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Binding kinetics of ligands acting at GPCRs.

Abstract：

: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.

journal_name

Mol Cell Endocrinol

journal_title

Molecular and cellular endocrinology

authors

Sykes DA,Stoddart LA,Kilpatrick LE,Hill SJ

doi

10.1016/j.mce.2019.01.018

subject

Has Abstract

pub_date

2019-04-05 00:00:00

pages

9-19

eissn

0303-7207

issn

1872-8057

pii

S0303-7207(19)30024-3

journal_volume

485

pub_type

杂志文章,评审

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