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

Autor:	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, Mikhail S. Drenichev
Jazyk:	angličtina
Rok vydání:	2022
Předmět:	nucleosides pentafuranose DNA repair tyrosyl-DNA phosphodiesterase 1 Tdp1 inhibition chirality Organic chemistry QD241-441
Zdroj:	Molecules, Vol 27, Iss 8, p 2433 (2022)
Druh dokumentu:	article
ISSN:	1420-3049
DOI:	10.3390/molecules27082433
Popis:	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.
Databáze:	Directory of Open Access Journals
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