Chirality Holds the Key for Potent Inhibition of the Botulinum Neurotoxin Serotype A Protease
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;...
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| Veröffentlicht in: | Organic letters 2010-02, Vol.12 (4), p.756-759 |
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| container_title | Organic letters |
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| creator | Stowe, G. Neil Šilhár, Peter Hixon, Mark S Silvaggi, Nicholas R Allen, Karen N Moe, Scott T Jacobson, Alan R Barbieri, Joseph T Janda, Kim D |
| description | 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. |
| doi_str_mv | 10.1021/ol902820z |
| format | Article |
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Neil</au><au>Šilhár, Peter</au><au>Hixon, Mark S</au><au>Silvaggi, Nicholas R</au><au>Allen, Karen N</au><au>Moe, Scott T</au><au>Jacobson, Alan R</au><au>Barbieri, Joseph T</au><au>Janda, Kim D</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Chirality Holds the Key for Potent Inhibition of the Botulinum Neurotoxin Serotype A Protease</atitle><jtitle>Organic letters</jtitle><addtitle>Org. Lett</addtitle><date>2010-02-19</date><risdate>2010</risdate><volume>12</volume><issue>4</issue><spage>756</spage><epage>759</epage><pages>756-759</pages><issn>1523-7060</issn><eissn>1523-7052</eissn><abstract>Botulinum neurotoxin serotype A (BoNT/A) is the most toxic protein known to man and also a bioterrorism agent. 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| ispartof | Organic letters, 2010-02, Vol.12 (4), p.756-759 |
| issn | 1523-7060 1523-7052 |
| language | eng |
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| source | ACS Publications; MEDLINE |
| subjects | Botulinum Toxins, Type A - antagonists & inhibitors Botulinum Toxins, Type A - metabolism Botulinum Toxins, Type A - toxicity Catalysis Clostridium - chemistry Crystallography, X-Ray Humans Hydroxamic Acids - chemical synthesis Hydroxamic Acids - chemistry Hydroxamic Acids - pharmacology Molecular Structure Neurotoxins - antagonists & inhibitors Protease Inhibitors - chemical synthesis Protease Inhibitors - chemistry Protease Inhibitors - pharmacology Stereoisomerism Structure-Activity Relationship |
| title | Chirality Holds the Key for Potent Inhibition of the Botulinum Neurotoxin Serotype A Protease |
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