Molecular mechanism of allosteric modulation at GPCRs: insight from a binding kinetics study at the human A(1) adenosine receptor

BACKGROUND AND PURPOSE: Many GPCRs can be allosterically modulated by small-molecule ligands. This modulation is best understood in terms of the kinetics of the ligand–receptor interaction. However, many current kinetic assays require at least the (radio)labelling of the orthosteric ligand, which is...

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Bibliographic Details
Published in:Br J Pharmacol
Main Authors: Guo, Dong, Venhorst, Suzanne N, Massink, Arnault, van Veldhoven, Jacobus P D, Vauquelin, Georges, IJzerman, Adriaan P, Heitman, Laura H
Format: Artigo
Language:Inglês
Published: BlackWell Publishing Ltd 2014
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Research Papers
Online Access:https://ncbi.nlm.nih.gov/pmc/articles/PMC4294041/
https://ncbi.nlm.nih.gov/pubmed/25040887
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1111/bph.12836
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