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Updated: May 9, 2026

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
Published on: February 20, 2018
[The pharmacological effect of allosteric regulation at GPCR heterodimer]
Ning Zhang1, Jing Chen, Lei Gong
1Qufu Normal University, Qufu 273165, China.
Abstract:
Traditionally GPCR can exist as monomer, and its function is linear. The signal is transduced when the ligand binds to the orthosteric site. It has been reported that GPCR can form homodimer or heterodimer. In the dimers, allosteric sites will form when ligand binds to one monomer and then regulates of another monomer. Therefore the signaling pathway and the function of the receptor will be changed. Compared to orthosteric agonists, allosteric modulators have a number of potential advantages, which make allosteric modulators as a drug discovery candidate for GPCR. Herein, we introduce the concept of allosteric regulation at GPCR dimers, and its impact on the function of the receptor. We also introduce the drug screening methods of allosteric regulator, and those will contribute to drug discovery for GPCR.
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