GPRC6A? is the receptor for osteocalcin as well as structurally unrelated ligands including L-amino acids, cations and anabolic steroids.1?GPRC6A is a potential therapeutic target for treating type 2 diabetes.2 DJ-V 159 (2253744-53-3) is an agonist at GPRC6A which activates ERK and upregulates cAMP levels in HEK-193 cells expressing GPRC6A. It stimulates insulin secretion in mouse β-cells and lowers blood glucose in mouse models.3
1) Pi and Quarles (2012),?Multiligand specificity and wide tissue expression of GPRC6A reveals new endocrine networks; Endocrinology,?153?2062
2) Pi?et al.?(2016),?GPRC6A: Jack of all metabolism (or master of none); Mol. Metab.,?6?185
3) Pi?et al.?(2018),?Computationally identified novel agonists for GPRC6A; PLoS One,?13?e0195980
