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Chem Commun (Camb). 2014 Mar 7;50(19):2445-7. doi: 10.1039/c3cc48818g. Epub 2014 Jan 22.

Rational hopping of a peptidic scaffold into non-peptidic scaffolds: structurally novel potent proteasome inhibitors derived from a natural product, belactosin A.

Author information

  • 1Faculty of Pharmaceutical Sciences, Hokkaido University, Kita-12, Nishi-6, Kita-ku, Sapporo 060-0812, Japan. shu@pharm.hokudai.ac.jp.

Abstract

Rational scaffold hopping of a natural product belactosin A derivative was successfully achieved based on the pharmacophore model constructed. The peptidic scaffold was replaced by significantly simplified non-peptidic scaffolds, by which weak belactosin A (IC50 = 1440 nM) was converted into highly potent non-peptidic inhibitors (IC50 = 26-393 nM).

PMID:
24452398
DOI:
10.1039/c3cc48818g
[PubMed - indexed for MEDLINE]
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