Discovery of inhibitors of the channel-activating protease prostasin (CAP1/PRSS8) utilizing structure-based design

  • Bioorg Med Chem Lett. 2008 Nov 15;18(22):5895-9. doi: 10.1016/j.bmcl.2008.08.029.
David C Tully  1 ,  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
Affiliations
  • 1. Genomics Institute of the Novartis Research Foundation, 10675 John J. Hopkins Dr., San Diego, CA 92121, USA. [email protected]
PMID: 18752942 DOI: 10.1016/j.bmcl.2008.08.029
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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