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Showing 1–4 of 4 results
Advanced filters: Author: Constant A. A. van Boeckel Clear advanced filters
  • Computer modelling of the antithrombin III–heparin–thrombin complex inspired the synthesis of novel glycoconjugates, whose factor Xa and thrombin inhibitory activites can be adjusted in a rational way, leading to anticoagulants with unprecedented characteristics.

    • Peter D.J. Grootenhuis
    • Pieter Westerduin
    • Constant A.A. van Boeckel
    Correspondence
    Nature Structural Biology
    Volume: 2, P: 736-739
  • Global antibiotic scarcity looms owing to bacterial resistance. Now the discovery of a class of allosteric inhibitors targeting DNA gyrase—essential for bacteria—yields a compound LEI-800 that exhibits activity against fluoroquinolone-resistant E. coli. The compound’s unique mode of action, revealed through cryo-EM, makes it a promising candidate for countering bacterial resistance.

    • Alexander T. Bakker
    • Ioli Kotsogianni
    • Mario van der Stelt
    ResearchOpen Access
    Nature Chemistry
    Volume: 16, P: 1462-1472
  • Chemotherapy-induced peripheral neuropathy (CIPN) represents a major reason for discontinuation of treatment. Here, the authors show that LEI-515, a peripherally restricted monoacylglycerol lipase inhibitor, suppresses CIPN without inducing central nervous system side effects or physical dependence.

    • Ming Jiang
    • Mirjam C. W. Huizenga
    • Mario van der Stelt
    ResearchOpen Access
    Nature Communications
    Volume: 14, P: 1-19
  • An inhibitor of NAPE-PLD involved in lipid biosynthesis lowers levels of the endocannabinoid anandamide and other N-acylethanolamines in cells and mouse brain and activates the hypothalamus–pituitary–adrenal axis and impaired fear extinction.

    • Elliot D. Mock
    • Mohammed Mustafa
    • Mario van der Stelt
    Research
    Nature Chemical Biology
    Volume: 16, P: 667-675