Synthesis, characterization and in vitro activity of thrombin-binding DNA aptamers with triazole internucleotide linkages
Anna Varizhuk
1
,
Olga N Tatarinova
1
,
Dmitry Kaluzhny
3
,
Vladimir L Florentiev
3
,
Edward N. Timofeev
3
,
A.K. SHCHYOLKINA
3
,
Olga F Borisova
3
,
Igor P. Smirnov
1
,
Sergei L Grokhovsky
3
,
Anton V Aseychev
1
,
Galina Pozmogova
1
Publication type: Journal Article
Publication date: 2013-09-01
scimago Q1
wos Q1
SJR: 1.142
CiteScore: 11.3
Impact factor: 5.9
ISSN: 02235234, 17683254
PubMed ID:
23850569
Organic Chemistry
Drug Discovery
General Medicine
Pharmacology
Abstract
A series of DNA aptamers bearing triazole internucleotide linkages that bind to thrombin was synthesized. The novel aptamers are structurally analogous to the well-known thrombin-inhibiting G-quadruplexes TBA15 and TBA31. The secondary structure stability, binding affinity for thrombin and anticoagulant effects of the triazole-modified aptamers were measured. A modification in the central loop of the aptamer quadruplex resulted in increased nuclease resistance and an inhibition efficiency similar to that of TBA15. The likely aptamer-thrombin binding mode was determined by molecular dynamics simulations. Due to their relatively high activity and the increased resistance to nuclease digestion imparted by the triazole internucleotide linkages, the novel aptamers are a promising alternative to known DNA-based anticoagulant agents.
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51
Total citations:
51
Citations from 2024:
6
(11.76%)
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GOST
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Varizhuk A. et al. Synthesis, characterization and in vitro activity of thrombin-binding DNA aptamers with triazole internucleotide linkages // European Journal of Medicinal Chemistry. 2013. Vol. 67. pp. 90-97.
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Varizhuk A., Tsvetkov V. B., Tatarinova O. N., Kaluzhny D., Florentiev V. L., Timofeev E. N., SHCHYOLKINA A., Borisova O. F., Smirnov I. P., Grokhovsky S. L., Aseychev A. V., Pozmogova G. Synthesis, characterization and in vitro activity of thrombin-binding DNA aptamers with triazole internucleotide linkages // European Journal of Medicinal Chemistry. 2013. Vol. 67. pp. 90-97.
Cite this
RIS
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TY - JOUR
DO - 10.1016/j.ejmech.2013.06.034
UR - https://doi.org/10.1016/j.ejmech.2013.06.034
TI - Synthesis, characterization and in vitro activity of thrombin-binding DNA aptamers with triazole internucleotide linkages
T2 - European Journal of Medicinal Chemistry
AU - Varizhuk, Anna
AU - Tsvetkov, Vladimir B.
AU - Tatarinova, Olga N
AU - Kaluzhny, Dmitry
AU - Florentiev, Vladimir L
AU - Timofeev, Edward N.
AU - SHCHYOLKINA, A.K.
AU - Borisova, Olga F
AU - Smirnov, Igor P.
AU - Grokhovsky, Sergei L
AU - Aseychev, Anton V
AU - Pozmogova, Galina
PY - 2013
DA - 2013/09/01
PB - Elsevier
SP - 90-97
VL - 67
PMID - 23850569
SN - 0223-5234
SN - 1768-3254
ER -
Cite this
BibTex (up to 50 authors)
Copy
@article{2013_Varizhuk,
author = {Anna Varizhuk and Vladimir B. Tsvetkov and Olga N Tatarinova and Dmitry Kaluzhny and Vladimir L Florentiev and Edward N. Timofeev and A.K. SHCHYOLKINA and Olga F Borisova and Igor P. Smirnov and Sergei L Grokhovsky and Anton V Aseychev and Galina Pozmogova},
title = {Synthesis, characterization and in vitro activity of thrombin-binding DNA aptamers with triazole internucleotide linkages},
journal = {European Journal of Medicinal Chemistry},
year = {2013},
volume = {67},
publisher = {Elsevier},
month = {sep},
url = {https://doi.org/10.1016/j.ejmech.2013.06.034},
pages = {90--97},
doi = {10.1016/j.ejmech.2013.06.034}
}
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