Allosteric receptor modulation in drug targeting by Norman G. Bowery

By Norman G. Bowery

Providing a wide range of illustrations and tables in each bankruptcy, this publication widely covers the rules of allosterism in connection with drug motion and progresses to a close exam of person ionotropic and G-protein coupled receptor systems-helping these new to the topic comprehend the significance of allosterism and supplying these already operating within the box with particular reference info. This name presents in-depth chapters on easy ideas of allosterism and its value at GABAA, 5HT3, nicotinic, and GABAB receptors, ionotropic and metabotropic receptors for glutamate, muscarinic receptors and alpha 2 adrenoceptors to supply an organization origin to the topic.

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Beyond receptor expression: the influence of receptor conformation, density, and affinity in HIV-1 infection. Virology 1997; 235: 179–190. 9. Lee B, Sharron M, Blanpain C, et al. Epitope mapping of CCR5 reveals multiple conformational states and distinct but overlapping structures involved in chemokine and coreceptor function. J Biol Chem 1999; 274:9617–9626. 10. Picard L, Simmons G, Power CA, Meyer A, Wiess RA, Clapham PR. Multiple extracellular domains of CCR-5 contribute to human immunodeficiency virus type 1 entry and fusion.

Neuropharmacology 1999; 38:A30–A36. 64. Alberts GL, Chio CL, Im WB. Allosteric modulation of the human 5-HT7A receptor by lipidic amphipathic compounds. Mol Pharmacol 2001; 60:1349–1355. © 2006 by Taylor & Francis Group, LLC 18 Daniels 65. Fillion G, Rousselle JC, Massot O, Zifa E, Fillion MP, Prudhomme N. A new peptide, 5-HT-moduline, isolated and purified from mammalian brain specifically interacts with 5-HT1B/1D receptors. Behav Brain Res 1996; 73:313–317. 66. Massot O, Rousselle JC, Fillion MP, et al.

These sites may bind the same ligand (with identical or different affinities) or may bind different ligands. The interaction in the former case is termed homotropic cooperativity, while the latter is termed heterotropic cooperativity. As the subject of this book is allosterism in drug discovery, I will concentrate primarily on the mathematical models that describe heterotropic interactions; however, little modification is required to apply any of these models to homotropic interactions. Once we define allosteric interactions as occurring between spacially distinct sites, a further © 2006 by Taylor & Francis Group, LLC Predicting Dose–Response Curve Behavior 41 property of allosteric interactions follows.

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