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New pieces to an old puzzle: identifying the warfarin-binding site that prevents clotting

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Warfarin has been the most widely prescribed anticoagulant for decades. It functions by inhibiting the membrane enzyme vitamin K epoxide reductase (VKOR), but the molecular details of this effect have remained elusive. Two new studies shed light on the warfarin-VKOR interaction. The work has implications for precision medicine and could guide drug discovery.

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Figure 1: Modeling, docking, and MD simulations of hVKOR identify the warfarin-binding site as located at the hydrophobic cleft proximal to the lumen.

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Authors and Affiliations

  1. Jacob K. Hilton and Wade D. Van Horn are at the School of Molecular Sciences, the Biodesign Center for Personalized Diagnostics, and the Magnetic Resonance Research Center, Arizona State University, Tempe, Arizona, USA.,

    Jacob K Hilton & Wade D Van Horn

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  1. Jacob K Hilton
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  2. Wade D Van Horn
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Correspondence to Wade D Van Horn.

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The authors declare no competing financial interests.

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Hilton, J., Van Horn, W. New pieces to an old puzzle: identifying the warfarin-binding site that prevents clotting. Nat Struct Mol Biol 24, 5–6 (2017). https://doi.org/10.1038/nsmb.3356

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