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A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
Published on: February 20, 2018
The GPCR, class C, group 6, subtype A (GPRC6A) receptor: from cloning to physiological function
C Clemmensen1, S Smajilovic, P Wellendorph
1Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark.
British Journal of Pharmacology
|September 17, 2013
Summary
The G protein-coupled receptor class C group 6 subtype A (GPRC6A) is activated by amino acids and cations. Studies suggest GPRC6A plays a role in inflammation, metabolism, and endocrine functions, making it a potential drug target.
Area of Science:
- Pharmacology
- Molecular Biology
- Endocrinology
Background:
- G protein-coupled receptor class C group 6 subtype A (GPRC6A) is a class C GPCR found in humans, mice, and rats.
- GPRC6A is activated by basic L-α-amino acids (e.g., L-arginine, L-lysine) and divalent cations (e.g., Ca2+).
- Osteocalcin and testosterone are also suggested as endogenous GPRC6A agonists.
Purpose of the Study:
- To investigate the physiological functions of GPRC6A.
- To explore the potential of GPRC6A as a therapeutic target.
Main Methods:
- Analysis of genetically modified mice lacking the GPRC6A receptor.
- Biochemical assays to determine receptor activation by various ligands.
Main Results:
- GPRC6A is widely expressed across species.
- Evidence suggests GPRC6A involvement in regulating inflammation, metabolism, and endocrine functions.
- Despite some discrepancies in research, a growing body of evidence supports GPRC6A's physiological roles.
Conclusions:
- GPRC6A is implicated in key physiological processes.
- GPRC6A represents a promising target for novel therapeutic interventions in inflammation, metabolic disorders, and endocrine diseases.
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