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

Hang Yin, Andrew D. Hamilton

Chemistry

Research output: Contribution to journal › Article › peer-review

Abstract

A group of novel Bcl-xL/Bak antagonists, based on a terephthalamide scaffold, were designed to mimic the α-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 μM).

Original language	English (US)
Pages (from-to)	1375-1379
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	14
Issue number	6
DOIs	https://doi.org/10.1016/j.bmcl.2003.09.096
State	Published - Mar 22 2004

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

Access to Document

10.1016/j.bmcl.2003.09.096

Cite this

@article{5aa29e61f6a4447ea6f25ed5a8d22d03,

title = "Terephthalamide derivatives as mimetics of the helical region of Bak peptide target Bcl-xL protein",

abstract = "A group of novel Bcl-xL/Bak antagonists, based on a terephthalamide scaffold, were designed to mimic the α-helical region of the Bak peptide. Good in vitro inhibition potencies in disrupting the Bak/Bcl-xL complex have been observed (terephthalamide 4, Ki=0.78±0.07 μM).",

author = "Hang Yin and Hamilton, {Andrew D.}",

note = "Funding Information: We thank the National Institutes of Health for financial support of this work.",

year = "2004",

month = mar,

day = "22",

doi = "10.1016/j.bmcl.2003.09.096",

language = "English (US)",

volume = "14",

pages = "1375--1379",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Ltd",

number = "6",

}

TY - JOUR

T1 - Terephthalamide derivatives as mimetics of the helical region of Bak peptide target Bcl-xL protein

AU - Yin, Hang

AU - Hamilton, Andrew D.

N1 - Funding Information: We thank the National Institutes of Health for financial support of this work.

PY - 2004/3/22

Y1 - 2004/3/22

N2 - A group of novel Bcl-xL/Bak antagonists, based on a terephthalamide scaffold, were designed to mimic the α-helical region of the Bak peptide. Good in vitro inhibition potencies in disrupting the Bak/Bcl-xL complex have been observed (terephthalamide 4, Ki=0.78±0.07 μM).

AB - A group of novel Bcl-xL/Bak antagonists, based on a terephthalamide scaffold, were designed to mimic the α-helical region of the Bak peptide. Good in vitro inhibition potencies in disrupting the Bak/Bcl-xL complex have been observed (terephthalamide 4, Ki=0.78±0.07 μM).

UR - http://www.scopus.com/inward/record.url?scp=1542285103&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=1542285103&partnerID=8YFLogxK

U2 - 10.1016/j.bmcl.2003.09.096

DO - 10.1016/j.bmcl.2003.09.096

M3 - Article

C2 - 15006365

AN - SCOPUS:1542285103

SN - 0960-894X

VL - 14

SP - 1375

EP - 1379

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 6

ER -

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

Abstract

ASJC Scopus subject areas

Access to Document

Other files and links

Fingerprint

Cite this