title: Aza-peptide Michael acceptors: a new class of inhibitors specific for caspases and other clan CD cysteine proteases.
abstract: Aza-peptide Michael acceptors are a new class of irreversible inhibitors that are highly potent and specific for clan CD cysteine proteases. The aza-Asp derivatives were specific for caspases, while aza-Asn derivatives were effective legumain inhibitors. Aza-Lys and aza-Orn derivatives were potent inhibitors of gingipain K and clostripain. Aza-peptide Michael acceptors showed no cross reactivity toward papain, cathepsin B, and calpain.
authors.affiliation: School of Chemistry and Biochemistry and the Parker H. Petit Institute for Bioengineering and Bioscience, Georgia Institute of Technology, Atlanta, GA 30332-0400, USA.
authors.forename: Ozlem Doğan
authors.initials: OD
authors.lastname: Ekici
authors.forename: Marion G
authors.initials: MG
authors.lastname: Götz
authors.forename: Karen Ellis
authors.initials: KE
authors.lastname: James
authors.forename: Zhao Zhao
authors.initials: ZZ
authors.lastname: Li
authors.forename: Brian J
authors.initials: BJ
authors.lastname: Rukamp
authors.forename: Juliana L
authors.initials: JL
authors.lastname: Asgian
authors.forename: Conor R
authors.initials: CR
authors.lastname: Caffrey
authors.forename: Elizabeth
authors.initials: E
authors.lastname: Hansell
authors.forename: Jan
authors.initials: J
authors.lastname: Dvorák
authors.forename: James H
authors.initials: JH
authors.lastname: McKerrow
authors.forename: Jan
authors.initials: J
authors.lastname: Potempa
authors.forename: James
authors.initials: J
authors.lastname: Travis
authors.forename: Jowita
authors.initials: J
authors.lastname: Mikolajczyk
authors.forename: Guy S
authors.initials: GS
authors.lastname: Salvesen
authors.forename: James C
authors.initials: JC
authors.lastname: Powers
mesh_terms: D018829:Adhesins, Bacterial; D001372:Aza Compounds / Q000138:chemical synthesis* / Q000737:chemistry; D061945:Caspase Inhibitors; D020169:Caspases / Q000737:chemistry; D003546:Cysteine Endopeptidases / Q000737:chemistry; D015853:Cysteine Proteinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry; D000080867:Gingipain Cysteine Endopeptidases; D006388:Hemagglutinins / Q000737:chemistry; D007700:Kinetics; D010455:Peptides / Q000138:chemical synthesis* / Q000737:chemistry
chemical_list: D018829:Adhesins, Bacterial; D001372:Aza Compounds; D061945:Caspase Inhibitors; D015853:Cysteine Proteinase Inhibitors; D000080867:Gingipain Cysteine Endopeptidases; D006388:Hemagglutinins; D010455:Peptides; D020169:Caspases; D003546:Cysteine Endopeptidases; C019913:clostripain