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Updated: Jan 10, 2026

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
07:41

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators

Published on: February 20, 2018

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Multiple Allosteric Sites Allow for Synergistic Enhancement of GPCR Signaling

Kai Wang, Snezana T Dimova, John N Hanson

    Biorxiv : the Preprint Server for Biology
    |November 24, 2025
    PubMed
    Summary

    Positive allosteric modulators (PAMs) can synergistically amplify signals at the D1 dopamine receptor (D1R). This study reveals a multi-site cooperative mechanism enhancing dopamine potency over 1,000-fold, offering new therapeutic strategies.

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