High impact information on GPRC6A

• Also, osteocalcin, a calcium-binding protein highly expressed in bone, dose-dependently stimulated GPRC6A activity in the presence of calcium but inhibited the calcium-dependent activation of CASR [1].
• Reverse transcription-PCR analyses showed that mouse GPRC6A is widely expressed in mouse tissues, including bone, calvaria, and the osteoblastic cell line MC3T3-E1 [1].
• In addition, calcium, magnesium, strontium, aluminum, gadolinium, and the calcimimetic NPS 568 resulted in a dose-dependent stimulation of GPRC6A overexpressed in human embryonic kidney cells 293 cells [1].
• Regulators of G-protein signaling (RGS) proteins, through their GTPase activating protein (GAP) activities, inhibit GPCR-mediated signaling by inactivating G proteins [2].
• We recently reported the cloning and analysis of expression of a novel human family C G-protein-coupled receptor, termed hGPRC6A [3].

Biological context of GPRC6A

• Alignment of GPRC6A with CASR revealed conservation of both calcium and calcimimetic binding sites [1].
• Three isoforms of GPRC6A are expressed from the same gene by alternative splicing [4].

Anatomical context of GPRC6A

• GPRC6A is widely expressed in brain and peripheral tissues with highest levels in kidney, skeletal muscle, testis, and leucocytes [5].
• Immunocytochemical analysis of the cloned mouse GPRC6A cDNA expressed in human embryonic kidney 293 cells demonstrated that GPRC6A was present on the plasma membrane, as well as in the endoplasmic reticulum and nuclear envelope membranes of transfected cells [6].

Associations of GPRC6A with chemical compounds

• Homology modeling of the hGPRC6A ATD based on the crystal structure of the metabotropic glutamate receptor subtype 1 predicted interaction with alpha-amino acids and was employed to rationally select potential ligands [3].
• Agonists for GPRC6A are basic amino acids, particularly the analogues and derivatives of L-arginine and L-ornithine [4].

Physical interactions of GPRC6A

• A new family of G-protein-coupled receptors (GPRC6A) has recently been described and characterized with unknown physiological role [4].

Other interactions of GPRC6A

• Molecular cloning, expression, and sequence analysis of GPRC6A, a novel family C G-protein-coupled receptor [5].
• The transcript, entitled GPRC6A (isoform 1), was cloned from a human kidney cDNA (DNA complementary to RNA) library and shown to encode a protein of 926 amino acids (aa) [5].
• The Ca2+-sensing receptor (CaR) is a pleiotropic, type III G protein-coupled receptor (GPCR) that associates functionally with the cytoskeletal protein filamin [7].

References