Aza-peptide Michael acceptors: a new class of inhibitors specific for caspases and other clan CD cysteine proteases.
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.
Ekici
Ozlem Doğan
OD
School of Chemistry and Biochemistry and the Parker H. Petit Institute for Bioengineering and Bioscience, Georgia Institute of Technology, Atlanta, GA 30332-0400, USA.
Götz
Marion G
MG
James
Karen Ellis
KE
Li
Zhao Zhao
ZZ
Rukamp
Brian J
BJ
Asgian
Juliana L
JL
Caffrey
Conor R
CR
Hansell
Elizabeth
E
Dvorák
Jan
J
McKerrow
James H
JH
Potempa
Jan
J
Travis
James
J
Mikolajczyk
Jowita
J
Salvesen
Guy S
GS
Powers
James C
JC
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
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