Kisspeptin-10 10mg

Description

Kisspeptin is a naturally occurring human protein that plays critical roles in hormone signaling during puberty and reproduction. It is primarily known for its ability to regulate gonadotropin-releasing hormone (GnRH), which is essential for reproductive function. Beyond reproduction, kisspeptin is also implicated in altering mood and behavior, promoting angiogenesis (the formation of new blood vessels), and regulating kidney function. The peptide is present in the brain and has been shown to suppress tumor growth and metastasis, highlighting its potential in cancer research.

Kisspeptin-10 Structure

Sequence: YNWNSFGLRF
Molecular Formula: C63H83N17O14
Molecular Weight: 1302.4 g/mol
PubChem CID: 25240297
Synonyms: KISS-1, Protein KISS-1, metastin, Kp-10 peptide

Source: PubChem

Kisspeptin-10 Research

Boosting Gonadotropin-Releasing Hormone

Gonadotropin-releasing hormone (GnRH) is synthesized and released by neurons in the hypothalamus. It is the initial hormone in the hypothalamic-pituitary-gonadal (HPG) axis and regulates the secretion of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) from the anterior pituitary gland. GnRH is the primary hormonal driver of puberty and controls the maturation of gametes in the reproductive organs. Therapeutically, GnRH analogues are used to manage menstruation, treat precocious puberty, and as continuous infusions in certain cancers.

Increasing Testosterone

Kisspeptin influences circulating levels of LH and FSH, thereby modulating testosterone levels, but this effect is sex-specific. In men, kisspeptin increases testosterone, while in women, it does not significantly affect testosterone. For example, in one study, intravenous administration of a kisspeptin derivative to six men resulted in nearly a threefold rise in plasma testosterone within 90 minutes[1]. Another kisspeptin analogue has been shown to modify the pulsatile frequency of LH release in men, helping to fine-tune normal sex hormone secretion. Healthy men given kisspeptin-10 exhibited a rapid, dose-dependent increase in serum LH and testosterone levels. At sufficiently high doses, kisspeptin-10 induced continuous LH release by causing rapid pulsations that blurred individual pulses[2]. These findings suggest potential applications for kisspeptin analogues in treating low testosterone and reproductive conditions.

Energy Balance

Kisspeptin neurons are highly sensitive to an individual’s energy status. Both undernutrition and severe overnutrition can blunt kisspeptin’s stimulation of GnRH release. Extreme energy imbalances can cause infertility in men and women, a process mediated by kisspeptin.

Emerging research indicates that kisspeptin itself may regulate energy balance. In mice lacking the kisspeptin receptor (Kiss1r), genetic manipulation led to increased fat accumulation and reduced energy expenditure. Kisspeptin receptors are expressed in adipose tissue, including brown fat[3]. This aligns with the close evolutionary relationship between energy status and reproductive fitness, suggesting kisspeptin as a key neurochemical link between energy regulation and reproductive behavior.

Cancer Research

Kisspeptin was discovered two decades ago to suppress melanoma metastasis by up to 95%. This anti-metastatic effect is believed to result from kisspeptin’s ability to reduce cancer cell migration. Additionally, kisspeptin may interfere with cancer cell adhesion, preventing their attachment to and invasion of other tissues. Various metastatic cancers—including breast, bladder, gastrointestinal, prostate, pancreatic, ovarian, skin, and thyroid cancers—show altered, generally decreased, kisspeptin expression levels, highlighting kisspeptin’s role in modulating cancer spread[4].

Source: ScienceDirect

The Complexity of Kisspeptin in Cancer Research

Interest in kisspeptin as a cancer treatment has fluctuated due to the peptide’s remarkable complexity. Ongoing research seeks to understand how kisspeptin can be manipulated, cleaved, recombined, or modified to produce beneficial effects across different cancer types. The challenge lies not in kisspeptin’s efficacy but rather in its multifaceted actions, which make it difficult to isolate its precise impact on various cancer cells[5]. Dr. Floriana Morgillo urges researchers to embrace these complexities, emphasizing kisspeptin’s potential to block metastasis in multiple organs, drastically reduce disease burden, extend patient lifespan, and improve responses to existing therapies.

Kisspeptin, Melatonin, and Tumor Growth: A Novel Connection

A fascinating link between kisspeptin, melatonin, and cancer emerged in early 2020. In an experiment, mice exposed to alternating cycles of daylight and darkness exhibited drastically different peptide levels: those in daylight had high kisspeptin and low melatonin, while mice in darkness showed the reverse. When injected with melanoma cells, daylight-exposed mice exhibited significantly higher tumor growth and volume, though metastasis was not measured[6]. These results suggest that melatonin and kisspeptin may interact to influence tumor suppression, though the exact nature of their relationship remains unclear. This highlights the complex physiological interplay through which kisspeptin may modulate tumor dynamics.

Studied Memory Enhancement

Certain kisspeptin analogues have been implicated in brain regions responsible for memory consolidation and 3-D spatial orientation. Research in mice indicates that administration of these peptides can reverse learning and navigational impairments caused by ethanol intoxication[7]. This suggests that kisspeptin and its analogues contribute to neuronal information encoding, making them promising candidates for addressing learning deficits associated with genetic disorders and chronic diseases. Although this research is in early stages, it broadens understanding of cognitive function and supports development of nootropics aimed at enhancing both healthy and impaired brain activity.

Impact on Mood and Behavior

Reproductive functions and emotions are deeply intertwined, and kisspeptin plays a role in both. To investigate this, a study administered kisspeptin versus placebo to 29 healthy heterosexual men, revealing that kisspeptin enhanced limbic brain activity. Participants exhibited increased reward-seeking behavior, heightened drive, and improved mood[8]. These findings suggest kisspeptin integrates sexual and emotional brain processing with reproductive function, offering insight into how mood, motivation, and drive are linked not only to sex but to broader aspects of human behavior.

Role in Kidney and Cardiovascular Function

Although primarily recognized for its role in reproduction, kisspeptin also plays important roles in kidney and cardiovascular health. Kisspeptin and its receptor are present in several kidney regions and are thought to influence kidney signaling and development. Studies in mice lacking the Kiss1 receptor indicate that kisspeptin is crucial for glomerular development, though whether this is a direct or indirect effect remains unclear[9].

Kisspeptin’s impact on the cardiovascular system likely relates to its effects on angiogenesis and vascular responses to injury. Research in mouse models suggests kisspeptin regulates vasoconstriction and cardiac output in specific vascular beds[9]. This vascular role may also underpin kisspeptin’s ability to inhibit tumor metastasis, given the importance of blood vessel growth and function in cancer progression. Further elucidation of kisspeptin’s vascular actions could accelerate its therapeutic applications.

Kisspeptin-10 Summary

Kisspeptin is a peptide primarily acting in the brain to regulate hormone secretion related to human reproduction. Its influence extends beyond reproduction, impacting testosterone levels, sex-related behaviors such as drive and motivation, and potentially mood and cognitive function.

For years, kisspeptin’s role in modulating cancer growth and metastasis has attracted scientific interest. While study results have varied, likely due to the peptide’s complex biological effects, kisspeptin’s influence on vascular growth and function offers a promising avenue for cancer treatment. Currently, kisspeptin is the focus of intensive research aimed at harnessing its versatile therapeutic potential.

Kisspeptin-10 demonstrates minimal to moderate side effects, with moderate oral and excellent subcutaneous bioavailability in mice; however, mouse dosing does not directly translate to humans. Commercially available kisspeptin-10 (e.g., from Peptide Sciences) is intended solely for educational and scientific research and is not approved for human consumption. Only licensed researchers should purchase this peptide.

Article Author

The above literature was researched, edited, and organized by Dr. E. Logan, M.D. Dr. Logan holds a medical doctorate from Case Western Reserve University School of Medicine and a B.S. degree in Molecular Biology.

Scientific Journal Author

Floriana Morgillo, M.D. is an Associate Professor of Medical Oncology at the University of Campania “Luigi Vanvitelli.” She earned her Medical Degree, cum laude, in 2000, completed her specialization in Medical Oncology in 2004 under Professor Fortunato Ciardiello, and obtained her PhD in Medical Oncology in 2008 at the same university. From 2004 to 2006, she worked at MD Anderson Cancer Center in the Thoracic Head and Neck Medical Department, focusing on acquired resistance to anti-EGFR targeted therapies in non-small cell lung cancer. In 2009, she received a Translational Research fellowship from ESMO. Dr. Morgillo serves as Principal Investigator and Sub-Investigator in numerous clinical trials and has co-authored various publications in prominent international journals, including research on the antitumor efficacy of Kisspeptin-10. She is referenced in citation [10].

Dr. Morgillo is recognized as a leading scientist in kisspeptin research and development. However, she does not endorse, advocate, or have any affiliation with the purchase, sale, or use of kisspeptin products. There is no relationship—implied or otherwise—between Dr. Morgillo and Peptide Sciences. The citation of Dr. Morgillo serves solely to credit her significant scientific contributions to the field.

References

1. W. S. Dhillo et al., “Kisspeptin-54 stimulates the hypothalamic-pituitary gonadal axis in human males,” J. Clin. Endocrinol. Metab., vol. 90, no. 12, pp. 6609–6615, Dec. 2005, doi: 10.1210/jc.2005-1468.
2. J. T. George et al., “Kisspeptin-10 is a potent stimulator of LH and increases pulse frequency in men,” J. Clin. Endocrinol. Metab., vol. 96, no. 8, pp. E1228-1236, Aug. 2011, doi: 10.1210/jc.2011-0089.
3. C. J. L. Harter, G. S. Kavanagh, and J. T. Smith, “The role of kisspeptin neurons in reproduction and metabolism,” J. Endocrinol., vol. 238, no. 3, pp. R173–R183, 2018, doi: 10.1530/JOE-18-0108.
4. E. J. Mead, J. J. Maguire, R. E. Kuc, and A. P. Davenport, “Kisspeptins: a multifunctional peptide system with a role in reproduction, cancer and the cardiovascular system,” Br. J. Pharmacol., vol. 151, no. 8, pp. 1143–1153, Aug. 2007, doi: 10.1038/sj.bjp.0707295.
5. T. Ly, S. Harihar, and D. R. Welch, “KISS1 in metastatic cancer research and treatment: potential and paradoxes,” Cancer Metastasis Rev., Mar. 2020, doi: 10.1007/s10555-020-09868-9.
6. P. Pazarci et al., “The effects of daylight exposure on melatonin levels, Kiss1 expression, and melanoma formation in mice,” Croat. Med. J., vol. 61, no. 1, pp. 55–61, Feb. 2020.
7. E. Gibula-Tarlowska and J. H. Kotlinska, “Kissorphin improves spatial memory and cognitive flexibility impairment induced by ethanol treatment in the Barnes maze task in rats,” Behav. Pharmacol., vol. 31, no. 2 & 3, pp. 272–282, Apr. 2020, doi: 10.1097/FBP.0000000000000557.
8. A. N. Comninos et al., “Kisspeptin modulates sexual and emotional brain processing in humans,” J. Clin. Invest., vol. 127, no. 2, pp. 709–719, doi: 10.1172/JCI89519.
9. M. Bhattacharya and A. V. Babwah, “Kisspeptin: Beyond the Brain,” Endocrinology, vol. 156, no. 4, pp. 1218–1227, Apr. 2015, doi: 10.1210/en.2014-1915.
10. Antitumor efficacy of Kisspeptin in human malignant mesothelioma cells. PubMed Central (PMC). https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5922395/

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