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Issue 9, 2008
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Rapid identification of the pharmacophore in a peptoid inhibitor of the proteasome regulatory particle

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Abstract

Here we report a simple and effective method to identify the minimal pharmacophore in the first peptoid inhibitor of the 19S proteasome regulatory particle, which has led to the development of a derivative that exhibits improved cellular activity, presumably due to a reduction in mass of about two-fold and the elimination of positively charged lysine-like residues.

Graphical abstract: Rapid identification of the pharmacophore in a peptoid inhibitor of the proteasome regulatory particle

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Publication details

The article was received on 19 Nov 2007, accepted on 03 Jan 2008 and first published on 24 Jan 2008


Article type: Communication
DOI: 10.1039/B717861A
Chem. Commun., 2008, 1064-1066

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    Rapid identification of the pharmacophore in a peptoid inhibitor of the proteasome regulatory particle

    H. Lim, C. T. Archer, Y. Kim, T. Hutchens and T. Kodadek, Chem. Commun., 2008, 1064
    DOI: 10.1039/B717861A

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