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

Abstract：

: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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Muppidi A,Li X,Chen J,Lin Q

doi

10.1016/j.bmcl.2011.10.009

subject

Has Abstract

pub_date

2011-12-15 00:00:00

pages

7412-5

issue

24

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(11)01397-7

journal_volume

21

pub_type

杂志文章

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