期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 19, 页码 5811-5813出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.01.111
关键词
Inhibitor design; Inhibitor synthesis; Botulinum neurotoxin; Metalloprotease; Biothreat agent; Pharmacophore; Drug design
资金
- Defense Threat Reduction Agency [3.10024_06_RD_B]
- MRMC and NCI, National Institutes of Health [Y3CM 100505, N01-CO-12400]
- Developmental Therapeutics Program in the Division of Cancer Treatment and Diagnosis of the National Cancer Institute
Botulinum neurotoxins, responsible for the neuroparalytic syndrome botulism, are the deadliest of known biological toxins. The work described in this study was based on a three-zone pharmacophore model for botulinum neurotoxin serotype A light chain inhibition. Specifically, the pharmacophore defined a separation between the overlaps of several different, non-zinc(II)-coordinating small molecule chemotypes, enabling the design and synthesis of a new structural hybrid possessing a K(i) = 600 nM (+/- 100 nM). (C) 2009 Published by Elsevier Ltd.
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