Discovery of inhibitors of the channel-activating protease prostasin (CAP1/PRSS8) utilizing structure-based design.
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.
Tully
David C
DC
Genomics Institute of the Novartis Research Foundation, 10675 John J. Hopkins Dr., San Diego, CA 92121, USA. dtully@gnf.org
Vidal
Agnès
A
Chatterjee
Arnab K
AK
Williams
Jennifer A
JA
Roberts
Michael J
MJ
Petrassi
H Michael
HM
Spraggon
Glen
G
Bursulaya
Badry
B
Pacoma
Reynand
R
Shipway
Aaron
A
Schumacher
Andrew M
AM
Danahay
Henry
H
Harris
Jennifer L
JL