Exploring and exploiting the host cell autophagy during Mycobacterium tuberculosis infection

Nagdev, Pavan Kumar; Agnivesh, Puja Kumari; Roy, Arnab; Sau, Shashikanta; Kalia, Nitin Pal

doi:10.1007/s10096-023-04663-0

Eur J Clin Microbiol Infect Dis

2023

DOI: 10.1007/s10096-023-04663-0

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Exploring and exploiting the host cell autophagy during Mycobacterium tuberculosis infection

Pavan Kumar Nagdev,

Puja Kumari Agnivesh,

Arnab Roy

et al.

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2024

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Cited by 3 publications

References 149 publications

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The hsa_circ_0002371/hsa-miR-502-5p/ATG16L1 axis modulates the survival of intracellular Mycobacterium tuberculosis and autophagy in macrophages

Zhang,

He,

Ruan

et al. 2024

Cellular Signalling

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The hsa_circ_0002371/hsa-miR-502-5p/ATG16L1 axis modulates the survival of intracellular Mycobacterium tuberculosis and autophagy in macrophages

Zhang,

He,

Ruan

et al. 2024

Cellular Signalling

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Review of research progress on different modalities of Macrophage death in Mycobacterium leprae infection

Jiang,

Zou,

Wang

2024

International Immunopharmacology

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2-Aryl-Benzoimidazoles as Type II NADH Dehydrogenase Inhibitors of Mycobacterium tuberculosis

Saha,

Sau,

Kalia

et al. 2024

ACS Infect. Dis.

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The nonproton pumping type II NADH dehydrogenase in Mycobacterium tuberculosis is essential for meeting the energy needs in terms of ATP under normal aerobic and stressful hypoxic environmental states. Type II NADH dehydrogenase conduits electrons into the electron transport chain in Mycobacterium tuberculosis, which results in ATP synthesis. Therefore, the inhibition of NDH-2 ensures the abolishment of the entire ATP synthesis machinery. Also, type II NADH dehydrogenase is absent in the mammalian genome, thus making it a potential target for antituberculosis drug discovery. Herein, we have screened a commercially available library of drug-like molecules and have identified a hit having a benzimidazole core moiety (6, H37Rv mc26230; minimum inhibitory concentration (MIC) = 16 μg/mL and ATP IC50 = 0.23 μg/mL) interfering with the oxidative phosphorylation pathway. Extensive medicinal chemistry optimization resulted in analogue 8, with MIC = 4 μg/mL and ATP IC50 = 0.05 μg/mL against the H37Rv mc26230 strain of Mycobacterium tuberculosis. Compounds 6 and 8 were found to be active against mono- and multidrug-resistant mycobacterium strains and demonstrated a bactericidal response. The Peredox-mCherry experiment and identification of single-nucleotide polymorphisms in mutants of CBR-5992 (a known type II NADH dehydrogenase inhibitor) were used to confirm the molecules as inhibitors of the type II NADH dehydrogenase enzyme. The safety index >10 for the test active molecules revealed the safety of test molecules.

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Exploring and exploiting the host cell autophagy during Mycobacterium tuberculosis infection

Cited by 3 publications

References 149 publications

The hsa_circ_0002371/hsa-miR-502-5p/ATG16L1 axis modulates the survival of intracellular Mycobacterium tuberculosis and autophagy in macrophages

The hsa_circ_0002371/hsa-miR-502-5p/ATG16L1 axis modulates the survival of intracellular Mycobacterium tuberculosis and autophagy in macrophages

Review of research progress on different modalities of Macrophage death in Mycobacterium leprae infection

2-Aryl-Benzoimidazoles as Type II NADH Dehydrogenase Inhibitors of Mycobacterium tuberculosis

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