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
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
收藏
页码:6794 / 6799
页数:6
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