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  • Title: Discovery of inhibitors of the channel-activating protease prostasin (CAP1/PRSS8) utilizing structure-based design.
    Author: Tully DC, Vidal A, Chatterjee AK, Williams JA, Roberts MJ, Petrassi HM, Spraggon G, Bursulaya B, Pacoma R, Shipway A, Schumacher AM, Danahay H, Harris JL.
    Journal: Bioorg Med Chem Lett; 2008 Nov 15; 18(22):5895-9. PubMed ID: 18752942.
    Abstract:
    Structure-based design was utilized to guide the early stage optimization of a substrate-like inhibitor to afford potent peptidomimetic inhibitors of the channel-activating protease prostasin. The first X-ray crystal structures of prostasin with small molecule inhibitors bound to the active site are also reported.
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