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; Thomas Kodadek

doi:10.1039/B717861A

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Chemical Communications

Issue 9, 2008

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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

Chem. Commun., 2008, 1064-1066

DOI: 10.1039/B717861A
Received 19 Nov 2007, Accepted 03 Jan 2008
First published on the web 24 Jan 2008

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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.

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Experimental details for synthesis and biological assays; structures of glycine-scanned compounds and C2
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Hyun-Suk Lim
Chase T. Archer
Young-Chan Kim
Troy Hutchens
Thomas Kodadek

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Chemical Communications

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

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