Work

Fluorescent ligands: Bringing light to emerging GPCR paradigms

Year: 2019

Type: review

Abstract: In recent years, several novel aspects of GPCR pharmacology have been described, which are thought to play a role in determining the in vivo efficacy of a compound. Fluorescent ligands have been used to study many of these, which have also required the development of new experimental approaches. Fluorescent ligands offer the potential to use the same fluorescent probe to perform a broad range of experiments, from single-molecule microscopy to in vivo BRET. This review provides an overview of the in vitro use of fluorescent ligands in further understanding emerging pharmacological paradigms within the GPCR field, including ligand-binding kinetics, allosterism and intracellular signalling, along with the use of fluorescent ligands to study physiologically relevant therapeutic agents.

Source: British Journal of Pharmacology

DOI: 10.1111/bph.14953

Authors: Mark Soave, Stephen J. Briddon, Stephen J. Hill, Leigh A. Stoddart

Institutions: University of Nottingham, University of Birmingham

Language: English

Topic: Receptor Mechanisms and Signaling

Subfield: Molecular Biology

Field: Biochemistry, Genetics and Molecular Biology

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: green

Funder: Medical Research Council