Synthetic substrate for application in both high and low throughput assays for botulinum neurotoxin B protease inhibitors.
A FRET peptide substrate was synthesized and evaluated for enzymatic cleavage by the BoNT/B light chain protease. The FRET substrate was found to be useful in both a high throughput assay to uncover initial 'hits' and a low throughput HPLC assay to determine kinetic parameters and modes of inhibition.
Salzameda
Nicholas T
NT
Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, La Jolla, CA 92037, USA.
Barbieri
Joseph T
JT
Janda
Kim D
KD
D000595:Amino Acid Sequence; D001905:Botulinum Toxins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D019274:Botulinum Toxins, Type A; D031541:Fluorescence Resonance Energy Transfer; D008969:Molecular Sequence Data; D010455:Peptides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D011480:Protease Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
D010455:Peptides; D011480:Protease Inhibitors; C096323:rimabotulinumtoxinB; D001905:Botulinum Toxins; D019274:Botulinum Toxins, Type A