Abstract 2610 Modified Carbapenem Derivatives exhibit Potential Inhibition against Mycobacterium tuberculosis Peptidoglycan Synthesis

Background: The burden of Tuberculosis (TB), has regained its position as the leading cause of death from a single infectious agent, Mycobacterium tuberculosis (Mtb) after COVID-19. Peptidoglycan synthesis is an underexplored drug target in Mtb treatment. Carbapenems are effective against TB as they are poor substrates for the Mtb β-lactamase BlaC and inhibit L, D-transpeptidases (LDTs), key β-lactam resistance mechanisms in Mtb. We hypothesize that substituting the C5α position and modifying the R2-side chain enhances carbapenem activity against Mtb.

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Publication Details

Journal
Journal of Biological Chemistry
Published
2025-05-01
DOI
https://doi.org/10.1016/j.jbc.2025.109076
Primary Topic
Cancer therapeutics and mechanisms
Type
article
Field-Weighted Citation Impact
0.00
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Abstract 2610 Modified Carbapenem Derivatives exhibit Potential Inhibition against Mycobacterium tuberculosis Peptidoglycan Synthesis

Robert A. Bonomo, David C. Nguyen, Eunjeong Shin, John D. Buynak et al.
Journal of Biological Chemistry
Cancer therapeutics and mechanisms
article

Abstract 2610 Modified Carbapenem Derivatives exhibit Potential Inhibition against Mycobacterium tuberculosis Peptidoglycan Synthesis

Robert A. Bonomo, David C. Nguyen, Eunjeong Shin, John D. Buynak, Magdalena A. Taracila, Khalid M Dousa, Mary Nantongo, Henry W. Boom, Christopher R. Bethel
article en

Abstract

Background: The burden of Tuberculosis (TB), has regained its position as the leading cause of death from a single infectious agent, Mycobacterium tuberculosis (Mtb) after COVID-19. Peptidoglycan synthesis is an underexplored drug target in Mtb treatment. Carbapenems are effective against TB as they are poor substrates for the Mtb β-lactamase BlaC and inhibit L, D-transpeptidases (LDTs), key β-lactam resistance mechanisms in Mtb. We hypothesize that substituting the C5α position and modifying the R2-side chain enhances carbapenem activity against Mtb.

Journal of Biological ChemistryVol. 301(5)
Case Western Reserve University (US)
Zero hunger
Openalex Percentile: Top 88%
Cancer therapeutics and mechanisms
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