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

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.

• Authors: Marilena Manea, Gábor Mező
• Journal: Protein and peptide letters (Protein Pept Lett) Vol. 20 Issue 4 Pg. 439-49 (Apr 2013) ISSN: 1875-5305 [Electronic] Netherlands
• PMID: 23016589 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Review)

Chemical References

• Antineoplastic Agents
• Maleates
• gonadotropin-releasing hormone-III
• maleic acid-vinylpyrrolidone copolymer
• Gonadotropin-Releasing Hormone
• Povidone
• Pyrrolidonecarboxylic Acid

Topics

• Amino Acid Substitution
• Animals
• Antineoplastic Agents (chemistry, pharmacology)
• Drug Design
• Gonadotropin-Releasing Hormone (analogs & derivatives, chemistry, pharmacology)
• Humans
• Lampreys (metabolism)
• Maleates (chemistry, pharmacology)
• Petromyzon (metabolism)
• Povidone (analogs & derivatives, chemistry, pharmacology)
• Protein Multimerization
• Pyrrolidonecarboxylic Acid (analogs & derivatives, chemistry, pharmacology)