Tchem KISS1R KiSS-1 receptor

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

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

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: 288.48   (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: 288.48   (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: 152

Tclin

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

Active Drug: 0

Active Ligands (152)

Explore Active Ligands

1 – 10 of 152

CHEMBL3645504

KISS1RTchem GPCR

IC50: 9.62

CHEMBL2151652

KISS1RTchem GPCR

Ki: 9.92

CHEMBL2151646

KISS1RTchem GPCR

Ki: 10.29

CHEMBL3086284

KISS1RTchem GPCR

Ki: 10.05

CHEMBL388586

KISS1RTchem GPCR

IC50: 9.15

CHEMBL2151655

KISS1RTchem GPCR

Ki: 9.92

CHEMBL3087931

KISS1RTchem GPCR

Ki: 9.96

CHEMBL1165222

KISS1RTchem GPCR

IC50: 8.13

CHEMBL2151654

KISS1RTchem GPCR

Ki: 10.11

CHEMBL3645499

KISS1RTchem GPCR

IC50: 9.92

Pathways (9)

Reactome (7)

KEGG (2)

Class A/1 (Rhodopsin-like receptors) (R-HSA-373076)

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Items per page:

5

1 – 5 of 7

Data Source	Name	Explore in Pharos	Explore in Source
Reactome	Class A/1 (Rhodopsin-like receptors)	323 targets	R-HSA-373076
Reactome	G alpha (q) signalling events	219 targets	R-HSA-416476
Reactome	GPCR downstream signalling	1152 targets	R-HSA-388396
Reactome	GPCR ligand binding	460 targets	R-HSA-500792
Reactome	Peptide ligand-binding receptors	189 targets	R-HSA-375276

Name	Explore in Pharos	Explore in Source
Class A/1 (Rhodopsin-like receptors)	323 targets	R-HSA-373076
G alpha (q) signalling events	219 targets	R-HSA-416476
GPCR downstream signalling	1152 targets	R-HSA-388396
GPCR ligand binding	460 targets	R-HSA-500792
Peptide ligand-binding receptors	189 targets	R-HSA-375276

Gene Ontology Terms (9)

Functions (2)

Components (5)

Processes (2)

Items per page:

10

1 – 2 of 2

GO Term	Evidence	Assigned by
neuropeptide receptor activity	Inferred from Direct Assay (IDA)	UniProtKB
G protein-coupled peptide receptor activity	Inferred from Biological aspect of Ancestor (IBA)	GO_Central

Protein-Protein Interactions (206)

Explore Interacting Targets

1 – 10 of 206

• See Interactions on String-DB

KISS1

Tbio

Novelty: 0.00111063

Score: 0.997

Data Source: Reactome,STRINGDB

GNRH1

Tbio

Novelty: 0.00024998

Score: 0.994

Data Source: STRINGDB

GNRHR

Tclin

Family: GPCR

Novelty: 0.00227536

Score: 0.979

Data Source: STRINGDB

TAC3

Tchem

Novelty: 0.00210451

Score: 0.979

Data Source: STRINGDB

PROK2

Tbio

Novelty: 0.00558025

Score: 0.965

Data Source: STRINGDB

NPS

Tbio

Novelty: 0.00011983

Score: 0.964

Data Source: STRINGDB

NPFF

Tbio

Novelty: 0.00350925

Score: 0.961

Data Source: STRINGDB

UTS2R

Tchem

Family: GPCR

Novelty: 0.01075176

Score: 0.957

Data Source: STRINGDB

GNRH2

Tbio

Novelty: 0.00305192

Score: 0.955

Data Source: STRINGDB

QRFP

Tbio

Novelty: 0.02279173

Score: 0.941

Data Source: STRINGDB

Publication Statistics

PubMed Score  288.48

PubMed score by year

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PubTator Score  268.32

PubTator score by year

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Patents

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Amino Acid Sequence

Residue Counts

Sequence

MHTVATSGPNASWGAPANASGCPGCGANASDGPVPSPRAVDAWLVPLFFAALMLLGLVGNSLVIYVICRH

1-70

KPMRTVTNFYIANLAATDVTFLLCCVPFTALLYPLPGWVLGDFMCKFVNYIQQVSVQATCATLTAMSVDR

70-140

WYVTVFPLRALHRRTPRLALAVSLSIWVGSAAVSAPVLALHRLSPGPRAYCSEAFPSRALERAFALYNLL

140-210

ALYLLPLLATCACYAAMLRHLGRVAVRPAPADSALQGQVLAERAGAVRAKVSRLVAAVVLLFAACWGPIQ

210-280

LFLVLQALGPAGSWHPRSYAAYALKTWAHCMSYSNSALNPLLYAFLGSHFRQAFRRVCPCAPRRPRRPRR

280-350

PGPSDPAAPHAELLRLGSHPAPARAQKPGSSGLAARGLCVLGEDNAPL

350-398

MHTVATSGPNASWGAPANASGCPGCGANASDGPVPSPRAVDAWLVPLFFAALMLLGLVGNSLVIYVICRHKPMRTVTNFYIANLAATDVTFLLCCVPFTALLYPLPGWVLGDFMCKFVNYIQQVSVQATCATLTAMSVDRWYVTVFPLRALHRRTPRLALAVSLSIWVGSAAVSAPVLALHRLSPGPRAYCSEAFPSRALERAFALYNLLALYLLPLLATCACYAAMLRHLGRVAVRPAPADSALQGQVLAERAGAVRAKVSRLVAAVVLLFAACWGPIQLFLVLQALGPAGSWHPRSYAAYALKTWAHCMSYSNSALNPLLYAFLGSHFRQAFRRVCPCAPRRPRRPRRPGPSDPAAPHAELLRLGSHPAPARAQKPGSSGLAARGLCVLGEDNAPL

Find similar targets by:

Uniprot Keyword

Cell membrane
Complete proteome
Disease mutation
Disulfide bond
G-protein coupled receptor
Glycoprotein
Hypogonadotropic hypogonadism
Membrane
Polymorphism
Receptor