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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

Dyrkheeva, Nadezhda S. ; Chernyshova, Irina A. ; Ivanov, Georgy A. ; [et al.]

MDPI AG ; 2022

In: Molecules Vol. 27, No. 8 ( 2022-04-09), p. 2433-

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In: Molecules, MDPI AG, Vol. 27, No. 8 ( 2022-04-09), p. 2433-

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.

Type of Medium: Online Resource

ISSN: 1420-3049

URL: Article

DOI: 10.3390/molecules27082433

Language: English

Publisher: MDPI AG

Publication Date: 2022

detail.hit.zdb_id: 2008644-1