ArticleThe Journal of biological chemistry2013
Thiolactomycin-based β-ketoacyl-AcpM synthase A (KasA) inhibitors: fragment-based inhibitor discovery using transient one-dimensional nuclear overhauser effect NMR spectroscopy.
Article in The Journal of biological chemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 36 citations in OpenAlex.
- Free energy perturbation and machine learning-assisted identification of novel molecules for the Mycobacterium tuberculosis KasA protein: a fragment-based drug design approach.Molecular diversity · 2026Article
- Exploring FabH inhibitors for antimicrobial therapy: medicinal chemistry, synthetic approaches, and SAR evaluation.Molecular diversity · 2026Review
- Unlocking Lactonase Enzymes as Biocatalysts for the Deracemisation of Chiral γ-Thiolactones.Angewandte Chemie (International ed. in English) · 2025Article
- Progress of anti-tuberculosis drug targets and novel therapeutic strategies.Frontiers in microbiology · 2025Review
- Design and Synthesis of Novel Antimicrobial Agents.Antibiotics (Basel, Switzerland) · 2023Review
- Implications of Fragment-Based Drug Discovery in Tuberculosis and HIV.Pharmaceuticals (Basel, Switzerland) · 2022Review
- Review
- Molecular Docking Suggests the Targets of Anti-Mycobacterial Natural Products.Molecules (Basel, Switzerland) · 2021Article
- Article
- Investigation of the anti-TB potential of selected propolis constituents using a molecular docking approach.Scientific reports · 2018Article
- Design, Synthesis and Biological Evaluation of Some Triazole Schiff's Base Derivatives as Potential Antitubercular Agents.The open medicinal chemistry journal · 2018Article
- A Structural Basis for Biguanide Activity.Biochemistry · 2017Article
- Thiolactomycin-Based Inhibitors of Bacterial β-Ketoacyl-ACP Synthases with in Vivo Activity.Journal of medicinal chemistry · 2016Article
- New approaches to target the mycolic acid biosynthesis pathway for the development of tuberculosis therapeutics.Current pharmaceutical design · 2014Review
- Structural basis for the recognition of mycolic acid precursors by KasA, a condensing enzyme and drug target from Mycobacterium tuberculosis.The Journal of biological chemistry · 2013Article
- Progress in targeting cell envelope biogenesis in Mycobacterium tuberculosis.Future microbiology · 2013Review
Corrections and comments
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Authors and funding
8 authors at 2 institutions in 2 countries.
Funding
Abstract
Thiolactomycin (TLM) is a natural product inhibitor of KasA, the β-ketoacyl synthase A from Mycobacterium tuberculosis. To improve the affinity of TLM for KasA, a series of TLM analogs have been synthesized based on interligand NOEs between TLM and a pantetheine analog when both are bound simultaneously to the enzyme. Kinetic binding data reveal that position 3 of the thiolactone ring is a suitable position for elaboration of the TLM scaffold, and the structure-activity relationship studies provide information on the molecular features that govern time-dependent inhibition in this enzyme system. These experiments also exemplify the utility of transient one-dimensional NOE spectroscopy for obtaining interligand NOEs compared with traditional steady state two-dimensional NOESY spectroscopy.
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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.