Rapid identification of the pharmacophore in a peptoid inhibitor of the proteasome regulatory particle
Open Access
- 1 January 2008
- journal article
- Published by Royal Society of Chemistry (RSC) in Chemical Communications
- No. 9,p. 1064-1066
- https://doi.org/10.1039/b717861a
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.Keywords
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