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2 results on '"pentafuranose"'

1. In Vitro and In Silico Studies of Human Tyrosyl-DNA Phosphodiesterase 1 (Tdp1) Inhibition by Stereoisomeric Forms of Lipophilic Nucleosides: The Role of Carbohydrate Stereochemistry in Ligand-Enzyme Interactions.

Author

Dyrkheeva, Nadezhda S., Chernyshova, Irina A., Ivanov, Georgy A., Porozov, Yuri B., Zenchenko, Anastasia A., Oslovsky, Vladimir E., Zakharenko, Alexandra L., Nasyrova, Darina I., Likhatskaya, Galina N., Mikhailov, Sergey N., Lavrik, Olga I., and Drenichev, Mikhail S.

Subjects
*NUCLEOSIDES, *DNA ligases, *STEREOCHEMISTRY, *CARBOHYDRATES, *NUCLEOSIDE derivatives, *URIDINE
Abstract

Inhibition of human DNA repair enzyme tyrosyl-DNA phosphodiesterase 1 (Tdp1) by different chiral lipophilic nucleoside derivatives was studied. New Tdp1 inhibitors were found in the series of the studied compounds with IC50 = 2.7–6.7 μM. It was shown that D-lipophilic nucleoside derivatives manifested higher inhibition activity than their L-analogs, and configuration of the carbohydrate moiety can influence the mechanism of Tdp1 inhibition. [ABSTRACT FROM AUTHOR]

Published
2022
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2. In Vitro and In Silico Studies of Human Tyrosyl-DNA Phosphodiesterase 1 (Tdp1) Inhibition by Stereoisomeric Forms of Lipophilic Nucleosides: The Role of Carbohydrate Stereochemistry in Ligand-Enzyme Interactions

Author

Nadezhda S. Dyrkheeva, Irina A. Chernyshova, Georgy A. Ivanov, Yuri B. Porozov, Anastasia A. Zenchenko, Vladimir E. Oslovsky, Alexandra L. Zakharenko, Darina I. Nasyrova, Galina N. Likhatskaya, Sergey N. Mikhailov, Olga I. Lavrik, and Mikhail S. Drenichev

Subjects
nucleosides, pentafuranose, DNA repair, tyrosyl-DNA phosphodiesterase 1, Tdp1 inhibition, chirality, Organic chemistry, QD241-441
Abstract

Inhibition of human DNA repair enzyme tyrosyl-DNA phosphodiesterase 1 (Tdp1) by different chiral lipophilic nucleoside derivatives was studied. New Tdp1 inhibitors were found in the series of the studied compounds with IC50 = 2.7–6.7 μM. It was shown that D-lipophilic nucleoside derivatives manifested higher inhibition activity than their L-analogs, and configuration of the carbohydrate moiety can influence the mechanism of Tdp1 inhibition.

Published
2022
Full Text
View/download PDF

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