Design and application of an α-helix-mimetic scaffold based on an oligoamide-foldamer strategy: Antagonism of the Bak BH3/Bcl-xL complex

Justin T. Ernst, Jorge Becerril, Hyung Soon Park, Hang Yin, Andrew D. Hamilton

Research output: Contribution to journalArticlepeer-review

Abstract

The prevention of cell death by the antiapoptotic protein Bcl-xL has been linked to a number of cancers. Bcl-xl binds to the BH3 domain of the proapoptotic protein Bak, thus preventing programmed cell death. A competitive assay and docking studies have shown that the polyamide scaffold 1, which was synthesized based on a rational structure-based design, interferes with the Bak BH3/Bcl-xl complexation.

Original languageEnglish (US)
Pages (from-to)535-539
Number of pages5
JournalAngewandte Chemie - International Edition
Volume42
Issue number5
DOIs
StatePublished - Feb 3 2003

Keywords

  • Amides
  • Helical structures
  • Peptidomimetics
  • Protein models
  • Proteins

ASJC Scopus subject areas

  • Catalysis
  • Chemistry(all)

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