title: 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.affiliation: Research Group of Peptide Chemistry, Hungarian Academy of Sciences, Eotvos L. University, 1117 Budapest, Pazmany P. stny. 1/A, Hungary. gmezo@elte.hu.
authors.forename: Marilena
authors.initials: M
authors.lastname: Manea
authors.forename: Gábor
authors.initials: G
authors.lastname: Mező
mesh_terms: D019943:Amino Acid Substitution; D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D015195:Drug Design; D007987:Gonadotropin-Releasing Hormone / Q000031:analogs & derivatives / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D007798:Lampreys / Q000378:metabolism; D008298:Maleates / Q000737:chemistry / Q000494:pharmacology; D048428:Petromyzon / Q000378:metabolism; D011205:Povidone / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology; D055503:Protein Multimerization; D011761:Pyrrolidonecarboxylic Acid / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D008298:Maleates; C448022:gonadotropin-releasing hormone-III; C114335:maleic acid-vinylpyrrolidone copolymer; D007987:Gonadotropin-Releasing Hormone; D011205:Povidone; D011761:Pyrrolidonecarboxylic Acid