Issue 39, 2014
From the journal:

Chemical Communications

Designer macrocyclic organo-peptide hybrids inhibit the interaction between p53 and HDM2/X by accommodating a functional α-helix†

Jessica M. Smith,a   John R. Frosta  and  Rudi Fasan*a  

* Corresponding authors

a Department of Chemistry, University of Rochester, Rochester, NY, USA
E-mail: fasan@chem.rochester.edu
Tel: +1-585-2733504

Abstract

We report the design of side-chain-to-tail linked organo-peptide hybrids incorporating an α-helical protein-binding motif. Using this strategy, macrocyclic inhibitors of the p53:HDM2 interaction displaying dual specificity against the HDMX homolog as well as increased proteolytic stability could be obtained.

Graphical abstract: Designer macrocyclic organo-peptide hybrids inhibit the interaction between p53 and HDM2/X by accommodating a functional α-helix

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Article information

DOI
https://doi.org/10.1039/C4CC01199F
Article type
Communication
Submitted
14 Feb 2014
Accepted
18 Mar 2014
First published
07 Apr 2014

Chem. Commun., 2014,50, 5027-5030

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Designer macrocyclic organo-peptide hybrids inhibit the interaction between p53 and HDM2/X by accommodating a functional α-helix

J. M. Smith, J. R. Frost and R. Fasan, Chem. Commun., 2014, 50, 5027 DOI: 10.1039/C4CC01199F

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