Kisspeptin
Kisspeptin-54 / Kisspeptin-10
Kisspeptin is a neuropeptide encoded by the KISS1 gene that plays a critical role in regulating the hypothalamic-pituitary-gonadal (HPG) axis. It stimulates gonadotropin-releasing hormone (GnRH) secretion by binding to the GPR54/Kiss1R receptor, making it essential for reproductive function, puberty onset, and fertility. Originally discovered as a metastasis suppressor in certain cancers, kisspeptin has emerged as a promising therapeutic target for reproductive disorders including infertility, hypothalamic amenorrhea, and hypoactive sexual desire disorder.
Clinical Benefits
Mechanism of Action
Kisspeptin exerts its effects by binding with high affinity to the G-protein coupled receptor GPR54 (also known as Kiss1R), which is predominantly expressed on GnRH neurons in the hypothalamus. Upon binding, it activates the Gq/11 signaling pathway, leading to increased intracellular calcium levels and phospholipase C activation. This cascade stimulates GnRH neurons to release GnRH into the hypothalamic-pituitary portal system, which subsequently binds to GnRH receptors on gonadotroph cells in the anterior pituitary. The result is pulsatile release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), which regulate gonadal steroidogenesis and gametogenesis. The kisspeptin/Kiss1R system serves as the master regulator of reproductive function and is essential for pubertal development and maintenance of fertility.
Proven Results
Medical Disclaimer
Kisspeptin is in Phase 2 clinical trials for reproductive applications. This information is for educational purposes only and should not be construed as medical advice. Any clinical use should occur only under medical supervision in approved research or clinical settings.