The role of kinetic context in apparent biased agonism at GPCRs

Biased agonists act at a receptor to preferentially induce distinct intracellular signalling responses over others. Here the authors show how kinetics of ligand binding and signaling responses greatly influence observed bias profiles, and hence must be considered when studying biased agonists.

Guardado en:

Detalles Bibliográficos
Autores principales:	Carmen Klein Herenbrink, David A. Sykes, Prashant Donthamsetti, Meritxell Canals, Thomas Coudrat, Jeremy Shonberg, Peter J. Scammells, Ben Capuano, Patrick M. Sexton, Steven J. Charlton, Jonathan A. Javitch, Arthur Christopoulos, J. Robert Lane
Formato:	article
Lenguaje:	EN
Publicado:	Nature Portfolio 2016
Materias:	Science Q
Acceso en línea:	https://doaj.org/article/0783ff6940594b04b8cd38d7c0762fb1
Etiquetas:	Agregar Etiqueta Sin Etiquetas, Sea el primero en etiquetar este registro!

id	oai:doaj.org-article:0783ff6940594b04b8cd38d7c0762fb1
record_format	dspace
spelling	oai:doaj.org-article:0783ff6940594b04b8cd38d7c0762fb12021-12-02T16:50:13ZThe role of kinetic context in apparent biased agonism at GPCRs10.1038/ncomms108422041-1723https://doaj.org/article/0783ff6940594b04b8cd38d7c0762fb12016-02-01T00:00:00Zhttps://doi.org/10.1038/ncomms10842https://doaj.org/toc/2041-1723Biased agonists act at a receptor to preferentially induce distinct intracellular signalling responses over others. Here the authors show how kinetics of ligand binding and signaling responses greatly influence observed bias profiles, and hence must be considered when studying biased agonists.Carmen Klein HerenbrinkDavid A. SykesPrashant DonthamsettiMeritxell CanalsThomas CoudratJeremy ShonbergPeter J. ScammellsBen CapuanoPatrick M. SextonSteven J. CharltonJonathan A. JavitchArthur ChristopoulosJ. Robert LaneNature PortfolioarticleScienceQENNature Communications, Vol 7, Iss 1, Pp 1-14 (2016)
institution	DOAJ
collection	DOAJ
language	EN
topic	Science Q
spellingShingle	Science Q Carmen Klein Herenbrink David A. Sykes Prashant Donthamsetti Meritxell Canals Thomas Coudrat Jeremy Shonberg Peter J. Scammells Ben Capuano Patrick M. Sexton Steven J. Charlton Jonathan A. Javitch Arthur Christopoulos J. Robert Lane The role of kinetic context in apparent biased agonism at GPCRs
description	Biased agonists act at a receptor to preferentially induce distinct intracellular signalling responses over others. Here the authors show how kinetics of ligand binding and signaling responses greatly influence observed bias profiles, and hence must be considered when studying biased agonists.
format	article
author	Carmen Klein Herenbrink David A. Sykes Prashant Donthamsetti Meritxell Canals Thomas Coudrat Jeremy Shonberg Peter J. Scammells Ben Capuano Patrick M. Sexton Steven J. Charlton Jonathan A. Javitch Arthur Christopoulos J. Robert Lane
author_facet	Carmen Klein Herenbrink David A. Sykes Prashant Donthamsetti Meritxell Canals Thomas Coudrat Jeremy Shonberg Peter J. Scammells Ben Capuano Patrick M. Sexton Steven J. Charlton Jonathan A. Javitch Arthur Christopoulos J. Robert Lane
author_sort	Carmen Klein Herenbrink
title	The role of kinetic context in apparent biased agonism at GPCRs
title_short	The role of kinetic context in apparent biased agonism at GPCRs
title_full	The role of kinetic context in apparent biased agonism at GPCRs
title_fullStr	The role of kinetic context in apparent biased agonism at GPCRs
title_full_unstemmed	The role of kinetic context in apparent biased agonism at GPCRs
title_sort	role of kinetic context in apparent biased agonism at gpcrs
publisher	Nature Portfolio
publishDate	2016
url	https://doaj.org/article/0783ff6940594b04b8cd38d7c0762fb1
work_keys_str_mv	AT carmenkleinherenbrink theroleofkineticcontextinapparentbiasedagonismatgpcrs AT davidasykes theroleofkineticcontextinapparentbiasedagonismatgpcrs AT prashantdonthamsetti theroleofkineticcontextinapparentbiasedagonismatgpcrs AT meritxellcanals theroleofkineticcontextinapparentbiasedagonismatgpcrs AT thomascoudrat theroleofkineticcontextinapparentbiasedagonismatgpcrs AT jeremyshonberg theroleofkineticcontextinapparentbiasedagonismatgpcrs AT peterjscammells theroleofkineticcontextinapparentbiasedagonismatgpcrs AT bencapuano theroleofkineticcontextinapparentbiasedagonismatgpcrs AT patrickmsexton theroleofkineticcontextinapparentbiasedagonismatgpcrs AT stevenjcharlton theroleofkineticcontextinapparentbiasedagonismatgpcrs AT jonathanajavitch theroleofkineticcontextinapparentbiasedagonismatgpcrs AT arthurchristopoulos theroleofkineticcontextinapparentbiasedagonismatgpcrs AT jrobertlane theroleofkineticcontextinapparentbiasedagonismatgpcrs AT carmenkleinherenbrink roleofkineticcontextinapparentbiasedagonismatgpcrs AT davidasykes roleofkineticcontextinapparentbiasedagonismatgpcrs AT prashantdonthamsetti roleofkineticcontextinapparentbiasedagonismatgpcrs AT meritxellcanals roleofkineticcontextinapparentbiasedagonismatgpcrs AT thomascoudrat roleofkineticcontextinapparentbiasedagonismatgpcrs AT jeremyshonberg roleofkineticcontextinapparentbiasedagonismatgpcrs AT peterjscammells roleofkineticcontextinapparentbiasedagonismatgpcrs AT bencapuano roleofkineticcontextinapparentbiasedagonismatgpcrs AT patrickmsexton roleofkineticcontextinapparentbiasedagonismatgpcrs AT stevenjcharlton roleofkineticcontextinapparentbiasedagonismatgpcrs AT jonathanajavitch roleofkineticcontextinapparentbiasedagonismatgpcrs AT arthurchristopoulos roleofkineticcontextinapparentbiasedagonismatgpcrs AT jrobertlane roleofkineticcontextinapparentbiasedagonismatgpcrs
_version_	1718383079082426368

The role of kinetic context in apparent biased agonism at GPCRs

Ejemplares similares