Work

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

Year: 2008

Type: article

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.

Source: Chemical Communications

DOI: 10.1039/b717861a

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

Institution: The University of Texas Southwestern Medical Center

Language: English

Topic: Ubiquitin and proteasome pathways

Subfield: Molecular Biology

Field: Biochemistry, Genetics and Molecular Biology

Domain: Life Sciences

Open Access status: green

Funders: National Heart, Lung, and Blood Institute, National Institute of General Medical Sciences

Awards: G1861434375, Post-translational modification of activators, G5134089285