Target intelligence / Profile preview

Kisspeptin protein (KP (or KISS1, depending on context))

Target
KP (or KISS1, depending on context)
Molecular classification
neuropeptide, RFamide peptide family, peptide hormone, ligand (for G protein-coupled receptor)
01

Overview

Kisspeptin is a family of peptide hormones encoded by the KISS1 gene, with key forms including kisspeptin-54 and shorter peptides like kisspeptin-10. Kisspeptins are endogenous ligands of the G protein-coupled receptor KISS1R (GPR54). Originally discovered as a metastasis-suppressor (metastin), kisspeptin is now recognized for its role as a central regulator of puberty onset and fertility through stimulation of gonadotropin-releasing hormone (GnRH) neurons in the hypothalamus, thus controlling pituitary release of LH and FSH and downstream sexual maturation[1][2][3][6][7]. Kisspeptin/KISS1R signaling also has roles in cancer biology (especially triple-negative breast cancer), metastasis suppression, and potentially metabolic regulation[4][10]. Therapeutic analogs and receptor antagonists/agonists are under investigation for disorders of puberty, infertility, and certain cancers, as well as for possible use as contraceptives[2][6][9].

Other names
metastinKISS1-derived peptideskisspeptin-54KP-54kisspeptin-10kisspeptin-13kisspeptin-14
02

Mechanism of action

stimulation or inhibition of GnRH secretion by acting as an endogenous ligand for GPR54/KISS1R (a G protein-coupled receptor), leading to downstream pituitary hormone (LH, FSH) release and regulation of sex steroid production[2][6][7][9]

03

Biological functions

regulation of gonadotropin-releasing hormone (GnRH) secretionpuberty onsetsexual maturationreproductive axis regulationmetastasis suppressionpotential role in metabolism
04

Disease associations

reproductive disorders (hypogonadotropic hypogonadism, precocious puberty)cancer (metastasis suppression in melanoma, breast cancer, involvement in triple-negative breast cancer)potential roles in metabolic, liver, and bone disorders
05

Safety considerations

rapid proteolytic degradation limits therapeutic utility for native peptides[6]hormonal side effects from agonism/antagonism of reproductive hormone axis (e.g., altered puberty, fertility issues)onco-metabolic concerns in some cancers[4][6]
06

Interacting drugs

kisspeptin analogs (agonists/antagonists, some in clinical studies)

1 more in the full profile.

07

Biomarkers

gonadotropin hormone levels (LH, FSH) as effect biomarkersplasma kisspeptin levels proposed for surveillance/diagnosis in disease contexts[4]KISS1/KISS1R expression linked to disease progression/recurrence in cancer[4]

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