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Principles: receptor theory in pharmacology
1Assay Development Compound Profiling, GlaxoSmithKline Research and Development, 5 Moore Drive, Research Triangle Park, NC 27709, USA. Terry.P.Kenakin@gsk.com
Trends in Pharmacological Sciences
|April 6, 2004
Summary
Pharmacological receptor theory has advanced significantly, with new models enhancing our understanding of G-protein-coupled receptor (GPCR) behavior. These discoveries offer novel avenues for therapeutic drug discovery.
Area of Science:
- Pharmacology
- Biochemistry
- Drug Discovery
Background:
- Pharmacological receptor theory has evolved over the past 25 years.
- Traditional models are being updated with more sophisticated approaches.
Purpose of the Study:
- To review advances in pharmacological receptor theory.
- To highlight new understandings of G-protein-coupled receptor (GPCR) behavior.
- To explore the potential for new drug discovery.
Main Methods:
- Discussion of operational models for drug-receptor interactions.
- Quantitative simulation of GPCR behavior using the extended ternary complex model.
- Characterization of novel GPCR behaviors.
Main Results:
- The operational model has become standard for analyzing drug-receptor interactions.
- The extended ternary complex model is routinely used for GPCR simulation.
- Six new GPCR behaviors identified, including spontaneous active states and allosteric mechanisms.
Conclusions:
- Recent advances in receptor theory provide a deeper understanding of GPCRs.
- Characterized GPCR behaviors present opportunities for developing new therapeutics.
- The study underscores the potential for significant therapeutic benefits through targeted drug discovery.