GPCR/G protein

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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B4876 K-Ras(G12C) inhibitor 12Summary: allosteric inhibitor of K-Ras(G12C) -
A8886 UNBS 5162Summary: A pan-antagonist of CXCL chemokines -
C5805 I-BOPSummary: TP specific agonist -
B1149 GSK962040Summary: Motilin receptor agonist -
A9025 Tecadenoson (CVT-510) -
A8975 CTOP TFA -
A8974 G-Protein antagonist peptide TFA -
C3828 1-(1-Naphthyl) piperazine (hydrochloride)Summary: ligand for 5-HT receptors -
C3123 FlibanserinSummary: full agonist of the serotonin 5-HT1A receptor and an antagonist of 5-HT2A. -
B8019 PimavanserinSummary: 5-HT2A inverse agonist
