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.
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- A8886 UNBS 5162Summary: A pan-antagonist of CXCL chemokines
- B4876 K-Ras(G12C) inhibitor 12Summary: allosteric inhibitor of K-Ras(G12C)
- C5822 p-iodo-Clonidine (hydrochloride)Summary: partial agonist of the α2-adrenergic receptor
- C5743 ONO-8130Summary: orally bioavailable antagonist of the prostaglandin E2 (PGE2) receptor EP
- C5824 GPR120 Compound ASummary: orally available, high-affinity agonist of GPR120
- C5802 CarazololSummary: high-affinity, lipophilic, non-selective ligand of the β-adrenergic receptors
- C5675 Fendiline (hydrochloride)Summary: α2-adrenergic receptor antagonist
- C5518 γ-Linolenic AcidSummary: weak LTB4 receptor antagonist
- C5416 REV 5901Summary: antagonist of cysteinyl-leukotriene receptors
- C5513 S-2 MethanandamideSummary: potent CB1 receptor agonist