doi: 10.1016/j.bmcl.2003.09.096.
Terephthalamide derivatives as mimetics of the helical region of Bak peptide target Bcl-xL protein
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- PMID: 15006365
- DOI: 10.1016/j.bmcl.2003.09.096
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Terephthalamide derivatives as mimetics of the helical region of Bak peptide target Bcl-xL protein
Bioorg Med Chem Lett.
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Abstract
A group of novel Bcl-xL/Bak antagonists, based on a terephthalamide scaffold, were designed to mimic the alpha-helical region of the Bak peptide. Good in vitro inhibition potencies in disrupting the Bak/Bcl-xL complex have been observed (terephthalamide 4, K(i)=0.78+/-0.07 microM).
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