By Bryan L. Roth (auth.), Kim A. Neve (eds.)
Functional selectivity refers back to the skill of alternative ligands performing at one receptor subtype to turn on a number of signaling pathways in distinctive combos; that's, one drug may be an agonist at pathway A and an antagonist or partial agonist at pathway B, and one other drug may have the opposite profile. sensible selectivity has profound implications for drug improvement, for chemical biology, and for the layout of experiments to represent receptor functionality. In useful Selectivity of G Protein-Coupled Receptors specialist neuroscientists and pharmacologists assessment the paintings that verified the lifestyles of useful selectivity, positioned it inside a theoretical framework, and supplied a mechanistic foundation for the phenomenon. This intriguing, accomplished, and future-oriented quantity comprises chapters that target theoretical and mechanistic points of sensible selectivity and that minimize throughout subfamilies of GPCRs. extra chapters specialise in subfamilies of therapeutically correct receptors the place there's enormous facts of ligand useful selectivity. available and authoritative, practical Selectivity of G Protein-Coupled Receptors is a useful academic software and reference resource for college students and scientists drawn to drug improvement, chemical biology, and GPCR functionality.
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Practical selectivity refers back to the skill of alternative ligands performing at one receptor subtype to turn on a number of signaling pathways in exact mixtures; that's, one drug will be an agonist at pathway A and an antagonist or partial agonist at pathway B, and one other drug may have the opposite profile.
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Additional resources for Functional Selectivity of G Protein-Coupled Receptor Ligands: New Opportunities for Drug Discovery
Though these artificial models allow to specifically focus on a single receptor subtype, this approach raises the question of whether such complex signaling reveals artifactual coupling or whether it is a genuine property of GPCRs. Indeed, the complexity in signaling was initially found to depend on the receptor expression level (26,105,125,126) suggesting that the measure of pharmacologic properties of drugs depends on the relative stoechiometry of receptors and other cellular components (127,128).
In addition, it is likely that the multiple couplings of a given receptor could involve common intracellular domains, limiting the interpretation of mutagenesis studies. Thus, deletion or substitution of these domains could severely impair the less efficient coupling, while the preferential coupling would appear partially affected (104,157). Yet, these trivial criticisms should not obscure convincing data highlighting the existence of distinct molecular determinants of a single receptor that ensure the coupling with multiple signaling cascades.
Neubig RR. Membrane organization in G-protein mechanisms. FASEB J 1994;8:939–46 6. Ostrom RS, Post SR, Insel PA. Stoichiometry and compartmentation in G protein-coupled receptor signaling: implications for therapeutic interventions involving G(s). J Pharmacol Exp Ther 2000;294:407–12 7. Ostrom RS, Insel PA. The evolving role of lipid rafts and caveolae in G protein-coupled receptor signaling: implications for molecular pharmacology. Br J Pharmacol 2004;143:235–45 8. Blank JL, Brattain KA, Exton JH.