GPCR

G-protein coupled receptors (GPCRs) are a diverse super-family of proteins located within the plasma membrane of eukaryotic cells which have a common architecture consisting of seven-transmembrane (7-TM) segments, connected by extracellular (ECL) and intracellular (ICL) loops. They differ from other 7-TM proteins in their ability to activate guanine-nucleotide binding proteins or β-arrestin and so initiate a signaling cascade. Therefore, they are among the most important pharmaceutical drug targets[1],[2]. GPCRs are activated by a wide variety of stimulants, including light, odorant molecules, peptide and non-peptide neurotransmitters, hormones, growth factors and lipids, and control a wide variety of physiological processes including sensory transduction, cell–cell communication, neuronal transmission, and hormonal signaling[3]. Upon activation by a stimulant (binding or conformational change of ligand), the conformation of the receptor is altered, which can result into two principal signal transduction pathways involving the G protein-coupled receptors: the cAMP signal pathway and the phosphatidylinositol signal pathway[4].
Analysis of the human genome revealed at least 799 unique GPCRs. One widely adopted scheme classify the GPCRs into six families, with the most important and extensively studied being: family A (Rhodopsin-like); family B (Secretin); family C (Metabotropic glutamate/pheromone); family D (Fungal mating hormone); family E (Cyclic AMP); family F (Frizzled/Smoothened)[5].


[1] Modeling the 3D structure of GPCRs: advances and application to drug discovery. Becker O.M., Shacham S., Marantz Y., Noiman S. Current Opinion in Drug Discovery & Development 2003, 6(3):353-361.
[2] G protein coupled receptors – exploiting flexible conformations. K.L. Chapman, J..BC.Findlay, G.K. Kinsella. Eur. Pharm. Rev. 2012, 6
[3] Tools for GPCR drug discovery. R. Zhang, X. Xie. Acta Pharmacologica Sinica (2012) 33: 372–384
[4] G proteins: transducers of receptor-generated signals. Gilman A.G. Annu. Rev. Biochem. 1987, 56, 615–49
[5] P. Joost, A. Methner. Phylogenetic analysis of 277 human G-protein-coupled receptors as a tool for the prediction of orphan receptor ligands. Gen. Biol. 2002, 3, 0063.

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Axon ID Name Description From price
1575 5-HT6 antagonist 29 Selective brain penetrant 5-HT6 receptor antagonist €90.00
2155 A 841720 Non-competitive mGluR1 antagonist €85.00
1990 A 943931 H4 antagonist €75.00
1179 A1B1 hydrochloride CCR1 antagonist €125.00
1510 ABT 239 tartrate H3 antagonist/inverse agonist €135.00
1250 ABT 724 trihydrochloride D4 agonist €85.00
1579 ACR 16 hydrochloride Dopaminergic stabilizer that stabilizes psychomotor activity Inquire
1188 Adenosine amine congener Adenosine A1 agonist €125.00
1751 ADL 5859 Selective δ-opioid receptor agonist €115.00
1492 Agomelatine Melatonin agonist; 5-HT2C antagonist €75.00
1335 AH 001 Melatonin agonist €80.00
1336 AH 002 Melatonin agonist Inquire
2062 Alprostadil Prostaglandin EP (1-4) receptor antagonist €105.00
2367 AM 095 (parent compound) Novel potent and selective LPA1 antagonist €125.00
1218 AM 251 CB1 antagonist €95.00

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