Assays with Detection of Fluorescence Anisotropy: Challenges and Possibilities for Characterizing Ligand Binding to GPCRs

Trends in Pharmacological Sciences
Ago RinkenSergei Kopanchuk

Abstract

Binding of fluorescent ligands (tracers) to their target receptors can be directly monitored over time, as the binding of a low-molecular-weight (LMW) tracer to a larger particle causes an increase of fluorescence anisotropy (FA). The combination of bright fluorophores, tracers with low nonspecific binding, and budded baculovirus particles (BVPs) for overexpression of G protein-coupled receptors (GPCRs) ensures a high signal-to-noise ratio in FA assays. The obtained data enable quantitative assessment of equilibrium binding and kinetic parameters for both the tracer and competing compounds as well as an estimation of the receptor concentration. FA assays have clear potential for implementation in drug screening systems, but also in studies of ligand-binding mechanisms for particular GPCRs.

Citations

Nov 19, 2019·The FEBS Journal·Pierre CalmetIsabel D Alves
Dec 14, 2019·Expert Opinion on Drug Discovery·Asko Uri, Olivier Etebe Nonga
Jul 26, 2019·Environmental Monitoring and Assessment·E ViirlaidT Rinken
Jan 16, 2020·ACS Medicinal Chemistry Letters·Max KellerNicholas D Holliday
Dec 16, 2020·Scientific Reports·Anni AllikaltDorothee Weikert
Dec 22, 2020·Biochimica Et Biophysica Acta. Molecular Cell Research·Lukas GrätzAgo Rinken
Mar 7, 2021·Biophysical Journal·Kirsten S KoretzAnne S Robinson
Aug 25, 2020·ACS Medicinal Chemistry Letters·Sabrina BiselliGünther Bernhardt
Jul 5, 2019·Langmuir : the ACS Journal of Surfaces and Colloids·Anand Lopez, Juewen Liu

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