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

G. Mező, András Czajlik, Marilena Manea, Annamária Jakab, Viktor Farkas, Zs. Majer, E. Vass, A. Bodor, Bence Kapuvári, Mariann Boldizsár, B. Vincze, O. Csuka, Magdolna Kovács, Michael Przybylski, A. Perczel, F. Hudecz

Research output: Contribution to journalArticle

22 Citations (Scopus)

Abstract

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, 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 1H NMR.

Original languageEnglish
Pages (from-to)806-820
Number of pages15
JournalPeptides
Volume28
Issue number4
DOIs
Publication statusPublished - Apr 2007

Fingerprint

Petromyzon
Dimers
Derivatives
Disulfides
Conformations
gonadotropin-releasing hormone-III
Tumors
Cells
Nuclear magnetic resonance
Hormones

Keywords

  • Antitumor activity
  • Enzymatic stability
  • lGnRH-III dimer
  • Receptor binding
  • Structure

ASJC Scopus subject areas

  • Biochemistry
  • Endocrinology
  • Physiology
  • Cellular and Molecular Neuroscience

Cite this

Structure, enzymatic stability and antitumor activity of sea lamprey GnRH-III and its dimer derivatives. / Mező, G.; Czajlik, András; Manea, Marilena; Jakab, Annamária; Farkas, Viktor; Majer, Zs.; Vass, E.; Bodor, A.; Kapuvári, Bence; Boldizsár, Mariann; Vincze, B.; Csuka, O.; Kovács, Magdolna; Przybylski, Michael; Perczel, A.; Hudecz, F.

In: Peptides, Vol. 28, No. 4, 04.2007, p. 806-820.

Research output: Contribution to journalArticle

Mező, G. ; Czajlik, András ; Manea, Marilena ; Jakab, Annamária ; Farkas, Viktor ; Majer, Zs. ; Vass, E. ; Bodor, A. ; Kapuvári, Bence ; Boldizsár, Mariann ; Vincze, B. ; Csuka, O. ; Kovács, Magdolna ; Przybylski, Michael ; Perczel, A. ; Hudecz, F. / Structure, enzymatic stability and antitumor activity of sea lamprey GnRH-III and its dimer derivatives. In: Peptides. 2007 ; Vol. 28, No. 4. pp. 806-820.
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