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Updated: Jan 19, 2026

Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors
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Harnessing Ion-Binding Sites for GPCR Pharmacology

Barbara Zarzycka1, Saheem A Zaidi1, Bryan L Roth2

  • 1Departments of Biological Sciences (B.Z., S.A.Z., V.K.) and Chemistry (V.K.), Bridge Institute, Michelson Center for Convergent Bioscience, University of Southern California, Los Angeles, California; and Department of Pharmacology (B.L.R.) and Division of Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy (B.L.R.), University of North Carolina at Chapel Hill, Chapel Hill, North Carolina.

Pharmacological Reviews
|September 26, 2019
PubMed
Summary

Monovalent and divalent ions, especially sodium (Na+), allosterically modulate G-protein coupled receptors (GPCRs). Understanding ion binding sites and mechanisms offers new strategies for drug design and developing targeted therapies.

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