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Download e-book for kindle: Allosteric receptor modulation in drug targeting by Norman G. Bowery

By Norman G. Bowery

ISBN-10: 0824727916

ISBN-13: 9780824727918

Delivering a wide range of illustrations and tables in each bankruptcy, this booklet widely covers the foundations 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 identify offers in-depth chapters on uncomplicated ideas of allosterism and its importance at GABAA, 5HT3, nicotinic, and GABAB receptors, ionotropic and metabotropic receptors for glutamate, muscarinic receptors and alpha 2 adrenoceptors to supply a company starting place to the topic.

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Extra info for Allosteric receptor modulation in drug targeting

Sample text

The first general property of allosterism can be used in some circumstances to detect and elucidate the allosteric nature of the receptor interaction. 1 on a saturation binding curve and/or an agonist dose–response curve. 1) Fract. Max. Resp. 0 –3 –2 –1 0 1 2 3 4 3 4 (B) Simple Competitive Fract. Max. Resp. 0 –3 –2 –1 0 1 Log ([A]/KA) 2 Figure 3 Effects of (A) an allosteric antagonist and (B) simple competitive (orthosteric) antagonist on dose–response curves to a receptor probe (either agonist or radioligand).

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Modelling and mutational analysis of a putative sodium-binding pocket on the dopamine D2 receptor. Molecular Pharmacology 2001; 60:373–381. 54. Schetz JA, Sibley DR. Zinc allosterically modulates antagonist binding to cloned D1 and D2 dopamine receptors. J Neurochem 1997; 68:1990–1997. 55. Rosenkilde MM, Lubicello M, Holst B, Schwartz TW. Natural agonist enhancing bis-His zinc-site in transmembrane segment V of the tachykinin NK3 receptor. FEBS Lett 1998; 439:35–40. 56. Schetz JA, Chu A, Sibley DR.

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Allosteric receptor modulation in drug targeting by Norman G. Bowery


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