Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1364576 | Bioorganic & Medicinal Chemistry Letters | 2008 | 5 Pages |
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.
Graphical abstractStructure-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 structure of a small molecule inhibitor bound to the active site of prostasin is also reported.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
David C. Tully, Agnès Vidal, Arnab K. Chatterjee, Jennifer A. Williams, Michael J. Roberts, H. Michael Petrassi, Glen Spraggon, Badry Bursulaya, Reynand Pacoma, Aaron Shipway, Andrew M. Schumacher, Henry Danahay, Jennifer L. Harris,