Title of article
Discovery of inhibitors of the channel-activating protease prostasin (CAP1/PRSS8) utilizing structure-based design
Author/Authors
David C. Tully، نويسنده , , Agnès Vidal، نويسنده , , Arnab K. Chatterjee، نويسنده , , Jennifer A. Williams، نويسنده , , Michael J. Roberts، نويسنده , , H. Michael Petrassi، نويسنده , , Glen Spraggon، نويسنده , , Badry Bursulaya، نويسنده , , Reynand Pacoma، نويسنده , , Aaron Shipway، نويسنده , , Andrew M. Schumacher، نويسنده , , Henry Danahay، نويسنده , , Jennifer L. Harris، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
5
From page
5895
To page
5899
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.
Keywords
ENaC activation , Peptidomimetic , Ketoheterocycle inhibitor , Prostasin , PRSS8 , hCAP , Channel-activating protease
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
800133
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