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Literature DB >> 22047690

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

Avinash Muppidi¹, Xiaolong Li, Jiandong Chen, Qing Lin.

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.

Entities: CellLine Chemical Disease Gene Mutation Species

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Year: 2011 PMID： 22047690 PMCID： PMC3569039 DOI： 10.1016/j.bmcl.2011.10.009

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

24 in total

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Authors: Jean-Guy Delcros; Sophie Tomasi; Simon Carrington; Bénédicte Martin; Jacques Renault; Ian S Blagbrough; Philippe Uriac
Journal: J Med Chem Date: 2002-11-07 Impact factor: 7.446

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Journal: Science Date: 1996-11-08 Impact factor: 47.728

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Journal: Proc Natl Acad Sci U S A Date: 1993-02-01 Impact factor: 11.205

9. Achieving cell penetration with distance-matching cysteine cross-linkers: a facile route to cell-permeable peptide dual inhibitors of Mdm2/Mdmx.

Authors: Avinash Muppidi; Zhiyong Wang; Xiaolong Li; Jiandong Chen; Qing Lin
Journal: Chem Commun (Camb) Date: 2011-07-19 Impact factor: 6.222

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5 in total

1. Synthesis of cell-permeable stapled BH3 peptide-based Mcl-1 inhibitors containing simple aryl and vinylaryl cross-linkers.

Authors: Avinash Muppidi; Kenichiro Doi; Carlo P Ramil; Hong-Gang Wang; Qing Lin
Journal: Tetrahedron Date: 2014-10-21 Impact factor: 2.457