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Showing 1–3 of 3 results
Advanced filters: Author: Geoffrey A. Holdgate Clear advanced filters

  • Understanding the role of enzymes in disease states and the implementation of strategies to modulate their activities for therapeutic benefit remains a key focus for drug discovery. Here, Holdgate and colleagues assess the benefits of conducting and applying high-quality mechanistic enzymology studies throughout a drug-discovery programme and assess the value of combining such knowledge with orthogonal biophysical methods.

    • Geoffrey A. Holdgate
    • Thomas D. Meek
    • Rachel L. Grimley
    Reviews
    Nature Reviews Drug Discovery
    Volume: 17, P: 115-132

  • Receptor tyrosine kinases are key mediators of cell proliferation that have been implicated in several disease states for which they represent promising drug targets. Here the authors determine the thermodynamic basis for the low propensity of FGFR1 to access the DFG-Phe-out conformation required to bind type-II inhibitors.

    • Tobias Klein
    • Navratna Vajpai
    • Alexander L. Breeze
    ResearchOpen Access
    Nature Communications
    Volume: 6, P: 1-12