Kisspeptin-10 5mg

Description

Kisspeptin: A History and Overview

Kisspeptin, a peptide encoded by the KISS1 gene, has emerged as a critical regulator of reproductive function, acting as a master regulator of the hypothalamic-pituitary-gonadal (HPG) axis. Initially identified for its role in suppressing metastasis in malignant melanomas, kisspeptin’s pivotal role in controlling gonadotropin-releasing hormone (GnRH) secretion, and thereby influencing puberty onset and fertility, has garnered significant attention in the fields of endocrinology and reproductive medicine.

Kisspeptin-10 Chemical Composition

• Chemical Structure: Kisspeptin-10 is a short peptide consisting of 10 amino acids, with the sequence Tyr-Asn-Trp-Asn-Ser-Phe-Gly-Leu-Arg-Phe-NH2, representing the active core of the larger kisspeptin molecule.
• Molecular Formula: The molecular formula for Kisspeptin-10 is C59H83N17O14, indicating its composition of carbon, hydrogen, nitrogen, oxygen, and sulfur atoms.
• Stability: Kisspeptin-10 is relatively stable at -20°C when stored in lyophilized form. Reconstitution with sterile water or a suitable buffer followed by refrigeration is recommended for short-term use.
• Solubility: It is soluble in water and aqueous buffers, making it suitable for experimental and therapeutic injections.
• Mechanism of Action: Kisspeptin-10 exerts its effects by binding to the G-protein-coupled receptor known as GPR54 (or KISS1R). This interaction stimulates the secretion of gonadotropin-releasing hormone (GnRH) from the hypothalamus, which in turn regulates the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) from the pituitary gland, crucial for reproductive function.
• Therapeutic Use: Research has focused on its potential in treating reproductive disorders, including hypothalamic amenorrhea and infertility, by exploiting its ability to stimulate the HPG axis. It is also being investigated for its role in suppressing metastasis in certain cancers.
• Efficacy: Clinical trials have demonstrated that administration of Kisspeptin-10 can effectively increase levels of LH and FSH, indicating its potential utility in treating disorders of the reproductive system.
• Side Effects: As of the last update, kisspeptin-10 is considered to have a favorable safety profile, with minimal side effects reported in human studies. However, further research is needed to fully understand its long-term safety.
• Safety Profile: Preliminary clinical studies suggest kisspeptin-10 is safe and well-tolerated in humans, with no significant adverse effects reported at therapeutic doses.
• Legal Status and Availability: Kisspeptin-10 is primarily available for research purposes and is not yet approved by regulatory agencies like the FDA for clinical use. Its use in humans is limited to clinical trials.
• Shelf Life: 36 months
• Appearance: White lipolyzed powder puck.

Kisspeptin and Puberty

Kisspeptin plays a crucial role in the initiation of puberty. Its interaction with the G protein-coupled receptor, GPR54 (also known as KISS1R), on GnRH neurons, triggers a cascade of hormonal events leading to the release of GnRH, which in turn stimulates the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) from the pituitary gland. This hormonal release is essential for the development of secondary sexual characteristics and the maturation of gonads. Mutations in the KISS1 or GPR54 genes have been linked to pubertal disorders, including precocious puberty and hypogonadotropic hypogonadism, underscoring the importance of kisspeptin in sexual maturation (de Roux et al., 2003; Seminara et al., 2003).

Kisspeptin and Fertility

Beyond puberty, kisspeptin is integral to reproductive health and fertility. In adults, it regulates the menstrual cycle and ovulation by modulating the release of GnRH in response to external and internal cues, including hormonal signals and environmental factors. The administration of kisspeptin has been shown to trigger LH surges in women, offering promising therapeutic potential for treating infertility, especially in cases of hypothalamic amenorrhea where GnRH production is insufficient (Jayasena et al., 2014).

Therapeutic Applications

The therapeutic applications of kisspeptin extend beyond fertility treatments. Its role in mediating metabolic interactions and appetite suggests potential uses in addressing obesity and metabolic syndrome. Moreover, given its initial discovery as a metastasis suppressor, ongoing research investigates its role in cancer biology, with the hope of developing novel anticancer therapies targeting the KISS1 signaling pathway.

Conclusion

Kisspeptin represents a seminal discovery in the field of reproductive biology, offering insights into the fundamental mechanisms underlying puberty, fertility, and possibly cancer metastasis. Its role as a gatekeeper of reproductive function underscores the complexity of hormonal regulation and highlights the potential for novel therapeutic interventions targeting the kisspeptin-GPR54 signaling axis. As research progresses, the therapeutic potential of kisspeptin continues to expand, promising new avenues for treating a variety of conditions related to reproductive health, metabolism, and cancer.

Referenced Citations

1. Modulations of human resting brain connectivity by kisspeptin enhance sexual and emotional functions – This study explored how kisspeptin can affect brain connectivity related to sexual and emotional functions. (https://dx.doi.org/10.1172/jci.insight.121958)
2. Kisspeptin enhances brain responses to olfactory and visual cues of attraction in men – Research indicating kisspeptin’s role in enhancing responses to attraction cues in men.
   (https://dx.doi.org/10.1172/jci.insight.133633)
3. Kisspeptin and the control of emotions, mood, and reproductive behaviour – This study discusses kisspeptin’s impact on emotions, mood, and reproductive behaviors.(https://dx.doi.org/10.1530/JOE-18-0269)
4. The metabolic regulation of kisspeptin and the link between energy balance and reproduction – A review focusing on how kisspeptin links reproductive function with energy balance. (https://www.nature.com/articles/nrendo.2010.117)
5. Advances in clinical applications of kisspeptin-GnRH pathway in female reproduction – Examines kisspeptin’s role in LH pulse modulation and its implications for female reproductive health.
   (https://rbej.biomedcentral.com/articles/10.1186/s12958-020-00652-6)
6. Kisspeptin signalling in the physiology and pathophysiology of the urogenital system – Discusses kisspeptin’s potential role in the diagnosis and prognosis of urogenital system cancers. (https://www.nature.com/articles/nrurol.2011.76)
7. Potential roles for the kisspeptin/kisspeptin receptor system in implantation and placentation – A review highlighting kisspeptin’s potential impact on reproductive processes like implantation and placentation. (https://doi.org/10.1093/humupd/dmy046)
8. Complete Kisspeptin Receptor Inactivation Does Not Impede Exogenous GnRH-Induced LH Surge in Humans – Investigates the effects of kisspeptin receptor inactivation on LH surge, providing insights into its role in human reproductive physiology. (https://doi.org/10.1210/jc.2018-00410)
9. Kisspeptin modulates gamma-aminobutyric acid levels in the human brain – This study explores how kisspeptin affects GABA levels, indicating its broader neuroendocrine roles.
   (https://pubmed.ncbi.nlm.nih.gov/30649364/)
10. Kisspeptin-10 Is a Potent Stimulator of LH and Increases Pulse Frequency in Men – A detailed study on kisspeptin-10’s effects on LH, FSH, and testosterone, suggesting therapeutic applications in reproductive health. (https://academic.oup.com/jcem/article/95/11/4855/2596344)