Description
Leuprolide (leuprorelin) is a peptide analog of gonadotropin-releasing hormone (GnRH) that binds and activates the GnRH1 receptor. Leuprorelin modulates fertility by stimulating release of reproductive hormones. Leuprorelin also prevents stress-induced immunosuppression in animal models. Additionally, leuprorelin exhibits anticancer activity, inhibiting proliferation of prostate cancer cells in vitro. Leuprorelin also inhibits proliferation of endometrial cancer cells by suppressing expression of human telomerase reverse transcriptase (hTERT). In endometrial cells, leuprorelin induces apoptosis by increasing levels of Bax and FasL and decreasing levels of Bcl-2. Leuprorelin also exhibits anti-angiogenic activity, decreasing production of VEGF-A and IL-1β in endothelial cells.
References
Ko YH, Ha YR, Kim JW, et al. Silencing of the GnRH type 1 receptor blocks the antiproliferative effect of the GnRH agonist, leuprolide, on the androgen-independent prostate cancer cell line DU145. J Int Med Res. 2011;39(3):729-39. PMID: 21819703.
Tesone M, Bilotas M, Barañao RI, et al. The role of GnRH analogues in endometriosis-associated apoptosis and angiogenesis. Gynecol Obstet Invest. 2008;66 Suppl 1:10-8. PMID: 18936547.
Umathe SN, Dixit PV, Wanjari MM, et al. Leuprolide--a GnRH agonist--prevents restraint stress-induced immunosuppression via sex steroid-independent peripheral mechanism in mice. Int Immunopharmacol. 2008 Jan;8(1):71-9. PMID: 18068102.
Nagai N, Oshita T, Mukai K, et al. GnRH agonist inhibits human telomerase reverse transcriptase mRNA expression in endometrial cancer cells. Int J Mol Med. 2002 Nov;10(5):593-7. PMID: 12373298.
