Adrenoceptors: Receptors, Ligands and Their Clinical Uses, Molecular Pharmacology and Assays.

Autor: Baker JG; Cell Signalling, Medical School, Queen's Medical Centre, University of Nottingham, Nottingham, UK. jillian.baker@nottingham.ac.uk.; Department of Respiratory Medicine, Nottingham University Hospitals NHS Trust, Nottingham, UK. jillian.baker@nottingham.ac.uk., Summers RJ; Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC, Australia. roger.summers@monash.edu.
Jazyk: angličtina
Zdroj: Handbook of experimental pharmacology [Handb Exp Pharmacol] 2024; Vol. 285, pp. 55-145.
DOI: 10.1007/164_2024_713
Abstrakt: The nine G protein-coupled adrenoceptor subtypes are where the endogenous catecholamines adrenaline and noradrenaline interact with cells. Since they are important therapeutic targets, over a century of effort has been put into developing drugs that modify their activity. This chapter provides an outline of how we have arrived at current knowledge of the receptors, their physiological roles and the methods used to develop ligands. Initial studies in vivo and in vitro with isolated organs and tissues progressed to cell-based techniques and the use of cloned adrenoceptor subtypes together with high-throughput assays that allow close examination of receptors and their signalling pathways. The crystal structures of many of the adrenoceptor subtypes have now been determined opening up new possibilities for drug development.
(© 2024. The Author(s), under exclusive license to Springer Nature Switzerland AG.)
Databáze: MEDLINE