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Principles: Receptor theory in pharmacology

2004; Elsevier BV; Volume: 25; Issue: 4 Linguagem: Inglês

10.1016/j.tips.2004.02.012

1873-3735

Terry Kenakin,

Cholesterol and Lipid Metabolism

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.