General Information of Drug Therapeutic Target (DTT) (ID: TTU2O6T)

DTT Name Metastasis-suppressor KiSS-1 (KISS1)
Synonyms KiSS-1; KISS1
Gene Name KISS1
DTT Type
Clinical trial target
[1]
UniProt ID
KISS1_HUMAN
TTD ID
T18872
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MNSLVSWQLLLFLCATHFGEPLEKVASVGNSRPTGQQLESLGLLAPGEQSLPCTERKPAA
TARLSRRGTSLSPPPESSGSPQQPGLSAPHSRQIPAPQGAVLVQREKDLPNYNWNSFGLR
FGKREAAPGNHGRSAGRG
Function
Metastasis suppressor protein in malignant melanomas and in some breast cancers. May regulate events downstream of cell- matrix adhesion, perhaps involving cytoskeletal reorganization. Generates a C-terminally amidated peptide, metastin which functions as the endogenous ligand of the G-protein coupled receptor GPR54. Activation of the receptor inhibits cell proliferation and cell migration, key characteristics of tumor metastasis. Kp-10 is a decapeptide derived from the primary translation product, isolated in conditioned medium of first trimester trophoblast. Kp-10, but not other kisspeptins, increased intracellular Ca(2+) levels in isolated first trimester trophoblasts. Kp-10 is a paracrine/endocrine regulator in fine- tuning trophoblast invasion generated by the trophoblast itself. The receptor is also essential for normal gonadotropin-released hormone physiology and for puberty. The hypothalamic KiSS1/GPR54 system is a pivotal factor in central regulation of the gonadotropic axis at puberty and in adulthood.
KEGG Pathway
Neuroactive ligand-receptor interaction (hsa04080 )
GnRH secretion (hsa04929 )
Reactome Pathway
G alpha (q) signalling events (R-HSA-416476 )
Peptide ligand-binding receptors (R-HSA-375276 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
1 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
TAK-448 DMD51RN Prostate cancer 2C82.0 Phase 2 [1]
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Molecular Expression Atlas (MEA) of This DTT

Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This DTT
Disease Name ICD 11 Studied Tissue p-value Fold-Change Z-score
Prostate cancer 2C82 Prostate 6.40E-01 -0.01 -0.04
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References

1 Pharmacologic profiles of investigational kisspeptin/metastin analogues, TAK-448 and TAK-683, in adult male rats in comparison to the GnRH analogue leuprolide.Eur J Pharmacol.2014 Jul 15;735:77-85.