Synthesis of GnRH analogues and their application in targeted gene delivery systems |
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Authors: | T V Yablokova P S Chelushkin M Yu Dorosh A M Efremov S V Orlov S V Burov |
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Institution: | 1.Institute of Macromolecular Compounds,Russian Academy of Sciences,St. Petersburg,Russia;2.Institute of Experimental Medicine,Russian Academy of Medical Sciences,Moscow,Russia |
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Abstract: | A set of GnRH analogues containing the nuclear localization signal (NLS) of the SV-40 virus was synthesized using solid phase
peptide synthesis and chemical ligation techniques. Selective chemical ligation was achieved through hydrazone formation upon
the interaction of NLS hydrazide and GnRH analogue modified with pyruvic acid. The efficiency of the synthesized compounds
was demonstrated in experiments on transfection of various human cancer cell lines with reporter luciferase and β-galactosidase
genes, as well as suicide thymidine kinase gene of HSV-1. Selectivity of the peptide-DNA complex effect on cancer cells is
achieved as a result of its penetration through the cell membrane via GnRH receptor-mediated endocytosis pathway. |
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