Synthesis of cell-permeable stapled peptide dual inhibitors of the p53-Mdm2/Mdmx interactions via photoinduced cycloaddition
作者:Michael M. Madden、Avinash Muppidi、Zhenyu Li、Xiaolong Li、Jiandong Chen、Qing Lin
DOI:10.1016/j.bmcl.2011.01.004
日期:2011.3
We report the first application of a photoinduced 1,3-dipolar cycloaddition reaction to 'staple' a peptide dual inhibitor of the p53-Mdm2/Mdmx interactions. A series of stapled peptide inhibitors were efficiently synthesized and showed excellent dual inhibitory activity in ELISA assay. Furthermore, the positively charged, stapled peptides showed enhanced cellular uptake along with modest in vivo activity. (C) 2011 Elsevier Ltd. All rights reserved.