrenergic receptors
- Fendiline (hydrochloride)Catalog No. :C5675α2-adrenergic receptor antagonist
- γ-Linolenic AcidCatalog No. :C5518weak LTB4 receptor antagonist
- REV 5901Catalog No. :C5416antagonist of cysteinyl-leukotriene receptors
- S-2 MethanandamideCatalog No. :C5513potent CB1 receptor agonist