Details of the Target

General Information of Target

Target ID LDTP09993
Target Name KiSS-1 receptor (KISS1R)
Gene Name KISS1R
Gene ID 84634
Synonyms
AXOR12; GPR54; KiSS-1 receptor; KiSS-1R; G-protein coupled receptor 54; G-protein coupled receptor OT7T175; hOT7T175; Hypogonadotropin-1; Kisspeptins receptor; Metastin receptor
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MGKLQSKHAAAARKRRESPEGDSFVASAYASGRKGAEEAERRARDKQELPNGDPKEGPFR
EDQCPLQVALPAEKAEGREHPGQLLSADDGERAANREGPRGPGGQRLNIDALQCDVSVEE
DDRQEWTFTLYDFDNCGKVTREDMSSLMHTIYEVVDASVNHSSGSSKTLRVKLTVSPEPS
SKRKEGPPAGQDREPTRCRMEGELAEEPRVADRRLSAHVRRPSTDPQPCSERGPYCVDEN
TERRNHYLDLAGIENYTSRFGPGSPPVQAKQEPQGRASHLQARSRSQEPDTHAVHHRRSQ
VLVEHVVPASEPAARALDTQPRPKGPEKQFLKSPKGSGKPPGVPASSKSGKAFSYYLPAV
LPPQAPQDGHHLPQPPPPPYGHKRYRQKGREGHSPLKAPHAQPATVEHEVVRDLPPTPAG
EGYAVPVIQRHEHHHHHEHHHHHHHHHFHPS
Target Type
Discontinued
Target Bioclass
GPCR
Family
G-protein coupled receptor 1 family
Subcellular location
Cell membrane
Function
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.
TTD ID
T39123
Uniprot ID
Q969F8
DrugMap ID
TT3KBZY
Ensemble ID
ENST00000234371.10
HGNC ID
HGNC:4510
ChEMBL ID
CHEMBL5413

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
NAIA_4
 Probe Info  		N.A.  LDD2226  [1]
TPP-AC
 Probe Info  		N.A.  LDD0427  [2]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Serine/threonine-protein phosphatase 2A catalytic subunit alpha isoform (PPP2CA) PPP phosphatase family P67775
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Guanine nucleotide-binding protein G(q) subunit alpha (GNAQ) G-alpha family P50148

The Drug(s) Related To This Target

Investigative
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
4-fluorobenzoyl-phe-gly-leu-arg-trp-nh2 Small molecular drug D0JE3Z
Kisspeptin-10 Small molecular drug D01VSI
Anz-100 . DB05967
Discontinued
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Tak-683 Small molecular drug D0P9KL

References

1 N-Acryloylindole-alkyne (NAIA) enables imaging and profiling new ligandable cysteines and oxidized thiols by chemoproteomics. Nat Commun. 2023 Jun 15;14(1):3564. doi: 10.1038/s41467-023-39268-w.
Mass spectrometry data entry: PXD041264
2 Differently Tagged Probes for Protein Profiling of Mitochondria. Chembiochem. 2019 May 2;20(9):1155-1160. doi: 10.1002/cbic.201800735. Epub 2019 Mar 26.