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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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Bibliografiske detaljer
Udgivet i: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
Sprog:Inglês
Udgivet: BlackWell Publishing Ltd 2014
Fag:
Online adgang: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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