NDLI: Analytical determination of receptor-ligand dissociation constants of two populations of receptors from displacement curves.

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Analytical determination of receptor-ligand dissociation constants of two populations of receptors from displacement curves.

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Analytical determination of receptor-ligand dissociation constants of two populations of receptors from displacement curves.

Content Provider	World Health Organization (WHO)-Global Index Medicus
Author	Almagor, H. Levitzki, A.
Description	Author Affiliation: Almagor H ( Fritz Haber Research Center for Molecular Dynamics, Hebrew University of Jerusalem, Israel.);
Abstract	The determination of receptor-ligand dissociation constants from displacement data has been restricted until recently to the condition of receptor saturation, in which the concentration of receptor is negligible as compared to the displaced ligand and the displacing ligand used. This restriction has lately been removed since an accurate method has been developed for the determination of the dissociation constants for all experimental conditions for a system that includes a single type of binding site. In many cases, however, there are two types of receptor binding sites that exhibit different affinities toward the ligand. The present study provides an analytic solution for the problem of determination of the two dissociation constants as well as the proportion of the two receptor types. The formal derivation of the equations is described, along with analysis of a displacement simulation. The sensitivity of the method to the ratio between the two dissociation constants is also investigated. The application of the method is demonstrated for the analysis of the binding of beta-adrenergic receptors to the agonist isoproterenol as monitored by the displacement of the beta-antagonist 125I-labeled cyanopindolol.
ISSN	00278424
e-ISSN	10916490
Journal	Proceedings of the National Academy of Sciences of the United States of America
Issue Number	17
Volume Number	87
Language	English
Publisher	National Academy of Sciences
Publisher Date	1990-10-01
Publisher Place	United States
Access Restriction	Open
Subject Keyword	Ligands Models, Theoretical Receptors, Cell Surface Metabolism Animals Binding, Competitive Cell Line Erythrocyte Membrane Iodocyanopindolol Isoproterenol Pharmacology Kinetics Mathematics Pindolol Analogs & Derivatives Receptors, Adrenergic, Beta Drug Effects Turkeys Research Support, Non-U.S. Gov't Research Support, U.S. Gov't, P.H.S. Multidisciplinary
Content Type	Text
Resource Type	Article
Subject	Multidisciplinary

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