Conjugation of spermine enhances cellular uptake of the stapled peptide-based inhibitors of p53-Mdm2 interaction.

Conjugation of spermine enhances cellular uptake of the stapled peptide-based inhibitors of p53-Mdm2 interaction.
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DOI:
10.1016/j.bmcl.2011.10.009
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发表时间:
2011-12-15
影响因子:
2.7
通讯作者:
Lin, Qing
Lin, Qing
中科院分区:
医学4区
文献类型:
--
作者:
Muppidi, Avinash;Li, Xiaolong;Chen, Jiandong;Lin, Qing

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We report the first synthesis of the C-terminally spermine-conjugated stapled peptide-based inhibitors of the p53-Mdm2 interaction. Subsequent biological, biophysical and cellular uptake assays with the spermine-conjugated stapled peptides revealed that spermine conjugation minimally affects biological activity while significantly increases peptide helicity and cellular uptake without apparent cytotoxicity.
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