Terephthalamide derivatives as mimetics of the helical region of Bak peptide target Bcl-xL protein.
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).
Department of Chemistry, Yale University, PO Box 20810, New Haven, CT 06511, USA.
Hang
H
Yin
Andrew D
AD
Hamilton
D016503:Drug Delivery Systems / Q000379:methods; D008565:Membrane Proteins / Q000032:analysis / Q000737:chemistry* / Q000378:metabolism; D018716:Molecular Mimicry; D010797:Phthalimides / Q000032:analysis / Q000737:chemistry* / Q000378:metabolism; D017433:Protein Structure, Secondary; D019253:Proto-Oncogene Proteins c-bcl-2 / Q000032:analysis / Q000737:chemistry* / Q000378:metabolism; D013237:Stereoisomerism; D050998:bcl-2 Homologous Antagonist-Killer Protein; D051020:bcl-X Protein
D008565:Membrane Proteins; D010797:Phthalimides; D019253:Proto-Oncogene Proteins c-bcl-2; D050998:bcl-2 Homologous Antagonist-Killer Protein; D051020:bcl-X Protein; C047750:terephthalamidine