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.
- B5360 Galanin (porcine)Summary: Endogenous porcine galanin receptor agonist
- B5361 Neuropeptide W-23 (human)Summary: Endogenous peptide agonist of Neuropeptide B/Neuropeptide W receptors NPBW1 and NPBW2
- B5362 α-CGRP (human)Summary: Endogenous calcitonin gene-related peptide receptor (CGRP) agonist
- B5363 [Nle4,D-Phe7]-α-MSHSummary: agonist at melanocortin receptors
- B5364 HOE 140Summary: Potent and selective bradykinin B2 receptor antagonist
- B5367 Cortistatin-8Summary: ghrelin receptor antagonist
- B5369 [D-p-Cl-Phe6,Leu17]-VIPSummary: Selective vasoactive intestinal peptide (VIP) receptor antagonist
- B5382 d[Cha4]-AVPSummary: human vasopressin V1B receptor agonist
- B5383 d[Leu4,Lys8]-VPSummary: Selective vasopressin V1B receptor agonist
- B5388 [Orn5]-URPSummary: Urotensin-II (UT) receptor pure antagonist