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Updated: Jul 16, 2025

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
Published on: February 20, 2018
Nanomolar range of FAM237B can activate receptor GPR83
Hao-Zheng Li1, Ya-Fen Wang1, Wen-Feng Hu1
1Research Center for Translational Medicine at East Hospital, School of Life Sciences and Technology, Tongji University, 1239 Siping Road, Shanghai, 200092, China.
Abstract:
Our recent study confirmed that the mature neuropeptide FAM237A, also known as neurosecretory protein GL (NPGL), is an efficient agonist for GPR83. The paralog FAM237B was previously reported as a weak agonist for GPR83. In the present study, we prepared mature human FAM237B via an intein-fusion approach and demonstrated that it could cause a significant activation effect at the nanomolar range (1‒10 nM) in a NanoBiT-based β-arrestin recruitment assay. Thus, FAM237B appears to be another endogenous agonist for GPR83 and future in vivo studies will be required to confirm this.
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