Orthogonal functionalisation of α-helix mimetics

被引：23

作者：

Barnard, Anna ^{[1
,2
]}

Long, Kerya ^{[1
,2
]}

Yeo, David J. ^{[1
,2
]}

Miles, Jennifer A. ^{[1
,2
]}

Azzarito, Valeria ^{[1
,2
]}

Burslem, George M. ^{[1
,2
]}

Prabhakaran, Panchami ^{[1
,2
]}

Edwards, Thomas A. ^{[2
,3
]}

Wilson, Andrew J. ^{[1
,2
]}

机构：

[1] Univ Leeds, Sch Chem, Leeds LS2 9JT, W Yorkshire, England

[2] Univ Leeds, Astbury Ctr Struct & Mol Biol, Leeds LS2 9JT, W Yorkshire, England

[3] Univ Leeds, Sch Mol & Cellular Biol, Leeds LS2 9JT, W Yorkshire, England

来源：

ORGANIC & BIOMOLECULAR CHEMISTRY | 2014年 / 12卷 / 35期

基金：

欧洲研究理事会;

关键词：

PROTEIN-PROTEIN INTERACTIONS; SOLID-PHASE; 1,3-DIPOLAR CYCLOADDITIONS; INHIBITORS; DESIGN; MCL-1; DERIVATIVES; ANTAGONISTS; DISRUPTION; MODULATORS;

D O I：

10.1039/c4ob00915k

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

alpha-Helix mediated protein-protein interactions are of major therapeutic importance. As such, the design of inhibitors of this class of interaction is of significant interest. We present methodology to modify N-alkylated aromatic oligoamide alpha-helix mimetics using 'click' chemistry. The effect is shown to modulate the binding properties of a series of selective p53/hDM2 inhibitors.

引用

页码：6794 / 6799

页数：6

共 53 条

[51] Terephthalamide derivatives as mimetics of helical peptides:: Disruption of the Bcl-xL/Bak interaction [J].