lGnRH-III - a Promising Candidate for Anticancer Drug Development

Manea, Marilena and Mező, Gábor (2013) lGnRH-III - a Promising Candidate for Anticancer Drug Development. Protein and Peptide Letters, 20 (4). pp. 439-449. ISSN ISSN: 1875-5305 (Online), ISSN: 0929-8665 (Print)

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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 can-cer 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 vitroand in vivoantitumor activity of lGnRH-III based compounds was demonstrated both on hormone dependent and independent tumors.

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