lGnRH-III - a Promising Candidate for Anticancer Drug Development

Title:lGnRH-III - a Promising Candidate for Anticancer Drug Development

Volume: 20 Issue: 4

Author(s): Marilena Manea and Gabor Mezo

Affiliation:

Keywords: Lamprey gonadotropin-releasing hormone-III (lGnRH-III), anticancer activity, targeted cancer chemotherapy, anthracyclines, peptide dimers, drug - peptide conjugates, antiproliferative effect, chemotherapeutic agent, tumor, steroid

Abstract: Lamprey gonadotropin-releasing hormone-III (lGnRH-III; Glp-His-Trp-Ser-His-Asp-Trp-Lys-Pro-Gly-NH2), a native isoform of human GnRH (GnRH-I), was initially isolated from the brain of the sea lamprey (Petromyzon marinus). It is a weak GnRH agonist, which exerts a direct antiproliferative effect on cancer cells and has an insignificant LH and FSH releasing potency in mammals. These features reveal the advantages of lGnRH-III and its derivatives for use in cancer therapy. Here we give an overview of various strategies to increase the antitumor activity of lGnRH-III, such as amino acid replacement, cyclization, dimerization and conjugation to polymers or to chemotherapeutic agents. In vitro and in vivo antitumor activity of lGnRH-III based compounds was demonstrated both on hormone dependent and independent tumors.

Cite this article as:

Manea Marilena and Mezo Gabor, lGnRH-III - a Promising Candidate for Anticancer Drug Development, Protein & Peptide Letters 2013; 20 (4) . https://dx.doi.org/10.2174/0929866511320040008