Benzylidene cyclopentenediones: First irreversible inhibitors against botulinum neurotoxin A's zinc endopeptidase.

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Capkova K, Hixon MS, Pellett S, Barbieri JT, Johnson EA, Janda KD

Benzylidene cyclopentenediones: First irreversible inhibitors against botulinum neurotoxin A's zinc endopeptidase.

Bioorg Med Chem Lett. 2010 Jan 1;20(1):206-8. doi: 10.1016/j.bmcl.2009.10.129. Epub 2009 Oct 31.

PubMed ID

19914829 [ View in PubMed

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Abstract

A series of benzylidene cyclopentenedione-based inhibitors, acting through covalent modification of the active site of botulinum neurotoxin A light chain metalloprotease, are reported.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
(2E)-3-(2,4-DICHLOROPHENYL)-N-HYDROXYACRYLAMIDE	Botulinum neurotoxin type A	IC 50 (nM)	900	N/A	N/A	Details
(2E)-3-(2,4-DICHLOROPHENYL)-N-HYDROXYACRYLAMIDE	Botulinum neurotoxin type A	IC 50 (nM)	900000	N/A	N/A	Details