1. Academic Validation
  2. lGnRH-III -- a promising candidate for anticancer drug development

lGnRH-III -- a promising candidate for anticancer drug development

  • Protein Pept Lett. 2013 Apr;20(4):439-49.
Marilena Manea 1 Gábor Mező
Affiliations

Affiliation

  • 1 Research Group of Peptide Chemistry, Hungarian Academy of Sciences, Eotvos L. University, 1117 Budapest, Pazmany P. stny. 1/A, Hungary. gmezo@elte.hu.
PMID: 23016589
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.

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