Journal
CHEMICAL SCIENCE
Volume 6, Issue 4, Pages 2434-2443Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c4sc03559c
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Funding
- European Research Council [ERC-StG-240324]
- Wellcome Trust [104920/Z/14/Z]
- Wellcome Trust [104920/Z/14/Z] Funding Source: Wellcome Trust
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The development of foldamers capable of selective molecular recognition of solvent exposed protein surfaces represents an outstanding challenge in supramolecular chemical biology. Here we introduce an oligoamide foldamer with well-defined conformation that bears all the hallmarks of an information rich oligomer. Specifically, the foldamer recognizes its target protein hDM2 leading to inhibition of its protein-protein interaction with p53 in a manner that depends upon the composition, spatial projection and stereochemistry of functional groups appended to the scaffold. Most significantly, selective inhibition of p53/hDM2 can be achieved against four other targets and the selectivity for p53/hDM2 inhibition versus Mcl-1/NOXA-B inhibition is critically dependent upon the stereochemistry of the helix mimetic.
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