Article ID Journal Published Year Pages File Type
1373168 Bioorganic & Medicinal Chemistry Letters 2011 4 Pages PDF
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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Related Topics
Physical Sciences and Engineering Chemistry Organic Chemistry
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