Journal
MOLECULES
Volume 16, Issue 1, Pages 202-220Publisher
MDPI
DOI: 10.3390/molecules16010202
Keywords
botulinum neurotoxin; inhibitor; drug discovery
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Botulinum neurotoxins (BoNTs) are the most potent of known toxins and are listed as category A biothreat agents by the U. S. CDC. The BoNT-mediated proteolysis of SNARE proteins inhibits the exocytosis of acetylcholine into neuromuscular junctions, leading to life-threatening flaccid paralysis. Currently, the only therapy for BoNT intoxication (which results in the disease state botulism) includes experimental preventative antibodies and long-term supportive care. Therefore, there is an urgent need to identify and develop inhibitors that will serve as both prophylactic agents and post-exposure 'rescue' therapeutics. This review focuses on recent progress to discover and develop small molecule inhibitors as therapeutic countermeasures for BoNT intoxication.
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