Benzylidene cyclopentenediones: First irreversible inhibitors against botulinum neurotoxin A's zinc endopeptidase.
A series of benzylidene cyclopentenedione-based inhibitors, acting through covalent modification of the active site of botulinum neurotoxin A light chain metalloprotease, are reported.
Capková
Katerina
K
Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA.
Hixon
Mark S
MS
Pellett
Sabine
S
Barbieri
Joseph T
JT
Johnson
Eric A
EA
Janda
Kim D
KD
D001597:Benzylidene Compounds / Q000737:chemistry*; D019274:Botulinum Toxins, Type A / Q000737:chemistry*; D020134:Catalytic Domain; D003517:Cyclopentanes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D008666:Metalloendopeptidases / Q000737:chemistry* / Q000378:metabolism; D011480:Protease Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D015032:Zinc / Q000737:chemistry*
D001597:Benzylidene Compounds; D003517:Cyclopentanes; D011480:Protease Inhibitors; D008666:Metalloendopeptidases; D019274:Botulinum Toxins, Type A; D015032:Zinc; C013905:cyclopentenone