Toward the discovery of potent inhibitors of botulinum neurotoxin A: development of a robust LC MS based assay operational from low to subnanomolar enzyme concentrations.
The development of a sensitive, yet reliable assay for the analysis of botulinum neurotoxin A (BoNT/A) inhibitors is described; using this assay a new protease inhibitor was characterized and found to be one of the most potent inhibitors reported to date.
Capková
Katerina
K
Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA.
Hixon
Mark S
MS
McAllister
Laura A
LA
Janda
Kim D
KD
D000218:Adamantane / Q000031:analogs & derivatives / Q000737:chemistry* / Q000494:pharmacology*; D001667:Binding, Competitive; D019274:Botulinum Toxins, Type A / Q000037:antagonists & inhibitors* / Q000737:chemistry*; D002384:Catalysis; D002851:Chromatography, High Pressure Liquid; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical / Q000379:methods*; D005453:Fluorescence; D013058:Mass Spectrometry; D012680:Sensitivity and Specificity
D019274:Botulinum Toxins, Type A; D000218:Adamantane