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Peptides. 2007 Apr;28(4):806-20. Epub 2007 Jan 4.

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

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  • 1Research Group of Peptide Chemistry, Hungarian Academy of Sciences, Eötvös L. University, POB 32, 1518 Budapest 112, Hungary. gmezo@elte.hu

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.

PMID:
17254668
[PubMed - indexed for MEDLINE]
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