Результаты исследований: Научные публикации в периодических изданиях › статья › Рецензирование
Synthesis of GnRH analogues and their application in targeted gene delivery systems. / Yablokova, T. V.; Chelushkin, P. S.; Dorosh, M. Yu; Efremov, A. M.; Orlov, S. V.; Burov, S. V.
в: Russian Journal of Bioorganic Chemistry, Том 38, № 1, 01.2012, стр. 22-29.Результаты исследований: Научные публикации в периодических изданиях › статья › Рецензирование
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TY - JOUR
T1 - Synthesis of GnRH analogues and their application in targeted gene delivery systems
AU - Yablokova, T. V.
AU - Chelushkin, P. S.
AU - Dorosh, M. Yu
AU - Efremov, A. M.
AU - Orlov, S. V.
AU - Burov, S. V.
N1 - Funding Information: ACKNOWLEDGMENTS The work was supported by the grant of the Minis try of Education and Science of the Russian Federa tion (State Contract no. 16.512.11.2052).
PY - 2012/1
Y1 - 2012/1
N2 - 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.
AB - 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.
KW - Antitumor activity
KW - GnRH
KW - Nuclear localization signal
KW - Suicide gene therapy
KW - Targeted gene delivery
UR - http://www.scopus.com/inward/record.url?scp=84861151348&partnerID=8YFLogxK
U2 - 10.1134/S1068162012010190
DO - 10.1134/S1068162012010190
M3 - Article
AN - SCOPUS:84861151348
VL - 38
SP - 22
EP - 29
JO - Russian Journal of Bioorganic Chemistry
JF - Russian Journal of Bioorganic Chemistry
SN - 1068-1620
IS - 1
ER -
ID: 86146771