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Heptahelical and Other G-Protein-Coupled Receptors (GPCRs) Signaling

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Abstract:

Heptahelical receptors are coupled to heterotrimeric GTP-binding proteins (G-proteins) which transduce most signals through their α and βγ subunits to effectors, enzymes and ion channels. Of the 367 heptahelical receptors for endogenous ligands, about 330 are potential targets for drug discovery with agonist, antagonist or inverse agonist properties. The term G-protein-coupled receptors (GPCRs) is a broader functional definition rather than a structural one referring to heptahelical receptors specifically. Non-heptahelical putative GPCRs include some transmembrane receptors with tyrosine-kinase activity on their cytosolic endings (EGF, insulin and IGF-1 receptors), other transmembrane receptors (mannose-6-phosphate/IGF-2 receptor and integrin-associated protein IAP or CD47), and some receptors belonging to the class of glycosylphosphatidylinositol (GPI)-anchored proteins and located on the outer face of the plasma membrane. Also, activators of G-protein signaling (AGS) proteins that regulate vesicular trafficking activate heterotrimeric G-proteins in the Golgi independently of receptor activation. Main effectors activated through their direct interactions with α subunits or βγ dimers of heterotrimeric G-proteins include adenylylcyclases, cGMPphosphodiesterase, phospholipases Cβ, phosphoinositide 3-kinase γ, CaV2 calcium channels, GIRK/Kir3 potassium channels, and guanine nucleotide exchange factors RasGEF and RhoGEF leading to small G-proteins and MAP-kinases activation. Current signaling cascades leading to final cell responses are depicted.

Keywords: GPCR; heptahelical receptor; signaling; transduction

Document Type: Research Article

DOI: http://dx.doi.org/10.2174/092986706775197953

Affiliations: Laboratoire de signalisation cellulaire ,CNRS UMR 7175-LC1, Faculte de Pharmacie, Universite - Strasbourg 1, BP24, 67401 Illkirch Cedex, France;

Publication date: January 1, 2006

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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