Search for Inhibitors of Mycobacterium tuberculosis Transketolase in a Series of Sulfo-Substituted Compounds

As a result of the computer screening of a library of sulfo-substituted compounds, molecules capable of binding to the active site of transketolase from were identified. An experimental verification of the inhibitory activity of the most promising compound, STK045765, against a highly purified recom...

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Published inActanaturae Vol. 15; no. 2; pp. 81 - 83
Main Authors Gushchina, I V, Nilov, D K, Shcherbakova, T A, Baldin, S M, Švedas, V K
Format Journal Article
LanguageEnglish
Published Russia (Federation) A.I. Gordeyev 01.04.2023
Subjects
ischemia/reperfusion
reactivity
perfusion
microvascular density
mesenchymal stem cells
intravenous transplantation
brain
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Summary:As a result of the computer screening of a library of sulfo-substituted compounds, molecules capable of binding to the active site of transketolase from were identified. An experimental verification of the inhibitory activity of the most promising compound, STK045765, against a highly purified recombinant enzyme preparation was carried out. It was shown that the STK045765 molecule competes for the binding site of the pyrophosphate group of the thiamine diphosphate cofactor and, at a micromolar concentrations, is able to suppress the activity of mycobacterial transketolase. The discovered furansulfonate scaffold may serve as the basis for the creation of anti-tuberculosis drugs.
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ISSN:2075-8251
DOI:10.32607/actanaturae.15709