Terephthalamide derivatives as mimetics of the helical region of Bak peptide target Bcl-xL protein |
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Authors: | Yin Hang Hamilton Andrew D |
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Affiliation: | Department of Chemistry, Yale University, PO Box 20810, New Haven, CT 06511, USA. |
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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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