Issue 9, 2008
From the journal:

Chemical Communications

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

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

* Corresponding authors

a Division of Translational Research, Departments of Internal Medicine and Molecular Biology, University of Texas Southwestern Medical Center, 5323 Harry Hines Boulevard, Dallas, Texas 75390-9185, USA
E-mail: thomas.kodadek@utsouthwestern.edu
Fax: +1-214-648-4156
Tel: +1-214-648-1239

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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Article information

DOI
https://doi.org/10.1039/B717861A
Article type
Communication
Submitted
19 Nov 2007
Accepted
03 Jan 2008
First published
24 Jan 2008

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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