title: Acyl dipeptides as reversible caspase inhibitors. Part 2: further optimization.
abstract: A new structural class of broad spectrum caspase inhibitors was optimized for its activity against caspases 1, 3, 6, 7, and 8. The most potent compound had low nanomolar broad spectrum activity, in particular, single digit nanomolar inhibitory activity against caspase 8.
authors.affiliation: Idun Pharmaceuticals, Inc., 9380 Judicial Drive, San Diego, CA 92121, USA. slinton@idun.com
authors.forename: Steven D
authors.initials: SD
authors.lastname: Linton
authors.forename: Donald S
authors.initials: DS
authors.lastname: Karanewsky
authors.forename: Robert J
authors.initials: RJ
authors.lastname: Ternansky
authors.forename: Ning
authors.initials: N
authors.lastname: Chen
authors.forename: Xian
authors.initials: X
authors.lastname: Guo
authors.forename: Kathy G
authors.initials: KG
authors.lastname: Jahangiri
authors.forename: Vincent J
authors.initials: VJ
authors.lastname: Kalish
authors.forename: Steven P
authors.initials: SP
authors.lastname: Meduna
authors.forename: Edward D
authors.initials: ED
authors.lastname: Robinson
authors.forename: Brett R
authors.initials: BR
authors.lastname: Ullman
authors.forename: Joe C
authors.initials: JC
authors.lastname: Wu
authors.forename: Brian
authors.initials: B
authors.lastname: Pham
authors.forename: Lalitha
authors.initials: L
authors.lastname: Kodandapani
authors.forename: Robert
authors.initials: R
authors.lastname: Smidt
authors.forename: Jose-Luis
authors.initials: JL
authors.lastname: Diaz
authors.forename: Lawrence C
authors.initials: LC
authors.lastname: Fritz
authors.forename: U
authors.initials: U
authors.lastname: von Krosigk
authors.forename: Silvio
authors.initials: S
authors.lastname: Roggo
authors.forename: Albert
authors.initials: A
authors.lastname: Schmitz
authors.forename: Kevin J
authors.initials: KJ
authors.lastname: Tomaselli
mesh_terms: D000215:Acylation; D061945:Caspase Inhibitors; D004151:Dipeptides / Q000138:chemical synthesis* / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D007202:Indicators and Reagents; D007527:Isoenzymes / Q000037:antagonists & inhibitors; D009842:Oligopeptides / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D061945:Caspase Inhibitors; D004151:Dipeptides; D004791:Enzyme Inhibitors; D007202:Indicators and Reagents; D007527:Isoenzymes; D009842:Oligopeptides