Gonadorelin

Gonadorelin (GnRH) is a decapeptide that functions as a gonadotropin-releasing hormone agonist. It works by stimulating the synthesis and release of luteinizing hormone (LH) and follicle stimulating hormone (FSH). In clinical settings, it is used to address issues like infertility, menstrual cycle irregularities, and hypogonadism, and is employed diagnostically to assess pituitary function. Current research is investigating its therapeutic promise in breast and prostate cancer treatment and in managing Alzheimer's disease.

Gonadorelin Structure

• Formula: C55H75N17O13
• Molecular Weight: 1182.29 g/mol
• Sequence: pyroGlu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2

Gonadorelin Effects

Gonadorelin Research and Breast Cancer Prevention

• Risk Factor: High lifetime exposure to estrogen is linked to an increased risk of developing breast cancer. This includes factors like early menarche, late menopause, and the use of estrogen-containing hormone therapies.
• Mechanism: Gonadorelin is being studied for its ability to suppress ovarian estrogen production. This mechanism is proposed as an effective primary prevention strategy for estrogen-receptor-positive breast cancer in high-risk postmenopausal women.
• Efficacy: Research suggests this safe and cost-effective therapy could reduce breast cancer risk by up to 60% over 10 years and 70% over 15 years [1].
• Synergy: By reducing estrogen at the source, gonadorelin could enhance the efficacy and extend the usefulness of existing anti-estrogen, receptor-blocking medications [4], which often face resistance over time.
• Alternative Therapy: Investigations in postmenopausal women with hyperandrogenism demonstrated that gonadorelin use reduced hormonal levels without serious adverse effects, offering an alternative to estrogen replacement therapy.

Gonadorelin a Breakthrough in Prostate Cancer

• Sensitivity: Prostate cancer is highly hormone-sensitive, making hormonal suppression a key treatment. Historically, this involved surgical castration.
• Medical Castration: The application of GnRH in 1979 led to the concept of medical castration and the development of the highly effective Combined Androgen Blockade therapy (CAB).
• CAB Success: GnRH analogues are most effective when used in combination (CAB). Research from gonadorelin has led to the development of new, safe prostate cancer drugs. When combined with early detection, CAB makes it possible to cure 99% of all prostate cancer.

Gonadorelin May Reduce Dementia Risk

• Hormonal Link: Luteinizing hormone (LH) is shown to influence neurological function, particularly in the hippocampus (the brain's primary memory center). Decreased LH (associated with menopause) correlates with improved cognitive abilities in mice [9].
• Abeta Pathology: Elevated LH levels are linked to amyloid-beta (Abeta) pathology [10], which is characteristic of Alzheimer's. Reducing or eliminating LH has been shown in mouse models to alleviate Abeta accumulation and plaque [11].
• Selective Targeting: Since testosterone is beneficial for neural health in aging males, the ideal strategy is to maintain testosterone while reducing LH. Research is ongoing to see if gonadorelin derivatives can selectively interfere with LH secretion.
• Leuprolide Finding: Leuprolide (a GnRH analogue) has been observed to offer a decreased risk and greater protection against Alzheimer's compared to other analogues [12]. Its effectiveness stems from its ability to down-regulate LH via suppressing CAR effects, which is important given CAR's association with Alzheimer’s progression [13].
• Genetic Interaction: Current research is examining how gonadorelin analogues influence the interaction of APOE and MS4A4A genetic loci, both associated with Abeta plaques. The goal is to understand this compensatory relationship [14] to develop better diagnostic and preventive tests.

Gonadorelin Research

Gonadorelin is a relatively new peptide, but it is built upon decades of research into the function of Gonadotropin-releasing hormone (GnRH) and its analogues. This research has yielded significant advances, including a highly effective treatment for prostate cancer and promising leads in breast cancer prevention and Alzheimer's disease. Gonadorelin has minimal adverse effects and shows low oral but excellent subcutaneous bioavailability in mice. Mouse dosage per kilogram is not translatable to human dosage. Gonadorelin for human application remains restricted to educational and scientific exploration. Human consumption remains prohibited. Only licensed researchers may obtain Gonadorelin if they are accredited investigators.

Article Author

The referenced literature underwent research, compilation, and organization by Dr. Logan, M.D. Dr. Logan possesses a doctorate qualification from Case Western Reserve University School of Medicine alongside a B.S. in molecular biology.

Scientific Journal Author

Dr. Giorgio Secreto is a prominent figure currently studying at the IRCCS National Cancer Institute in Italy. He holds degrees in Medicine/Surgery and Endocrinology and served at the National Cancer Institute of Milan until 2010. His primary field of investigation is the role of androgens in breast cancer. He is recognized for his work on GnRH's effectiveness in reducing ovarian androgen levels.

Dr. Giorgio Secreto is acknowledged for his scientific contributions to Gonadorelin research. He does not endorse or promote the acquisition, distribution, or application of this compound for any purpose. No association, affiliation, or connection exists between Peptide Sciences and this researcher. This citation serves only to recognize his significant investigative and developmental contributions, as identified in references [1] and [3].

Referenced Citations

G. Secreto et al., "A novel approach to breast cancer prevention: reducing excessive ovarian androgen production in elderly women," Breast Cancer Res. Treat., vol. 158, no. 3, pp. 553–561, 2016. D. V. Spicer and M. C. Pike, "Sex steroids and breast cancer prevention," J. Natl. Cancer Inst. Monogr., no. 16, pp. 139–147, 1994. G. Secreto, P. Muti, M. Sant, E. Meneghini, and V. Krogh, "Medical ovariectomy in menopausal breast cancer patients with high testosterone levels: a further step toward tailored therapy," Endocr. Relat. Cancer, vol. 24, no. 11, pp. C21–C29, 2017. E. S. Volleard, A. P. van Beck, F. A. J. Verburg, A. Rozs, and J. A. Land, "Gonadotropin releasing hormone agonist treatment in premenopausal women with hyperandrogenism of ovarian origin," J. Clin. Endocrinol. Metab., vol. 96, no. 5, pp. 1197–1201, May 2011. F. Labrie, "Hormonal therapy of prostate cancer," Prog. Brain Res., vol. 182, pp. 321–341, 2010. F. Labrie, "GnRH agonists and the rapidly increasing use of combined androgen blockade in prostate cancer," Endocr. Relat. Cancer, vol. 21, no. 4, pp. R301–317, Aug. 2014. F. Labrie, "Combined blockade of testicular and locally made androgens in prostate cancer: a highly significant medical progress based upon intracrinology," J. Steroid Biochem. Mol. Biol., vol. 145, pp. 144–156, Jan. 2015. F. Labrie, "Keynote of endocrinology in the victory against prostate cancer," Bull. Cancer (Paris), vol. 93, no. 9, pp. 849–868, Sep. 2006. V. Burnham, C. Sundby, A. Laman-Maharg, and J. Thornton, "Luteinizing hormone acts at the hippocampus to dampen spatial memory," Horm. Behav., vol. 89, pp. 55–63, 2017. C. V. Rao, "Involvement of Luteinizing Hormone in Alzheimer Disease Development in Elderly Women," Reprod. Sci. Thousand Oaks Calif, vol. 24, no. 3, pp. 355–368, 2017. J. Lin et al., "Genetic ablation of luteinizing hormone receptor improves the amyloid pathology in a mouse model of Alzheimer disease," J. Neuropathol. Exp. Neurol., vol. 69, no. 3, pp. 253–261, Mar. 2010. R. L. Bowen, T. Butler, and C. S. Atwood, "Nad All Androgen Deprivation Therapies Are Created Equal: Leuprolide and the Decreased Risk of Developing Alzheimer's Disease," J. Clin. Oncol., vol. 34, no. 23, p. 2800, Aug. 2016. M. A. Smith, P. L. Bowen, R. O. Nguyen, G. Perry, C. S. Atwood, and A. A. Rimm, "Putative Gonadorelin Releasing Hormone Against Therapy and Dementia: An Application of Medicare Hospitalization Claims Data to PLA JAD, vol. 63, no. 4, pp. 1259–1277, 2018. A. Clelems, J. E. Vargas, and J. R. Gonzalez, "APOE and MS4A4A interact with GnRH signaling in Alzheimer's disease: Disrupting in mab and Alzheimer Dement. J. Alzheimers Assoc., vol. 13, no. 4, pp. 493–497, Apr. 2017.