Principles: receptor theory in pharmacology. [Trends Pharmacol Sci. 2004]

SearchDatabase nameforSearch term

Advanced Search (beta)

Your browser version may not work well with NCBI's Web applications. More information here...

Display Show

All: 1

Review: 1

Click to change filter selection through MyNCBI.

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

Principles: receptor theory in pharmacology.

Kenakin T.

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

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 [PubMed - indexed for MEDLINE]

Emerging concepts of guanine nucleotide-binding protein-coupled receptor (GPCR) function and implications for high throughput screening. [Assay Drug Dev Technol. 2007]
The origins of diversity and specificity in g protein-coupled receptor signaling. [J Pharmacol Exp Ther. 2005]
Homo- and hetero-oligomerization of G protein-coupled receptors. [Life Sci. 2003]
G protein-coupled receptor signaling complexity in neuronal tissue: implications for novel therapeutics. [Curr Alzheimer Res. 2007]
G-protein-coupled receptor heterodimerization: assay technologies to clinical significance. [Curr Opin Drug Discov Devel. 2007]
» See all Related Articles...

Display Show

Principles: receptor theory in pharmacology.

Related Articles