LGnRH-III - A promising candidate for anticancer drug development

Marilena Manea, Mezo Gbor

Research output: Contribution to journalArticle

9 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)439-449
Number of pages11
JournalProtein and Peptide Letters
Volume20
Issue number4
DOIs
Publication statusPublished - Apr 1 2013

Keywords

  • Anthracyclines
  • Anticancer activity
  • Lamprey gonadotropin-releasing hormone-iii (lgnrh-iii)
  • Peptide dimers drug - peptide conjugates
  • Targeted cancer chemotherapy

ASJC Scopus subject areas

  • Structural Biology
  • Biochemistry

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