ArticleCell chemical biology2022
Identification of cell wall synthesis inhibitors active against Mycobacterium tuberculosis by competitive activity-based protein profiling.
Article in Cell chemical biology, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 37 citations in OpenAlex.
- Analysis of Confounding Factors in Reactive Cysteine Profiling Reveals Enhanced Chromatin-Protein Association via CDK7 Inhibition by THZ1.ACS chemical biology · 2026Article
- Identification of covalent inhibitors of Staphylococcus aureus serine hydrolases important for virulence and biofilm formation.Nature communications · 2025Article
- Mixed alkyl/aryl phosphonates identify metabolic serine hydrolases as antimalarial targets.Cell chemical biology · 2024Article
- Shifting Mycobacterial Serine Hydrolase Activity Visualized Using Multi-Layer In-Gel Activity Assays.Molecules (Basel, Switzerland) · 2024Article
- Chemical biology tools to probe bacterial glycans.Current opinion in chemical biology · 2024Review
- Mixed Alkyl/Aryl Phosphonates Identify Metabolic Serine Hydrolases as Antimalarial Targets.bioRxiv : the preprint server for biology · 2024Article
- Activity-based protein profiling of serine hydrolases and penicillin-binding proteins inFEMS microbes · 2024Article
- Chemoproteomic identification of a DPP4 homolog in Bacteroides thetaiotaomicron.Nature chemical biology · 2023Article
- Activity-based probes in pathogenic bacteria: Investigating drug targets and molecule specificity.Current opinion in chemical biology · 2023Review
- Activity-based protein profiling in microbes and the gut microbiome.Current opinion in chemical biology · 2023Review
- 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
- Sequence and Structural Motifs Controlling the Broad Substrate Specificity of the Mycobacterial Hormone-Sensitive Lipase LipN.ACS omega · 2023Article
- Activity-based Tools for Interrogating Host Biology During Infection.Israel journal of chemistry · 2023Article
- Chemoproteomic Approaches for Unraveling Prokaryotic Biology.Israel journal of chemistry · 2023Article
- Strategies for Competitive Activity-Based Protein Profiling in Small Molecule Inhibitor Discovery and Characterization.Israel journal of chemistry · 2023Article
- Multi-omics Investigation into the Mechanism of Action of an Anti-tubercular Fatty Acid Analogue.Journal of the American Chemical Society · 2022Article
- Identification of covalent inhibitors that disrupt M. tuberculosis growth by targeting multiple serine hydrolases involved in lipid metabolism.Cell chemical biology · 2022Article
- Integrated genomics and chemical biology herald an era of sophisticated antibacterial discovery, from defining essential genes to target elucidation.Cell chemical biology · 2022Review
- Optimized APEX2 peroxidase-mediated proximity labeling in fast- and slow-growing mycobacteria.Methods in enzymology · 2022Article
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11 authors at 5 institutions in 2 countries.
Funding
Abstract
The identification and validation of a small molecule's targets is a major bottleneck in the discovery process for tuberculosis antibiotics. Activity-based protein profiling (ABPP) is an efficient tool for determining a small molecule's targets within complex proteomes. However, how target inhibition relates to biological activity is often left unexplored. Here, we study the effects of 1,2,3-triazole ureas on Mycobacterium tuberculosis (Mtb). After screening ∼200 compounds, we focus on 4 compounds that form a structure-activity series. The compound with negligible activity reveals targets, the inhibition of which is functionally less relevant for Mtb growth and viability, an aspect not addressed in other ABPP studies. Biochemistry, computational docking, and morphological analysis confirms that active compounds preferentially inhibit serine hydrolases with cell wall and lipid metabolism functions and that disruption of the cell wall underlies biological activity. Our findings show that ABPP identifies the targets most likely relevant to a compound's antibacterial activity.
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