Tchem KISS1R KiSS-1 receptor

Protein Summary

Description

Receptor for metastin (kisspeptin-54 or kp-54), a C-terminally amidated peptide of KiSS1. KiSS1 is a metastasis suppressor protein that suppresses metastases in malignant melanomas and in some breast carcinomas without affecting tumorigenicity. The metastasis suppressor properties may be mediated in part by cell cycle arrest and induction of apoptosis in malignant cells. The receptor is essential for normal gonadotropin-released hormone physiology and for puberty. The hypothalamic KiSS1/KISS1R system is a pivotal factor in central regulation of the gonadotropic axis at puberty and in adulthood. The receptor is also probably involved in the regulation and fine-tuning of trophoblast invasion generated by the trophoblast itself. Analysis of the transduction pathways activated by the receptor identifies coupling to phospholipase C and intracellular calcium release through pertussis toxin-insensitive G(q) proteins. The protein encoded by this gene is a galanin-like G protein-coupled receptor that binds metastin, a peptide encoded by the metastasis suppressor gene KISS1. The tissue distribution of the expressed gene suggests that it is involved in the regulation of endocrine function, and this is supported by the finding that this gene appears to play a role in the onset of puberty. Mutations in this gene have been associated with hypogonadotropic hypogonadism and central precocious puberty. [provided by RefSeq, Jul 2008]

Uniprot Accession IDs

• Q969F8
• A5D8U2
• B2RTV1
• Q96QG0
• KiSS-1R

Gene Name

• KISS1R

Ensembl ID

• ENST00000234371
• ENSP00000234371
• ENSG00000116014

Symbol

• AXOR12
• GPR54
• HH8
• CPPB1
• GPR54
• AXOR12
• KISS-1R
• HOT7T175

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
cell type or tissue	0.9
biological process	0.77
biological term	0.7
phenotype	0.63
transcription factor	0.6

Protein Classes

PANTHER Classes

Protein / Receptor / G-protein Coupled Receptor / Kiss-1 Receptor

DTO Classes

Protein / G-protein Coupled Receptor / Class A Rhodopsin Like / Kisspeptin Receptor / Kiss-1 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: 402.74   (req: < 5)

Gene RIFs: 75   (req: <= 3)

Antibodies: 315   (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: 402.74   (req: >= 5)

Gene RIFs: 75   (req: > 3)

Antibodies: 315   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 4

Tchem

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

Active Ligands: 207

Tclin

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

Active Drug: 0