Allosteric agonist modulators.
This article discusses a model to describe the effects of molecules that bind to a site on the receptor separate from that of the endogenous agonist to actively produce receptor signals (direct agonism). In addition, these molecules also modify the biological responses of the endogenous agonist (either potentiation or antagonism). The effects of such compounds in high-throughput screening assays are described as well as their effects on the dose-response curves to conventional agonists.
Kenakin
Terry
T
Biochemical Reagents and Assay Development, GlaxoSmithKline Research and Development, Research Triangle Park, North Carolina 27709, USA. Terry.P.Kenakin@gsk.com
D000494:Allosteric Regulation; D000495:Allosteric Site; D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004336:Drug Antagonism; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D006801:Humans; D007700:Kinetics; D008024:Ligands; D008956:Models, Chemical; D011956:Receptors, Cell Surface / Q000378:metabolism; D043562:Receptors, G-Protein-Coupled / Q000737:chemistry; D015398:Signal Transduction; D013678:Technology, Pharmaceutical / Q000379:methods
D008024:Ligands; D011956:Receptors, Cell Surface; D043562:Receptors, G-Protein-Coupled