Conformational Dynamics of Single G Protein-Coupled Receptors in Solution

作者: Samuel Bockenhauer , Alexandre Fürstenberg , Xiao Jie Yao , Brian K. Kobilka , W. E. Moerner

DOI: 10.1021/JP204843R

关键词:

摘要: G protein-coupled receptors (GPCRs) comprise a large family of seven-helix transmembrane proteins which regulate cellular signaling by sensing light, ligands, and binding proteins. The GPCR activation process, however, is not simple on–off switch; current models suggest complex conformational landscape in the active, state includes multiple conformations with similar downstream activity. present study probes dynamics single β2-adrenergic (β2ARs) solution phase Anti-Brownian ELectrokinetic (ABEL) trapping. ABEL trap uses fast electrokinetic feedback microfluidic configuration to allow direct observation fluorescently labeled β2AR for hundreds milliseconds seconds. By choosing reporter dye labeling site sensitive ligand binding, we observe diversity discrete fluorescence intensity lifetime levels β2ARs, indicating varying radiative range states ...

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