Abstract 1804 Identification of Small Molecule Inhibitors of Mycobacterium tuberculosis Topoisomerase I by Machine Learning and In vitro assays

Background: DNA topoisomerases play critical roles during cell proliferation and survival in stress response by managing DNA topology and overcoming topological barriers. They are important drug targets for bacterial infection and cancer treatments. Bacterial topoisomerase I belonging to the type IA subfamily is essential for cell viability in many bacterial pathogens including Mycobacterium tuberculosis. Small molecule inhibitors of Mycobacterium tuberculosis topoisomerase I may interact with both DNA and enzyme or may interfere with the binding of Mg+2 required for catalysis at the active site of the enzyme.

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Journal
Journal of Biological Chemistry
Published
2025-05-01
DOI
https://doi.org/10.1016/j.jbc.2025.109042
Primary Topic
Tuberculosis Research and Epidemiology
Type
article
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article

Abstract 1804 Identification of Small Molecule Inhibitors of Mycobacterium tuberculosis Topoisomerase I by Machine Learning and In vitro assays

Yuk‐Ching Tse‐Dinh, Somaia Haque Chadni
Journal of Biological Chemistry
Tuberculosis Research and Epidemiology
article

Abstract 1804 Identification of Small Molecule Inhibitors of Mycobacterium tuberculosis Topoisomerase I by Machine Learning and In vitro assays

Yuk‐Ching Tse‐Dinh, Somaia Haque Chadni
article en

Abstract

Background: DNA topoisomerases play critical roles during cell proliferation and survival in stress response by managing DNA topology and overcoming topological barriers. They are important drug targets for bacterial infection and cancer treatments. Bacterial topoisomerase I belonging to the type IA subfamily is essential for cell viability in many bacterial pathogens including Mycobacterium tuberculosis. Small molecule inhibitors of Mycobacterium tuberculosis topoisomerase I may interact with both DNA and enzyme or may interfere with the binding of Mg+2 required for catalysis at the active site of the enzyme.

Journal of Biological ChemistryVol. 301(5)
International University (KH)
Good health and well-being
Openalex Percentile: Top 83%
Tuberculosis Research and Epidemiology
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