Terephthalamide derivatives as mimetics of the helical region of Bak peptide target Bcl-xL protein

Hang Yin; Andrew D Hamilton

doi:10.1016/j.bmcl.2003.09.096

Terephthalamide derivatives as mimetics of the helical region of Bak peptide target Bcl-xL protein

Bioorg Med Chem Lett. 2004 Mar 22;14(6):1375-9. doi: 10.1016/j.bmcl.2003.09.096.

Authors

Hang Yin¹, Andrew D Hamilton

Affiliation

¹ Department of Chemistry, Yale University, PO Box 20810, New Haven, CT 06511, USA.

PMID: 15006365
DOI: 10.1016/j.bmcl.2003.09.096

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).

Publication types

Research Support, U.S. Gov't, P.H.S.

MeSH terms

Drug Delivery Systems / methods
Membrane Proteins / analysis
Membrane Proteins / chemistry*
Membrane Proteins / metabolism
Molecular Mimicry*
Phthalimides / analysis
Phthalimides / chemistry*
Phthalimides / metabolism
Protein Structure, Secondary
Proto-Oncogene Proteins c-bcl-2 / analysis
Proto-Oncogene Proteins c-bcl-2 / chemistry*
Proto-Oncogene Proteins c-bcl-2 / metabolism
Stereoisomerism
bcl-2 Homologous Antagonist-Killer Protein
bcl-X Protein

Substances

Membrane Proteins
Phthalimides
Proto-Oncogene Proteins c-bcl-2
bcl-2 Homologous Antagonist-Killer Protein
bcl-X Protein
terephthalamidine