Journal
TRENDS IN PHARMACOLOGICAL SCIENCES
Volume 25, Issue 4, Pages 186-192Publisher
ELSEVIER SCIENCE LONDON
DOI: 10.1016/j.tips.2004.02.012
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Pharmacological receptor theory is discussed with special reference to advances made during the past 25 years. Thus, the operational model has supplanted analysis of drug-receptor interaction in functional systems whereas the extended ternary complex model is used routinely to simulate quantitatively G-protein-coupled receptor (GPCR) behavior. Six new behaviors for GPCRs, centered on spontaneous production of receptor active states, ligand-selective receptor active states, oligomerization with other proteins (receptor and nonreceptor) and allosteric mechanisms, have been characterized and each holds the potential for new drug discovery for therapeutic benefit.
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