Ontology highlight
ABSTRACT:
SUBMITTER: Madden MM
PROVIDER: S-EPMC3057119 | biostudies-literature | 2011 Mar
REPOSITORIES: biostudies-literature
Madden Michael M MM Muppidi Avinash A Li Zhenyu Z Li Xiaolong X Chen Jiandong J Lin Qing Q
Bioorganic & medicinal chemistry letters 20110107 5
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. ...[more]