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Communication

Chem. Commun., 2008, 1064 - 1066, DOI: 10.1039/b717861a

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

Hyun-Suk Lim, Chase T. Archer, Young-Chan Kim, Troy Hutchens and Thomas Kodadek

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 image for this article (ID: b717861a)