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Achieving cell penetration with distance-matching cysteine cross-linkers: a facile route to cell-permeable peptide dual inhibitors of Mdm2/Mdmx†
Avinash Muppidi,Zhiyong Wang,Xiaolong Li,Jiandong Chen,Qing Lin
Chemical Communications Pub Date : 07/19/2011 00:00:00 , DOI:10.1039/C1CC13320A
Abstract

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.

Graphical abstract: 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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