Structure, enzymatic stability and antitumor activity of sea lamprey GnRH-III and its dimer derivatives.

Abstract	Direct antitumor activity of sea lamprey (Petromyzon marinus) gonadotropin-releasing hormone III (Glp-His-Trp-Ser-His-Asp-Trp-Lys-Pro-Gly-NH(2); lGnRH-III) was described on several tumor cells. To improve the selectivity of antitumor effects without increasing the hormone releasing activity and to enhance the enzymatic stability, lGnRH-III dimers were prepared via disulfide bond formation. Our results demonstrate that the lGnRH-III dimer derivatives exhibited higher antiproliferative effect and enzymatic stability in comparison with the native lGnRH-III, while lower LH-releasing potency was determined. In order to find a correlation between the biological and structural features of these compounds, the conformation of lGnRH-III and its dimer derivatives was determined by ECD, VCD, FT-IR and (1)H NMR.
Authors	Gábor Mezo, András Czajlik, Marilena Manea, Annamária Jakab, Viktor Farkas, Zsuzsa Majer, Elemér Vass, Andrea Bodor, Bence Kapuvári, Mariann Boldizsár, Borbála Vincze, Orsolya Csuka, Magdolna Kovács, Michael Przybylski, András Perczel, Ferenc Hudecz
Journal	Peptides (Peptides) Vol. 28 Issue 4 Pg. 806-20 (Apr 2007) ISSN: 0196-9781 [Print] United States
PMID	17254668 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References	Antineoplastic Agents Oligopeptides gonadotropin-releasing hormone-III Gonadotropin-Releasing Hormone Chymotrypsin Pyrrolidonecarboxylic Acid
Topics	Amino Acid Sequence Animals Antineoplastic Agents (chemistry, metabolism, pharmacology) Blotting, Western Cell Line, Tumor Cell Proliferation (drug effects) Cells, Cultured Chromatography, High Pressure Liquid Chymotrypsin (metabolism) Circular Dichroism Computer Simulation Dimerization Enzyme Stability Gonadotropin-Releasing Hormone (chemistry, metabolism, pharmacology) Humans Lampreys (metabolism) Magnetic Resonance Spectroscopy Models, Chemical Molecular Sequence Data Oligopeptides (chemistry, metabolism, pharmacology) Protein Binding Pyrrolidonecarboxylic Acid (analogs & derivatives, chemistry, metabolism, pharmacology) Rats Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization Spectroscopy, Fourier Transform Infrared

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