GnRH receptor-mediated gene therapy of gynecological cancers

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Group Leaders: Prof. Dr. rer. nat. Carsten Gründker and Prof. Dr. med. Günter Emons

The majority of ovarian (>80%) and endometrial (>80%) cancers express GnRH receptors. Apart from reproductive organs (ovary, fallopian tube, uterus) that are normally removed during surgical therapy of ovarian or endometrial cancer, other organs and hematopoetic stem cells do not express GnRH receptors. In addition, a tumor specific signal transduction exists in the tumor cells, which is basically different of the classical GnRH receptor signal transduction, known to operate in the pituitary gonadotrophs. We have recently shown specific activation of nucleus factor kappa B (NFkB) in ovarian and endometrial cancers after treatment with GnRH. These properties of GnRH would make it an ideal candidate to induce the expression of a therapeutic gene in GnRH-receptor positive tumors. Based on these findings we have developed a novel gene therapy concept using the tumor specific GnRH receptor signal transduction pathway.
In this study we could demonstrate that GnRH agonist-induced activation of different reporter genes via NFkB promotor was restricted to GnRH receptor-positive cancer cell lines. Using the reporter gene LacZ, the concept of gene therapy via GnRH receptor dependent tumor specific signal transduction pathway was successfully tested in nude mice bearing xenografts of human ovarian or endometrial cancers. The GnRH receptor-positive tumors as well as the reproductive organs exclusively showed activation of LacZ. All other organs did not show any activation of LacZ. Using Herpes Simplex thymidine kinase as therapeutic gene, Ganciclovir as pro-drug and GnRH agonist Triptorelin as inductor we could demonstrate specific killing of GnRH receptor-positive cancer cells in vitro. No effects were observed on GnRH-receptor negative cells. Because of the different GnRH receptor signal transduction no toxic effects could as well be observed in the GnRH receptor-positive pituitary gonadotrophs. In the meantime, the Proof-Of Principle could be demonstrated in vivo on tumor-bearing nude mice. The tumor volume of the gene therapy given mice was significantly lower than with the control animals. Toxic side effects were not observed.

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