lGnRH-III - a Promising Candidate for Anticancer Drug Development

Author(s): Marilena Manea, Gabor Mezo

Journal Name: Protein & Peptide Letters

Volume 20 , Issue 4 , 2013

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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.

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

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Article Details

Year: 2013
Published on: 18 February, 2013
Page: [439 - 449]
Pages: 11
DOI: 10.2174/0929866511320040008
Price: $65

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