Issue 33, 2011
From the journal:

Chemical Communications

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

Avinash Muppidi,a   Zhiyong Wang,a   Xiaolong Li,b   Jiandong Chenb  and  Qing Lin*a  

* Corresponding authors

a Department of Chemistry, State University of New York at Buffalo, Buffalo, USA
E-mail: qinglin@buffalo.edu
Fax: +01 (716) 645 6963
Tel: +01 (716) 645 4254

b Department of Molecular Oncology, H. Lee Moffitt Cancer Center, Tampa, USA

Abstract

We report the design of bisarylmethylene bromides as a new class of rigid, distance-matching cysteine cross-linkers. By cross-linking a peptide dual inhibitor of Mdm2/Mdmx containing cysteines at i,i+7 positions, dramatic enhancement in cell permeability was achieved, along with increased helicity and biological activity.

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

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Article information

DOI
https://doi.org/10.1039/C1CC13320A
Article type
Communication
Submitted
03 Jun 2011
Accepted
01 Jul 2011
First published
19 Jul 2011

Chem. Commun., 2011,47, 9396-9398

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

A. Muppidi, Z. Wang, X. Li, J. Chen and Q. Lin, Chem. Commun., 2011, 47, 9396 DOI: 10.1039/C1CC13320A

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