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Binding kinetics of ligands acting at GPCRs

Sykes, David A.; Stoddart, Leigh A.; Kilpatrick, Laura E.; Hill, Stephen J.

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David A. Sykes

Leigh A. Stoddart

Professor of Molecular Pharmacology


The influence of drug-receptor binding kinetics has often been overlooked during the development of new therapeutics that target G protein-coupled receptors (GPCRs). Over the last decade there has been a growing understanding that an in-depth knowledge of binding kinetics at GPCRs is required to successfully target this class of proteins. Ligand binding to a GPCR is often not a simple single step process with ligand freely diffusing in solution. This review will discuss the experiments and equations that are commonly used to measure binding kinetics and how factors such as allosteric regulation, rebinding and ligand interaction with the plasma membrane may influence these measurements. We will then consider the molecular characteristics of a ligand and if these can be linked to association and dissociation rates.


Sykes, D. A., Stoddart, L. A., Kilpatrick, L. E., & Hill, S. J. (2019). Binding kinetics of ligands acting at GPCRs. Molecular and Cellular Endocrinology, 485, 9-19.

Journal Article Type Article
Acceptance Date Jan 19, 2019
Online Publication Date Feb 8, 2019
Publication Date Apr 5, 2019
Deposit Date Feb 25, 2019
Publicly Available Date Mar 1, 2019
Journal Molecular and Cellular Endocrinology
Print ISSN 0303-7207
Electronic ISSN 1872-8057
Publisher Elsevier
Peer Reviewed Peer Reviewed
Volume 485
Pages 9-19
Keywords GPCR; Binding kinetics; Association; Dissociation
Public URL
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