Achieving cell penetration with distance-matching cysteine cross-linkers: a facile route to cell-permeable peptide dual inhibitors of Mdm2/Mdmx.
Achieving cell penetration with distance-matching cysteine cross-linkers: a facile route to cell-permeable peptide dual inhibitors of Mdm2/Mdmx.
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DOI：
10.1039/c1cc13320a
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发表时间：
2011-09-07
期刊：
影响因子：
--
通讯作者：
Lin Q
中科院分区：
文献类型：
--
作者：
Muppidi A;Wang Z;Li X;Chen J;Lin Q
我们报告了双芳基亚甲基溴的设计，作为一类新型刚性、距离匹配的半胱氨酸交联剂。通过交联在 i,i+7 位点含有半胱氨酸的 Mdm2/Mdmx 肽双重抑制剂，可以显着增强细胞通透性，同时增加螺旋性和生物活性。
We report the design of bisarylmethylene bromides as a new class of rigid, distance-matching cysteine cross-linkers. By cross-linking a peptide dual inhibitor of Mdm2/Mdmx containing cysteines at i,i+7 positions, dramatic enhancement in cell permeability was achieved, along with increased helicity and biological activity.