| Beta-cyclodextrin derivatives that inhibit anthrax lethal toxin. | |
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MedLine Citation:
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PMID: 16169738 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Recently, we demonstrated that simultaneous blocking of bacterial growth by antibiotics and inhibition of anthrax toxin action with antibodies against protective antigen were beneficial for the treatment of anthrax. The present study examined the hypothesis that blocking the pore formed by protective antigen can inhibit the action of anthrax toxin. The potential inhibitors were chosen by a structure-based design using beta-cyclodextrin as the starting molecule. Several beta-cyclodextrin derivatives were evaluated for their ability to protect RAW 264.7 cells from the action of anthrax lethal toxin. Per-substituted aminoalkyl derivatives displayed inhibitory activity and were protective against anthrax lethal toxin action at low micromolar concentrations. These results provide the basis for a structure-based drug discovery program, with the goal of identifying new drug candidates for anthrax treatment. |
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Authors:
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Vladimir A Karginov; Adiamseged Yohannes; Tanisha M Robinson; Nour Eddine Fahmi; Kenneth Alibek; Sidney M Hecht |
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Publication Detail:
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Type: Journal Article; Research Support, N.I.H., Extramural Date: 2005-09-19 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry Volume: 14 ISSN: 0968-0896 ISO Abbreviation: Bioorg. Med. Chem. Publication Date: 2006 Jan |
Date Detail:
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Created Date: 2005-11-21 Completed Date: 2006-05-04 Revised Date: 2007-11-14 |
Medline Journal Info:
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Nlm Unique ID: 9413298 Medline TA: Bioorg Med Chem Country: England |
Other Details:
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Languages: eng Pagination: 33-40 Citation Subset: IM |
Affiliation:
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Innovative Biologics, Inc., 10900 University Blvd., Manassas, VA 20110, USA. vak@innovbio.com |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Antigens, Bacterial Bacterial Toxins / antagonists & inhibitors* Cell Line Mice beta-Cyclodextrins / chemistry, pharmacology* |
| Grant Support | |
ID/Acronym/Agency:
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1R43AI052894-01/AI/NIAID NIH HHS |
| Chemical | |
Reg. No./Substance:
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0/Antigens, Bacterial; 0/Bacterial Toxins; 0/anthrax toxin; 0/beta-Cyclodextrins; 7585-39-9/betadex |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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