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

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2007
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Mező, Gábor
Czajlik, András
Jakab, Annamaria
Farkas, Viktor
Majer, Zsuzsa
Vass, Elemer
Bodor, Andrea
Kapuvári, Bence
Boldizsar, Mariann
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Peptides. 2007, 28(4), pp. 806-820. ISSN 0196-9781. Available under: doi: 10.1016/j.peptides.2006.12.014
Zusammenfassung

Direct antitumor activity of sea lamprey (Petromyzon marinus) gonadotropin-releasing hormone III (Glp-His-Trp-Ser-His-Asp-Trp-Lys-Pro-Gly-NH2; 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, IGnRH-III dimers were prepared via disulfide bond formation. Our results demonstrate that the IGnRH-III dimer derivatives exhibited higher antiproliferative effect and enzymatic stability in comparison with the native IGnRH-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.

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540 Chemie
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lGnRH-III dimer, Receptor binding, Antitumor activity, Enzymatic stability, Structure, Gonadotropin-releasing-hormone, Cancer cell-growth, Analogs, Breast, Binding
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ISO 690MEZŐ, Gábor, András CZAJLIK, Marilena MANEA, Annamaria JAKAB, Viktor FARKAS, Zsuzsa MAJER, Elemer VASS, Andrea BODOR, Bence KAPUVÁRI, Mariann BOLDIZSAR, Borbála VINCZE, Orsolya CSUKA, Magdolna KOVACS, Michael PRZYBYLSKI, Andras PERCZEL, Ferenc HUDECZ, 2007. Structure, enzymatic stability and antitumor activity of sea lamprey GnRH-III and its dimer derivatives. In: Peptides. 2007, 28(4), pp. 806-820. ISSN 0196-9781. Available under: doi: 10.1016/j.peptides.2006.12.014
BibTex
@article{Mezo2007-04Struc-17246,
  year={2007},
  doi={10.1016/j.peptides.2006.12.014},
  title={Structure, enzymatic stability and antitumor activity of sea lamprey GnRH-III and its dimer derivatives},
  number={4},
  volume={28},
  issn={0196-9781},
  journal={Peptides},
  pages={806--820},
  author={Mező, Gábor and Czajlik, András and Manea, Marilena and Jakab, Annamaria and Farkas, Viktor and Majer, Zsuzsa and Vass, Elemer and Bodor, Andrea and Kapuvári, Bence and Boldizsar, Mariann and Vincze, Borbála and Csuka, Orsolya and Kovacs, Magdolna and Przybylski, Michael and Perczel, Andras and Hudecz, Ferenc}
}
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