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Literature DB >> 16386899

Guanidinylated 2,5-dideoxystreptamine derivatives as anthrax lethal factor inhibitors.

Guan-Sheng Jiao¹, Lynne Cregar, Mark E Goldman, Sherri Z Millis, Cho Tang.

Abstract

Anthrax lethal factor is a Zn(2+)-dependent metalloprotease and the key virulence factor of tripartite anthrax toxin secreted by Bacillus anthracis, the causative agent of anthrax. A series of guanidinylated 2,5-dideoxystreptamine derivatives were designed and synthesized as inhibitors of lethal factor, some of which show strong inhibitory activity against lethal factor in an in vitro FRET assay. Preparation and structure-activity relationships of these compounds are presented.

Entities: Chemical Species

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Year: 2006 PMID： 16386899 DOI： 10.1016/j.bmcl.2005.12.038

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

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Cited

10 in total

1. Inhibition of prohormone convertases PC1/3 and PC2 by 2,5-dideoxystreptamine derivatives.

Authors: Mirella Vivoli; Thomas R Caulfield; Karina Martínez-Mayorga; Alan T Johnson; Guan-Sheng Jiao; Iris Lindberg
Journal: Mol Pharmacol Date: 2011-12-14 Impact factor: 4.436

2. Identification of potent and compartment-selective small molecule furin inhibitors using cell-based assays.

Authors: Bruno Ramos-Molina; Adam N Lick; Elias H Blanco; J Alejandro Posada-Salgado; Karina Martinez-Mayorga; Alan T Johnson; Guan-Sheng Jiao; Iris Lindberg
Journal: Biochem Pharmacol Date: 2015-05-21 Impact factor: 5.858

3. Small molecule pan-dengue and West Nile virus NS3 protease inhibitors.

Authors: Lynne Cregar-Hernandez; Guan-Sheng Jiao; Alan T Johnson; Axel T Lehrer; Teri Ann S Wong; Stephen A Margosiak
Journal: Antivir Chem Chemother Date: 2011-05-12

4. Synthetic small molecule furin inhibitors derived from 2,5-dideoxystreptamine.

Authors: Guan-Sheng Jiao; Lynne Cregar; Jinzhi Wang; Sherri Z Millis; Cho Tang; Sean O'Malley; Alan T Johnson; Sina Sareth; Jason Larson; Gary Thomas
Journal: Proc Natl Acad Sci U S A Date: 2006-12-18 Impact factor: 11.205

5. Development of a comprehensive, validated pharmacophore hypothesis for anthrax toxin lethal factor (LF) inhibitors using genetic algorithms, Pareto scoring, and structural biology.

Authors: Ting-Lan Chiu; Elizabeth A Amin
Journal: J Chem Inf Model Date: 2012-06-25 Impact factor: 4.956

Guanidinylated 2,5-dideoxystreptamine derivatives as anthrax lethal factor inhibitors.

1. Inhibition of prohormone convertases PC1/3 and PC2 by 2,5-dideoxystreptamine derivatives.

2. Identification of potent and compartment-selective small molecule furin inhibitors using cell-based assays.

3. Small molecule pan-dengue and West Nile virus NS3 protease inhibitors.

4. Synthetic small molecule furin inhibitors derived from 2,5-dideoxystreptamine.

5. Development of a comprehensive, validated pharmacophore hypothesis for anthrax toxin lethal factor (LF) inhibitors using genetic algorithms, Pareto scoring, and structural biology.

6. Highly predictive support vector machine (SVM) models for anthrax toxin lethal factor (LF) inhibitors.

7. Small molecule inhibitors of anthrax lethal factor toxin.

8. Structure-activity relationship studies of a novel series of anthrax lethal factor inhibitors.

Review 9. Furin-mediated protein processing in infectious diseases and cancer.

10. Design and use of a novel substrate for simple, rapid, and specific early detection of anthrax infection.