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.
