ArticleAngewandte Chemie (International ed. in English)2018
An Antibacterial β-Lactone Kills Mycobacterium tuberculosis by Disrupting Mycolic Acid Biosynthesis.
Article in Angewandte Chemie (International ed. in English), 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 36 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
36 citing papers in PubMed, 71 citations in OpenAlex.
- ClpC1-dependent iron homeostasis underlies mycobacterial defense against oxygen-driven Fenton reaction during reactivation.Microbiology spectrum · 2026Article
- Description and Comparative Genomic Analysis of Salipiger Bruguierae sp. nov., a Novel Member of the Family Roseobacteraceae Isolated from Mangrove Sediments.Current microbiology · 2026Article
- Key Proteins and Enzymatic Mechanisms Underlying Drug Resistance in Mycobacterium tuberculosis.Advances in experimental medicine and biology · 2026Review
- Synthesis and evaluation ofSynlett : accounts and rapid communications in synthetic organic chemistry · 2025Article
- Intercepting a Mycobacterial Biosynthetic Pathway with Covalent Labeling.Journal of the American Chemical Society · 2025Article
- Structure-based Virtual Screening and Hit Identification of Novel designed Quinazolin-4(3H)-one Derivatives as Antitubercular Agent against TargetsCurrent drug discovery technologies · 2025Article
- Cryo-electron microscopy structure of the di-domain core ofMicrobiology (Reading, England) · 2024Article
- Aqueous extract-mediated green synthesis of CuO nanoparticles: Potential anti-tuberculosis agents.Food science & nutrition · 2024Article
- Polyketide Synthase 13 (Pks13) Inhibition: A Potential Target for New Class of Anti-tubercular Agents.Current topics in medicinal chemistry · 2024Review
- Anti-biofilm potential of human senescence marker protein 30 against Mycobacterium smegmatis.World journal of microbiology & biotechnology · 2023Article
- Review
- Target Identification in Anti-Tuberculosis Drug Discovery.International journal of molecular sciences · 2023Review
- Chemical approaches to unraveling the biology of mycobacteria.Cell chemical biology · 2023Review
- Therapeutic potential of coumestan Pks13 inhibitors for tuberculosis.Antimicrobial agents and chemotherapy · 2023Article
- An integrated computational approach towards novel drugs discovery against polyketide synthase 13 thioesterase domain of Mycobacterium tuberculosis.Scientific reports · 2023Article
- Chemoproteomic Approaches for Unraveling Prokaryotic Biology.Israel journal of chemistry · 2023Article
- Antimicrobial Activity of Lactones.Antibiotics (Basel, Switzerland) · 2022Review
- Identification of covalent inhibitors that disrupt M. tuberculosis growth by targeting multiple serine hydrolases involved in lipid metabolism.Cell chemical biology · 2022Article
- Identification of cell wall synthesis inhibitors active against Mycobacterium tuberculosis by competitive activity-based protein profiling.Cell chemical biology · 2022Article
- Design, Synthesis and Biological Evaluation ofMolecules (Basel, Switzerland) · 2022Article
Corrections and comments
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Authors and funding
12 authors at 4 institutions in 2 countries.
Funding
Abstract
The spread of antibiotic resistance is a major challenge for the treatment of Mycobacterium tuberculosis infections. In addition, the efficacy of drugs is often limited by the restricted permeability of the mycomembrane. Frontline antibiotics inhibit mycomembrane biosynthesis, leading to rapid cell death. Inspired by this mechanism, we exploited β-lactones as putative mycolic acid mimics to block serine hydrolases involved in their biosynthesis. Among a collection of β-lactones, we found one hit with potent anti-mycobacterial and bactericidal activity. Chemical proteomics using an alkynylated probe identified Pks13 and Ag85 serine hydrolases as major targets. Validation through enzyme assays and customized
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.