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

doi:10.1002/anie.200390154

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

Chemistry

Research output: Contribution to journal › Article › peer-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 language	English (US)
Pages (from-to)	535-539
Number of pages	5
Journal	Angewandte Chemie - International Edition
Volume	42
Issue number	5
DOIs	https://doi.org/10.1002/anie.200390154
State	Published - Feb 3 2003

Keywords

Amides
Helical structures
Peptidomimetics
Protein models
Proteins

ASJC Scopus subject areas

Catalysis
General Chemistry

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10.1002/anie.200390154

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AU - Hamilton, Andrew D.

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

Abstract

Keywords

ASJC Scopus subject areas

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