Abstract
α-Helix mediated protein-protein interactions are of major therapeutic importance. As such, the design of inhibitors of this class of interaction is of significant interest. We present methodology to modify N-alkylated aromatic oligoamide α-helix mimetics using 'click' chemistry. The effect is shown to modulate the binding properties of a series of selective p53/hDM2 inhibitors.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Amides / chemistry
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Biomimetics
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Click Chemistry
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Humans
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Inhibitory Concentration 50
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Myeloid Cell Leukemia Sequence 1 Protein / chemistry
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Protein Binding
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Protein Interaction Mapping
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Protein Structure, Secondary
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Proteomics / methods
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Proto-Oncogene Proteins c-mdm2 / antagonists & inhibitors
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Proto-Oncogene Proteins c-mdm2 / chemistry*
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Solvents / chemistry
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Surface Properties
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Tumor Suppressor Protein p53 / antagonists & inhibitors
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Tumor Suppressor Protein p53 / chemistry*
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bcl-X Protein / chemistry
Substances
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Amides
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MCL1 protein, human
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Myeloid Cell Leukemia Sequence 1 Protein
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Solvents
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TP53 protein, human
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Tumor Suppressor Protein p53
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bcl-X Protein
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MDM2 protein, human
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Proto-Oncogene Proteins c-mdm2