ArticleChemical communications (Cambridge, England)2015
Facile synthesis of borofragments and their evaluation in activity-based protein profiling.
Article in Chemical communications (Cambridge, England), 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed.
- The role of protein palmitoylation in disease pathogenesis and therapeutic innovation.Annals of medicine · 2026Review
- Kinetically Stable Boron-Heteroatom Bonds.Angewandte Chemie (International ed. in English) · 2026Article
- Bench-Stable Boryl Thianthrenium Dication Enables Aziridinyl Boronate Synthesis via Metal-Free Late-Stage Aziridination with Diverse Nitrogen Nucleophiles.Angewandte Chemie (International ed. in English) · 2026Article
- Protein S-acylation: Pathological mechanisms and novel therapeutic targets for diabetic complications.Chinese herbal medicines · 2026Review
- Palmitoylation: an emerging therapeutic target bridging physiology and disease.Cellular & molecular biology letters · 2025Review
- Potential of Boronic Acid Derivatization and Activity in Agrochemical Discovery.Molecules (Basel, Switzerland) · 2025Review
- Recent developments in the medicinal chemistry of single boron atom-containing compounds.Acta pharmaceutica Sinica. B · 2021Review
- α/β-Hydrolase Domain (ABHD) Inhibitors as New Potential Therapeutic Options against Lipid-Related Diseases.Journal of medicinal chemistry · 2021Review
- α-Hydroxy boron-enabled regioselective access to bifunctional halo-boryl alicyclic ethers and α-halo borons.Chemical communications (Cambridge, England) · 2021Article
- Isonitrile-Based Multicomponent Synthesis of β-Amino Boronic Acids as β-Lactamase Inhibitors.Antibiotics (Basel, Switzerland) · 2020Article
- Insight into the factors controlling the equilibrium of allylic azides.RSC advances · 2020Article
- A modular and concise approach to MIDA acylboronatesChemical science · 2019Article
- Facile synthesis of α-aminoboronic acids from amines and potassium acyltrifluoroborates (KATs)Chemical science · 2018Article
- Multicomponent mapping of boron chemotypes furnishes selective enzyme inhibitors.Nature communications · 2017Article
- The versatility of boron in biological target engagement.Nature chemistry · 2017Review
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9 authors.
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Abstract
The discovery of enzyme inhibitors relies on synthetic methods that enable rapid and modular construction of small molecules. Heterocyclic fragments designed to maximize enthalpic interactions with their protein targets represent a particularly desirable class of molecules. Here we describe a reagent that enables straightforward construction of "borofragments", in which a heterocycle is separated from the boron center by two or three rotatable bonds. The stability of these molecules depends on the MIDA group which likely acts as a slow-release element under biological conditions. Borofragments can be used to discover inhibitors of enzymes that use catalytic oxygen nucleophiles. We have employed this method to identify inhibitors of ABHD10 and the predicted carboxypeptidase CPVL. This technique should be applicable to other classes of targets.
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