Journal
PEPTIDES
Volume 28, Issue 4, Pages 806-820Publisher
ELSEVIER SCIENCE INC
DOI: 10.1016/j.peptides.2006.12.014
Keywords
lGnRH-III dimer; receptor binding; antitumor activity; enzymatic stability; structure
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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 H-1 NMR. (c) 2007 Elsevier Inc. All rights reserved.
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