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

Mező, Gábor; Czajlik, András; Manea, Marilena; Jakab, Annamaria; Farkas, Viktor; Majer, Zsuzsa; Vass, Elemer; Bodor, Andrea; Kapuvári, Bence; Boldizsar, Mariann; Vincze, Borbála; Csuka, Orsolya; Kovacs, Magdolna; Przybylski, Michael; Perczel, Andras; Hudecz, Ferenc

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

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Datum

2007

Autor:innen

Mező, Gábor

Czajlik, András

Manea, Marilena

Jakab, Annamaria

Farkas, Viktor

Majer, Zsuzsa

Vass, Elemer

Bodor, Andrea

Kapuvári, Bence

Boldizsar, Mariann

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Publikationstyp

Zeitschriftenartikel

Publikationsstatus

Published

Erschienen in

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.

Fachgebiet (DDC)

540 Chemie

Schlagwörter

lGnRH-III dimer, Receptor binding, Antitumor activity, Enzymatic stability, Structure, Gonadotropin-releasing-hormone, Cancer cell-growth, Analogs, Breast, Binding

Zitieren

ISO 690

MEZŐ, 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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Universitätsbibliographie

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