Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 21, Issue 5, Pages 1472-1475Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.01.004
Keywords
Inhibitors; Protein-protein interaction; Dipolar cycloaddition; Cellular uptake; Stapled peptides
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Funding
- Pardee Foundation
- National Institutes of Health [GM 085092, CA 109636, 118210]
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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.
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