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Toxicon. 2009 Oct;54(5):575-82. doi: 10.1016/j.toxicon.2009.03.016. Epub 2009 Mar 25.

Investigations into small molecule non-peptidic inhibitors of the botulinum neurotoxins.

Author information

1
Departments of Chemistry and Immunology, and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA, 92037, USA.

Abstract

Botulinum neurotoxins (BoNTs), proteins secreted by the bacteria genus Clostridium, represent a group of extremely lethal toxins and a potential bioterrorism threat. As the current therapeutic options are of a predominantly prophylactic nature and cannot be used en masse, new strategies and ultimately potential treatments are desperately needed to combat any widespread release of these neurotoxins. In these regards, our laboratory has been working on developing new alternatives to treat botulinum intoxication through the development of inhibitors of the light chain proteases, the etiological agent which causes BoNT intoxication. Such a strategy has required the construction of two high-throughput screens and small molecule non-peptidic libraries; excitingly, inhibitors of the BoNT/A protease have been uncovered and are being optimized via structure activity relationship studies.

PMID:
19327377
PMCID:
PMC2730986
DOI:
10.1016/j.toxicon.2009.03.016
[Indexed for MEDLINE]
Free PMC Article

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