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Issue 39, 2014
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Designer macrocyclic organo-peptide hybrids inhibit the interaction between p53 and HDM2/X by accommodating a functional α-helix

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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


Submitted
14 Feb 2014
Accepted
18 Mar 2014
First published
07 Apr 2014

Chem. Commun., 2014,50, 5027-5030
Article type
Communication
Author version available

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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