title: Peptidomimetic aminomethylene ketone inhibitors of interleukin-1 beta-converting enzyme (ICE).
abstract: Pyridone-based peptidomimetic inhibitors of recombinant human Interleukin-1 beta-converting enzyme (ICE, caspase-1) with an aminomethylene ketone activating group in the P1' position are described. Several analogues with sub-nanomolar Ki's versus ICE and improved aqueous solubility are reported.
authors.affiliation: Department of Medicinal Chemistry, Ferring Research Institute, Chilworth Research Centre, Southampton, U.K.
authors.forename: G
authors.initials: G
authors.lastname: Semple
authors.forename: D M
authors.initials: DM
authors.lastname: Ashworth
authors.forename: A R
authors.initials: AR
authors.lastname: Batt
authors.forename: A J
authors.initials: AJ
authors.lastname: Baxter
authors.forename: D W
authors.initials: DW
authors.lastname: Benzies
authors.forename: L H
authors.initials: LH
authors.lastname: Elliot
authors.forename: D M
authors.initials: DM
authors.lastname: Evans
authors.forename: R J
authors.initials: RJ
authors.lastname: Franklin
authors.forename: P
authors.initials: P
authors.lastname: Hudson
authors.forename: P D
authors.initials: PD
authors.lastname: Jenkins
authors.forename: G R
authors.initials: GR
authors.lastname: Pitt
authors.forename: D P
authors.initials: DP
authors.lastname: Rooker
authors.forename: S
authors.initials: S
authors.lastname: Yamamoto
authors.forename: Y
authors.initials: Y
authors.lastname: Isomura
mesh_terms: D000577:Amides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D061945:Caspase Inhibitors; D015853:Cysteine Proteinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D007700:Kinetics; D015394:Molecular Structure; D011728:Pyridones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors; D012995:Solubility; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D061945:Caspase Inhibitors; D015853:Cysteine Proteinase Inhibitors; D011728:Pyridones; D011994:Recombinant Proteins