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Article

Ligand modulation of the conformational dynamics of the A2A adenosine receptor revealed by single-molecule fluorescence.

Scientific reports - 15 Mar 2021

Fernandes Dennis D, Neale Chris, Gomes Gregory-Neal W, Li Yuchong, Malik Aimen, Pandey Aditya, Orazietti Alexander P, Wang Xudong, Ye Libin, Scott Prosser R, Gradinaru Claudiu C

Abstract excerpt

G protein-coupled receptors (GPCRs) are the largest class of transmembrane proteins, making them an important target for therapeutics. Activation of these receptors is modulated by orthosteric ligands, which stabilize one or several states within a complex conformational ensemble. The intra- and inter-state dynamics, however, is not well documented. Here, we used single-molecule fluorescence to measure...

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Identifiers

PMID: 33723285
DOI: 10.1038/s41598-021-84069-0
PMCID: PMC7960716

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