Reevaluating equilibrium and kinetic binding parameters for lipophilic drugs based on a structural model for drug interaction with biological membranes

Structure-function activity relationships of drugs that bind to certain membrane-associated receptors must take into account the local membrane bilayer environment where the binding event occurs. In this Perspective, we have reexamined a model used in the equilibrium dissociation constant determinat...

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Bibliographic Details
Published in:Journal of medicinal chemistry 1991-03, Vol.34 (3), p.869-877
Main Authors: MASON, R. P, RHODES, D. G, HERBETTE, L. G
Format: Article
Language:English
Subjects:
Biological and medical sciences
Cell Membrane - metabolism
Chemical Phenomena
Chemistry, Physical
General pharmacology
Kinetics
lipid bilayers
Lipid Bilayers - metabolism
Medical sciences
Membrane Lipids - metabolism
Models, Molecular
Molecular Structure
Pharmaceutical Preparations - chemistry
Pharmaceutical Preparations - metabolism
Pharmacology. Drug treatments
Physicochemical properties. Structure-activity relationships
reviews
Structure-Activity Relationship
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Summary:Structure-function activity relationships of drugs that bind to certain membrane-associated receptors must take into account the local membrane bilayer environment where the binding event occurs. In this Perspective, we have reexamined a model used in the equilibrium dissociation constant determination for certain lipid-soluble drugs based on recent experimental data describing the interaction of these drugs with the membrane bilayer.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm00107a001