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