Issue 33, 2011

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

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

Supplementary files

Article information

Article type
Communication
Submitted
03 Jun 2011
Accepted
01 Jul 2011
First published
19 Jul 2011

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

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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