A Pharmacology Primer by Terry Kenakin
Author:Terry Kenakin [Kenakin, Terry]
Language: eng
Format: azw3
ISBN: 9780128139585
Publisher: Elsevier Science
Published: 2018-10-25T16:00:00+00:00
Figure 8.25 Inhibition curves for the allosteric modulator for CCR5 receptors, aplaviroc in blocking the binding of the chemokine RANTES (blue curve) and the CCR5-mediated calcium transient response to RANTES (red curve). It can be seen that aplaviroc produces a differentially greater inhibition of efficacy (agonist response) than affinity (binding species). Equations next to the curve illustrate that different receptor species mediate the response production in each assay. Data redrawn from T.P. Kenakin, Collateral efficacy in drug discovery: taking advantage of the good (allosteric) nature of 7TM receptors. Trends Pharmacol. Sci. 28 (2007) 407–415.
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