Achieving cell penetration with distance-matching cysteine cross-linkers: a facile route to cell-permeable peptide dual inhibitors of Mdm2/Mdmx

作者：Muppidi Avinash; Wang Zhiyong; Li Xiaolong; Chen Jiandong; Lin Qing^*

来源：Chemical Communications, 2011, 47(33): 9396-9398.

DOI：10.1039/c1cc13320a

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.

• 出版日期2011