Literature DB >> 18314330

Inhibitors of anthrax lethal factor based upon N-oleoyldopamine.

Brandon D Gaddis1, Charles M Rubert Pérez, Jean Chmielewski.   

Abstract

The structural features of an anthrax lethal factor inhibitor, N-oleoyldopamine (OLDA, 1) have been probed. The oleic acid moiety is critical, but, more interestingly, the presence of the double bond and its geometry were found to play an essential role. One compound, 5, was found to be an uncompetitive inhibitor of lethal factor (LF) with a K(i) value of 2.2microM and a cell-based IC(50) value of 4.3microM.

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Year:  2008        PMID： 18314330     DOI： 10.1016/j.bmcl.2008.02.044

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


  4 in total

1.  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

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

Authors:  Xia Zhang; Elizabeth Ambrose Amin
Journal:  J Mol Graph Model       Date:  2015-11-17       Impact factor: 2.518

3.  Small molecule inhibitors of Bacillus anthracis protective antigen proteolytic activation and oligomerization.

Authors:  Alexander N Wein; Brian N Williams; Shihui Liu; Boris Ermolinsky; Daniele Provenzano; Ruben Abagyan; Andrew Orry; Stephen H Leppla; Michael Peredelchuk
Journal:  J Med Chem       Date:  2012-09-18       Impact factor: 7.446

4.  Inhibition of anthrax lethal factor by curcumin and chemically modified curcumin derivatives.

Authors:  Anthony C Antonelli; Yu Zhang; Lorne M Golub; Francis Johnson; Sanford R Simon
Journal:  J Enzyme Inhib Med Chem       Date:  2013-10-09       Impact factor: 5.051
  4 in total

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