959424-27-2Relevant academic research and scientific papers
Discovery of inhibitors of the channel-activating protease prostasin (CAP1/PRSS8) utilizing structure-based design
Tully, David C.,Vidal, Agnes,Chatterjee, Arnab K.,Williams, Jennifer A.,Roberts, Michael J.,Petrassi, H. Michael,Spraggon, Glen,Bursulaya, Badry,Pacoma, Reynand,Shipway, Aaron,Schumacher, Andrew M.,Danahay, Henry,Harris, Jennifer L.
scheme or table, p. 5895 - 5899 (2009/05/31)
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.
Compounds and Compositions as Channel Activating Protease Inhibitors
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Page/Page column 99; 113, (2008/06/13)
The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating channel activating proteases, and methods for, using such compounds to treat, ameliorate or prevent a condition associated with a channel activating protease, including but not limited to prostasin, PRSS22, TMPRSS11 (e.g., TMPRSS11B, TMPRSS11E), TMPRSS2, TMPRSS3, TMPRSS4 (MTSP-2), matriptase (MTSP-1), CAP2, CAP3, trypsin, cathepsin A, or neutrophil elastase.
