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Trends Pharmacol Sci. 2004 Apr;25(4):186-92.

Principles: receptor theory in pharmacology.

Author information

1
Assay Development Compound Profiling, GlaxoSmithKline Research and Development, 5 Moore Drive, Research Triangle Park, NC 27709, USA. Terry.P.Kenakin@gsk.com

Abstract

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 non-receptor) and allosteric mechanisms, have been characterized and each holds the potential for new drug discovery for therapeutic benefit.

PMID:
15063082
DOI:
10.1016/j.tips.2004.02.012
[Indexed for MEDLINE]

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