Literature DB >> 20158239

Botulinum neurotoxin A protease: discovery of natural product exosite inhibitors.

Peter Silhár1, Katerina Capková, Nicholas T Salzameda, Joseph T Barbieri, Mark S Hixon, Kim D Janda.   

Abstract

A new mechanistic class of BoNT/A zinc metalloprotease inhibitors, from Echinacea, exemplified by the natural product d-chicoric acid (I1) is disclosed. A detailed evaluation of chicoric acid's mechanism of inhibition reveals that the inhibitor binds to an exosite, displays noncompetitive partial inhibition, and is synergistic with a competitive active site inhibitor when used in combination. Other components found in Echinacea, I3 and I4, were also inhibitors of the protease.

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Year:  2010        PMID： 20158239      PMCID： PMC2832098          DOI： 10.1021/ja910761y

Source DB:  PubMed          Journal:  J Am Chem Soc        ISSN： 0002-7863            Impact factor:   15.419


  14 in total

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6.  Quinolinol and peptide inhibitors of zinc protease in botulinum neurotoxin A: effects of zinc ion and peptides on inhibition.

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7.  L-chicoric acid inhibits human immunodeficiency virus type 1 integration in vivo and is a noncompetitive but reversible inhibitor of HIV-1 integrase in vitro.

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Review 10.  The evolving field of biodefence: therapeutic developments and diagnostics.

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  22 in total

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8.  Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.

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9.  Newly Designed Quinolinol Inhibitors Mitigate the Effects of Botulinum Neurotoxin A in Enzymatic, Cell-Based, and ex Vivo Assays.

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10.  Identification of exosite-targeting inhibitors of anthrax lethal factor by high-throughput screening.

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