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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1064 Prop-2-ynyl-2-aminotetraline hydrochloride Dopamine agonist Inquire
1107 (+)-MDL 105725 5-HT2A antagonist €95.00
1073 (+)-PD 128907 hydrochloride D3 agonist €110.00
1071 (+)-PHNO hydrochloride D2 agonist €110.00
1108 (-)-MDL 105725 5-HT2A antagonist Inquire
1092 (-)-NPPCC 5-HT1A agonist Inquire
1074 (-)-PD 128907 hydrochloride D3 agonist €135.00
1359 (-)-WAY 100135 dihydrochloride 5-HT1A antagonist €95.00
1049 (R)-(+)-5-methoxy-2-aminotetraline hydrochloride Dopamine agonist Inquire
1013 (R)-(+)-7-Hydroxy-DPAT hydrobromide D3 agonist Inquire
1016 (R)-(+)-8-Hydroxy-DPAT hydrobromide 5-HT1A agonist €105.00
1058 (R)-(+)-8-Methoxy-2-aminotetraline hydrochloride Building Block; 5-HT1A agonist Inquire
1714 (R)-(+)-SLV 319 Inactive enantiomer of SLV 319 €95.00
1095 (R)-(-)-LY 426965 dihydrochloride 5-HT1A antagonist €115.00
1007 (R)-5-Hydroxy-DPAT hydrobromide D2 antagonist €145.00

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