Abstract
The use of cell-membrane translocating sequences for intracellular delivery of peptides can be a powerful approach to validate drug discovery targets in cellular settings. To accomplish this, a protocol has been implemented to couple the antennapedia third helix (residues 43-58) to a potent antagonist of the p53/hdm2 protein-protein interaction without affecting its in vitro inhibitory activity.
MeSH terms
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Antennapedia Homeodomain Protein
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Binding, Competitive / drug effects
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Homeodomain Proteins / chemistry
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Homeodomain Proteins / pharmacology*
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Humans
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Nuclear Proteins*
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Peptide Fragments / pharmacology
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Protein Structure, Secondary
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Proto-Oncogene Proteins / metabolism*
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Proto-Oncogene Proteins c-mdm2
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Transcription Factors*
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Tumor Suppressor Protein p53 / metabolism*
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Tumor Suppressor Protein p53 / physiology
Substances
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Antennapedia Homeodomain Protein
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Homeodomain Proteins
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Nuclear Proteins
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Peptide Fragments
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Proto-Oncogene Proteins
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Transcription Factors
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Tumor Suppressor Protein p53
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MDM2 protein, human
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Proto-Oncogene Proteins c-mdm2