期刊
ORGANIC LETTERS
卷 8, 期 8, 页码 1729-1732出版社
AMER CHEMICAL SOC
DOI: 10.1021/ol0603211
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资金
- NIAID NIH HHS [N01 AI030050] Funding Source: Medline
- FDA HHS [BT010-04] Funding Source: Medline
Botulinum neurotoxins (BoNTs), etiological agents of the deadly food poisoning disease botulism, are the most toxic proteins currently known. By using in situ lead identification chemistry, we have uncovered the first class of inhibitors that displays nanomolar potency. From a 15 mu M lead compound, structure-activity relationship studies were performed granting the most potent BoNT/A inhibitor reported to date that displays an inhibition constant of 300 nM.
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