Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 18, Issue 22, Pages 5895-5899Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.08.029
Keywords
Prostasin; PRSS8; hCAP; Channel-activating protease; ENaC activation; Peptidomimetic; Ketoheterocycle inhibitor
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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. (C) 2008 Elsevier Ltd. All rights reserved.
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