Kisspeptin-10 is a naturally occurring peptide derived from the KISS1 gene. It plays a pivotal role in regulating the hypothalamic-pituitary-gonadal axis, influencing the secretion of gonadotropin-releasing hormone (GnRH) and subsequently affecting reproductive hormone release. Kisspeptin-10 is of significant interest in research related to puberty, reproduction, and endocrine signaling.
Gonadotropin-releasing hormone (GnRH) is synthesized and released by GnRH neurons in the hypothalamus. It is the initial hormone in the hypothalamic-pituitary-gonadal axis and regulates the secretion of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) from the anterior pituitary gland. GnRH plays a crucial role in triggering puberty and controls the maturation of gametes in the reproductive organs. Therapeutically, it is used to regulate menstruation in specific cases, treat precocious puberty, and as a continuous infusion in certain cancer treatments.
By influencing circulating levels of LH and FSH, kisspeptin can modulate testosterone levels. This effect, however, appears to be sex-specific. In men, kisspeptin increases testosterone levels, whereas in women it has no significant impact. In one study, six men received an intravenous derivative of kisspeptin and exhibited a nearly threefold increase in plasma testosterone levels within 90 minutes. Another kisspeptin analog was found to modify the pulse frequency of LH in men, indicating that kisspeptin helps fine-tune the normal pulsatile release of sex hormones. A study on healthy men given kisspeptin-10 showed a rapid, dose-dependent rise in serum LH and a concurrent increase in testosterone. Kisspeptin-10 achieves this by enhancing the pulsatile release of LH; at sufficiently high doses, the pulsation becomes so rapid that individual pulses merge, resulting in continuous LH release. These findings suggest potential applications for kisspeptin and its analogs in contexts ranging from pregnancy to treatment of low testosterone.
Kisspeptin neurons are known to be sensitive to an individual's energy status. Both undernutrition and severe overnutrition can suppress the ability of kisspeptin neurons to stimulate GnRH release. Drastic changes in energy balance can cause infertility in both sexes, a process mediated by kisspeptin.
It is well established that kisspeptin production and release are sensitive to energy balance. Emerging evidence suggests that kisspeptin itself may regulate energy balance. This insight arose from studies in mice genetically modified to lack the kisspeptin receptor (Kiss1r), which showed increased fat accumulation and reduced energy expenditure. The kisspeptin receptor is present in both white and brown adipose (fat) tissues. Given the tight link between energy status and reproductive fitness, it is not surprising that kisspeptin may be a key mediator in neurochemical pathways that regulate energy-related behaviors in relation to reproduction.
Twenty years ago, kisspeptin was found to suppress melanoma (malignant skin cancer) metastasis by up to 95%, primarily by reducing cancer cell migration. There is also evidence suggesting that kisspeptin may reduce cell adhesion, preventing cancer cells from invading other tissues. Screening across multiple metastatic cancer types, including breast, bladder, gastrointestinal, prostate, pancreatic, ovarian, skin, and thyroid cancers, has revealed general decreases in kisspeptin levels, confirming its role in cancer spread.
Interest in kisspeptin as a cancer treatment has fluctuated due to the peptide’s complexity. Ongoing research aims to understand how kisspeptin can be manipulated—cut, recombined, or altered—to exert therapeutic effects on various cancers. Rather than lacking efficacy, kisspeptin’s diverse actions make it challenging to isolate its precise impact on different cancer cells. Dr. Floriana Morgillo encourages researchers to embrace this complexity to unlock kisspeptin’s potential to block metastasis in multiple organs, substantially reduce disease burden, extend patients’ lifespans, and enhance the effectiveness of existing treatments.
A noteworthy link between kisspeptin, melatonin, and cancer was discovered in early 2020 through experiments relating peptide levels to daylight exposure. Mice exposed to alternating periods of daylight and darkness exhibited markedly different melatonin and kisspeptin levels. Daylight-exposed mice showed high kisspeptin and low melatonin levels, while those kept in darkness exhibited the reverse. When injected with melanoma cells, the daylight mice developed larger tumors with higher growth rates. Although metastasis was not assessed, this suggests a complex interaction where melatonin and kisspeptin influence tumor suppression, with one modulating the other; however, the exact relationship remains unclear. This example highlights kisspeptin’s multifaceted role in tumor growth regulation.
Certain kisspeptin analogs appear important in brain regions responsible for memory consolidation and spatial orientation. Mouse studies indicate that administering these peptides can reverse learning and navigation impairments caused by ethanol intoxication. These findings imply that kisspeptin and its analogs contribute to neuronal information encoding and may have potential in counteracting learning deficits associated with genetic and chronic diseases. Although early-stage, this research broadens understanding of learning mechanisms and advances the development of nootropics that enhance brain function in both healthy and impaired individuals.
Reproductive and energy status are linked, and similarly, reproduction and emotion are interconnected. Given kisspeptin’s role in reproduction and energy homeostasis, researchers investigated its influence on emotion and behavior. In a study with 29 healthy heterosexual men, kisspeptin administration enhanced limbic brain activity, increased reward-seeking behavior, drive, and improved overall mood compared to placebo. These results suggest kisspeptin integrates sexual and emotional brain processes with reproductive functions, enhancing understanding of mood, motivation, and drive as they relate to human behavior beyond sexual contexts.
While kisspeptin’s reproductive role is well-known, it also plays important roles in the kidney. Kisspeptin and its receptor are present in multiple kidney regions and are believed to contribute to kidney function signaling. Studies in mice lacking the Kiss1 receptor show kisspeptin is essential for proper glomerular development during kidney formation, although whether this action is direct or indirect remains unclear.
Although kisspeptin’s precise role in the kidney is not fully understood, it may be linked to its broader function in regulating vascular development and responses to injury. Cardiovascular disease research in mice indicates kisspeptin may control vasoconstriction and cardiac output in specific vascular beds. Its influence on both the kidney and cardiovascular system likely relates to its effects on angiogenesis and vascular function, traits that may also underlie its ability to reduce tumor metastasis. Understanding kisspeptin’s vascular actions will facilitate its therapeutic development.
Kisspeptin is a peptide that primarily acts in the brain to regulate hormone secretion related to human reproduction. There is substantial interest in how kisspeptin influences testosterone levels and sex-related behaviors such as drive and motivation. It has also been known for years that kisspeptin can affect cancer cell growth and metastasis, though studies have yielded mixed results, causing fluctuating research focus on its use in chemotherapy. Kisspeptin’s impact on metastasis may be connected to its role in vascular growth and function. Currently, kisspeptin is the subject of intensive research aiming to deepen understanding of this versatile, potentially life-saving peptide.
Kisspeptin-10 exhibits minimal to moderate side effects, moderate oral bioavailability, and excellent subcutaneous bioavailability in mice. Dosages effective in mice do not scale directly to humans. Kisspeptin-10 sold by Peptide Sciences is strictly for educational and scientific research purposes only and is not intended for human consumption. Purchase is restricted to licensed researchers.
Kisspeptin-10 is primarily utilized in scientific studies focusing on:
Kisspeptin-10 is intended strictly for laboratory research and is not approved for human consumption. Handle with care, following appropriate safety protocols. Ensure proper storage conditions to maintain the integrity and efficacy of the compound.
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