Tclin CASR Extracellular calcium-sensing receptor

Protein Summary

Description

G-protein-coupled receptor that senses changes in the extracellular concentration of calcium ions and plays a key role in maintaining calcium homeostasis (PubMed:7759551, PubMed:8702647, PubMed:8636323, PubMed:8878438, PubMed:17555508, PubMed:19789209, PubMed:21566075, PubMed:22114145, PubMed:23966241, PubMed:25292184, PubMed:25104082, PubMed:26386835, PubMed:25766501, PubMed:22789683). Senses fluctuations in the circulating calcium concentration and modulates the production of parathyroid hormone (PTH) in parathyroid glands (By similarity). The activity of this receptor is mediated by a G-protein that activates a phosphatidylinositol-calcium second messenger system (PubMed:7759551). The G-protein-coupled receptor activity is activated by a co-agonist mechanism: aromatic amino acids, such as Trp or Phe, act concertedly with divalent cations, such as calcium or magnesium, to achieve full receptor activation (PubMed:27434672, PubMed:27386547). The protein encoded by this gene is a plasma membrane G protein-coupled receptor that senses small changes in circulating calcium concentration. The encoded protein couples this information to intracellular signaling pathways that modify parathyroid hormone secretion or renal cation handling, and thus this protein plays an essential role in maintaining mineral ion homeostasis. Mutations in this gene are a cause of familial hypocalciuric hypercalcemia, neonatal severe hyperparathyroidism, and autosomal dominant hypocalcemia. [provided by RefSeq, Aug 2017]

Uniprot Accession IDs

• P41180
• Q13912
• Q16108
• Q16109
• Q16110
• Q16379
• Q2M1T0
• Q4PJ19
• CaR

Gene Name

• CASR

Ensembl ID

• ENST00000498619
• ENSP00000420194
• ENSG00000036828
• ENST00000638421
• ENSP00000492190
• ENST00000639785
• ENSP00000491584

Symbol

• GPRC2A
• PCAR1
• CAR
• FHH
• FIH
• HHC
• EIG8
• HHC1
• NSHPT
• PCAR1
• hCasR
• GPRC2A
• HYPOC1

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
protein domain	0.85
phenotype	0.81
biological term	0.78
disease	0.68
chemical	0.67

Protein Classes

PANTHER Classes

Protein / Transporter / Ion Channel / Ligand-gated Ion Channel / Ionotropic Glutamate Receptor / Extracellular Calcium-sensing Receptor

Protein / Receptor / Ligand-gated Ion Channel / Ionotropic Glutamate Receptor / Extracellular Calcium-sensing Receptor

Protein / Receptor / G-protein Coupled Receptor / Extracellular Calcium-sensing Receptor

DTO Classes

Protein / G-protein Coupled Receptor / Class C Metabotropic Glutamate/pheromone / Calcium-sensing Receptor / Extracellular Calcium-sensing Receptor

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 2028.74   (req: < 5)

Gene RIFs: 420   (req: <= 3)

Antibodies: 596   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 2028.74   (req: >= 5)

Gene RIFs: 420   (req: > 3)

Antibodies: 596   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 43

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 233

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drugs: 4