Journal article

New small molecule fluorescent probes for G protein-coupled receptors: valuable tools for drug discovery

Joshua W Conner, Daniel P Poole, Manuela Jorg, Nicholas A Veldhuis

FUTURE MEDICINAL CHEMISTRY | FUTURE SCI LTD | Published : 2020

Abstract

G protein-coupled receptors (GPCRs) are essential signaling proteins and tractable therapeutic targets. To develop new drug candidates, GPCR drug discovery programs require versatile, sensitive pharmacological tools for ligand binding and compound screening. With the availability of new imaging modalities and proximity-based ligand binding technologies, fluorescent ligands offer many advantages and are increasingly being used, yet labeling small molecules remains considerably more challenging relative to peptides. Focusing on recent fluorescent small molecule studies for family A GPCRs, this review addresses some of the key challenges, synthesis approaches and structure-activity relationship..

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University of Melbourne Researchers

Grants

Awarded by Australian Research Council Centre of Excellence in Convergent Bio-Nano Science and Technology


Awarded by Newcastle Monash Academic Track (NUMAcT) Scheme by Research England


Funding Acknowledgements

This work was supported by the Australian Research Council Centre of Excellence in Convergent Bio-Nano Science and Technology (project no. CE140100036). Research in the laboratory of D Poole and N Veldhuis is funded in part by Takeda Pharmaceuticals Inc. M Jorg is a Monash and Newcastle University Fellow supported the Newcastle Monash Academic Track (NUMAcT) Scheme (ref. 131911) by Research England. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.