Superagonism at G protein-coupled receptors and beyond
R Schrage, A De Min, K Hochheiser, E Kostenis, K Mohr
British Journal of Pharmacology | WILEY | Published : 2016
Ligands targeting GPCRs can be categorized according to their intrinsic efficacy to trigger a specific, receptor-mediated response. A ligand endowed with the same level of efficacy as the endogenous agonist can be classified as a full agonist, whereas a compound that displays greater efficacy, that is, higher receptor signalling output than the endogenous agonist, can be called a superagonist. Subsequent to GPCR activation, an intracellular signalling cascade is set in motion, which may generate substantial amplification of the signal. This may obscure superagonism in pharmacological assays and, therefore, the definition of superagonism necessitates a combination of operational approaches, r..View full abstract
A. D. M. was supported by the research training group 1873, Deutsche Forschungsgemeinschaft (DFG).