Chirality holds the key for potent inhibition of the botulinum neurotoxin serotype a protease.
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ABSTRACT:
SUBMITTER: Stowe GN
PROVIDER: S-EPMC2821465 | biostudies-literature | 2010 Feb
REPOSITORIES: biostudies-literature
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Chirality holds the key for potent inhibition of the botulinum neurotoxin serotype a protease.
Stowe G Neil GN Silhár Peter P Hixon Mark S MS Silvaggi Nicholas R NR Allen Karen N KN Moe Scott T ST Jacobson Alan R AR Barbieri Joseph T JT Janda Kim D KD
Organic letters 20100201 4
Botulinum neurotoxin serotype A (BoNT/A) is the most toxic protein known to man and also a bioterrorism agent. As defined by our previous research targeting the etiological agent responsible for BoNT/A intoxication, a protease, we now report on the asymmetric synthesis of four new BoNT/A inhibitors; the most potent of this series is roughly 2-fold more active than the best small molecule inhibitor currently known. ...[more]
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