Chapter 9. Kinetics and Mechanisms of GPCR Activation

Autor:	Martin J. Lohse, Manuela Ambrosio
Rok vydání:	2011
Předmět:	Chemistry Kinetics Allosteric regulation Receptor Cell biology G protein-coupled receptor
DOI:	10.1039/9781849733441-00199
Popis:	The development of several fluorescent approaches has enabled the monitoring the kinetics of GPCR activation and signalling in real-time. Such fluorescent-based assays—first established for isolated reconstituted receptors and later developed to follow the activation of GPCRs in living cells—suggest that GPCR activation can occur faster than previously thought and that different agonists may induce distinct conformations with different speeds of GPCRs activation. Some of those approaches have allowed the detection of both the modulation triggered by allosteric ligands on the receptor conformation and the transconformational switches occurring between two protomers constituting a heterodimer in intact cells. This chapter describes and summarizes recent studies on the agonist-dependent switching behaviour of GPCRs.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::412f3834e8dd1bf52e48d4632db6979a https://doi.org/10.1039/9781849733441-00199 Zobrazit plný text záznamu