Design and modular parallel synthesis of a MCR derived α-helix mimetic protein-protein interaction inhibitor scaffold

被引:43
作者
Antuch, W
Menon, S
Chen, QZ
Lu, YC
Sakamuri, S
Beck, B
Schauer-Vukasinovic, V
Agarwal, S
Hess, S
Dömling, A
机构
[1] ABC Pharma, D-81243 Munich, Germany
[2] Morphochem AG, D-81379 Munich, Germany
[3] Morphochem Inc, Monmouth Jct, NJ USA
关键词
protein interaction antagonist; cancer; Bc1; family; apoptosis; multicomponent reaction; isocyanide;
D O I
10.1016/j.bmcl.2005.11.102
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A terphenyl alpha-helix mimetic scaffold recognized to be capable of disrupting protein-protein interactions was structurally morphed into an easily amenable and versatile multicomponent reaction (MCR) backbone. The design, modular in-parallel library synthesis, initial cell based biological data, and preliminary in vitro screening for the disruption of the Bcl-w/Bak protein-protein interaction by representatives of the MCR derived scaffold are presented. (C) 2006 Published by Elsevier Ltd.
引用
收藏
页码:1740 / 1743
页数:4
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