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

Research output: Contribution to journalArticle

20 Citations (Scopus)

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.

Original languageEnglish (US)
Pages (from-to)1064-1066
Number of pages3
JournalChemical Communications
Issue number9
DOIs
StatePublished - 2008
Externally publishedYes

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Peptoids
Proteasome Inhibitors
Proteasome Endopeptidase Complex
Lysine
Derivatives

ASJC Scopus subject areas

  • Chemistry(all)

Cite this

Rapid identification of the pharmacophore in a peptoid inhibitor of the proteasome regulatory particle. / Lim, Hyun-Suk; Archer, Chase T.; Kim, Young Chan; Hutchens, Troy; Kodadek, Thomas.

In: Chemical Communications, No. 9, 2008, p. 1064-1066.

Research output: Contribution to journalArticle

Lim, Hyun-Suk ; Archer, Chase T. ; Kim, Young Chan ; Hutchens, Troy ; Kodadek, Thomas. / Rapid identification of the pharmacophore in a peptoid inhibitor of the proteasome regulatory particle. In: Chemical Communications. 2008 ; No. 9. pp. 1064-1066.
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