ArticleChemical science2021
Hit-optimization using target-directed dynamic combinatorial chemistry: development of inhibitors of the anti-infective target 1-deoxy-d-xylulose-5-phosphate synthase.
Article in Chemical science, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 34 citations in OpenAlex.
- Identification of Natural-Product Inhibitors of the 2ACS medicinal chemistry letters · 2026Article
- Dynamic combinatorial chemistry directed by proteins and nucleic acids: a powerful tool for drug discovery.Chemical Society reviews · 2025Review
- GlnA3Journal of bacteriology · 2025Article
- Synthesis and Antimycobacterial Assays of Some New Ethambutol Analogs.Molecules (Basel, Switzerland) · 2025Article
- Dynamic Combinatorial Chemistry Unveils Nsp10 Inhibitors with Antiviral Potential Against SARS-CoV-2.Chemistry (Weinheim an der Bergstrasse, Germany) · 2025Article
- Article
- Evaluation of ketoclomazone and its analogues as inhibitors of 1-deoxy-d-xylulose 5-phosphate synthases and other thiamine diphosphate (ThDP)-dependent enzymes.RSC medicinal chemistry · 2024Article
- Potent Inhibition ofACS infectious diseases · 2024Article
- Fighting antibiotic resistance-strategies and (pre)clinical developments to find new antibacterials.EMBO reports · 2023Review
- In Situ Inhibitor Synthesis and Screening by Fluorescence Polarization: An Efficient Approach for Accelerating Drug Discovery.Angewandte Chemie (Weinheim an der Bergstrasse, Germany) · 2022Article
- In Situ Inhibitor Synthesis and Screening by Fluorescence Polarization: An Efficient Approach for Accelerating Drug Discovery.Angewandte Chemie (International ed. in English) · 2022Article
- Total Synthesis and Biological Evaluation of Modified Ilamycin Derivatives.Marine drugs · 2022Article
- Discovery of novel drug-like antitubercular hits targeting the MEP pathway enzyme DXPS by strategic application of ligand-based virtual screening.Chemical science · 2022Article
- Identification of RAD51-BRCA2 Inhibitors UsingACS medicinal chemistry letters · 2022Article
- Thiamine analogues as inhibitors of pyruvate dehydrogenase and discovery of a thiamine analogue with non-thiamine related antiplasmodial activity.RSC medicinal chemistry · 2022Article
- Teaching an Old Compound New Tricks: Reversible Transamidation in Maleamic Acids.Chemistry (Weinheim an der Bergstrasse, Germany) · 2022Article
- First crystal structures of 1-deoxy-D-xylulose 5-phosphate synthase (DXPS) from Mycobacterium tuberculosis indicate a distinct mechanism of intermediate stabilization.Scientific reports · 2022Article
Corrections and comments
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Authors and funding
13 authors at 4 institutions in 4 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Target-directed dynamic combinatorial chemistry (tdDCC) enables identification, as well as optimization of ligands for un(der)explored targets such as the anti-infective target 1-deoxy-d-xylulose-5-phosphate synthase (DXPS). We report the use of tdDCC to first identify and subsequently optimize binders/inhibitors of the anti-infective target DXPS. The initial hits were also optimized for their antibacterial activity against
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Registered trials
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