Target General Infomation
Target ID
T18872
Former ID
TTDR01010
Target Name
Malignant melanoma metastasis-suppressor KiSS-1
Gene Name
KISS1
Synonyms
KiSS-1; KISS1
Target Type
Clinical Trial
Disease Prostate cancer [ICD9: 185; ICD10: C61]
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.
BioChemical Class
Kisspeptin
UniProt ID
Sequence
MNSLVSWQLLLFLCATHFGEPLEKVASVGNSRPTGQQLESLGLLAPGEQSLPCTERKPAA
TARLSRRGTSLSPPPESSGSPQQPGLSAPHSRQIPAPQGAVLVQREKDLPNYNWNSFGLR
FGKREAAPGNHGRSAGRG
Drugs and Mode of Action
Drug(s) TAK-448 Drug Info Phase 2 Prostate cancer [525106]
Modulator TAK-448 Drug Info
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
References
Ref 525106ClinicalTrials.gov (NCT02381288) Effects of TAK-448 in Middle-aged and Older Men With Low Testosterone. U.S. National Institutes of Health.

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