Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1373168 | Bioorganic & Medicinal Chemistry Letters | 2011 | 4 Pages |
Abstract
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.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Michael M. Madden, Avinash Muppidi, Zhenyu Li, Xiaolong Li, Jiandong Chen, Qing Lin,