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-Reference-Cited by-同舟云学术

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

Published:2022-04-09 Issue:8 Volume:27 Page:2433
ISSN:1420-3049
Container-title:Molecules
language:en
Short-container-title:Molecules

Author:

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

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.

Funder

Russian Foundation for Basic Research

Program of Fundamental Scientific Research of the State Academies of Sciences

Publisher

MDPI AG

Subject

Chemistry (miscellaneous),Analytical Chemistry,Organic Chemistry,Physical and Theoretical Chemistry,Molecular Medicine,Drug Discovery,Pharmaceutical Science

Link

https://www.mdpi.com/1420-3049/27/8/2433/pdf

Reference42 articles.

1. Drug chirality and its pharmacological consequences;Hutt,2005

2. [125I]N6-(3-iodo-4-hydroxyphenyl)isopropyladenosine: The use of the diastereomers as ligands for adenosine receptors in rat brain

3. Chiral recognition and determination of enantiomeric excess by mass spectrometry: A review

4. Recent Advances in Stereoselective Drug Targeting

5. Chiral discrimination in platinum anticancer drugs.

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