Peptides and peptidomimetics with structural similarity to human p53 that activate p53 function
AssigneeBayer Aktiengesellschaft
InventorsThanos Halazonetis, Wolfgang Hartwig
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Abstract
The present invention provides peptides and peptidomimetics corresponding to part or to the entirety of the region encompassed by residues 360-386 of human p53, said peptides and peptidomimetics characterized by the ability to activate DNA binding of wild-type p53 and to select tumor-derived p53 mutants. Pharmaceutical compositions of the compounds of the invention and methods of using these compositions therapeutically are also provided.
Claims26
A peptide consisting essentially of at least four sequential amino acids from a negative regulatory region which maps to residues 361-383 of p53, said peptide not being a subfragment of human p53, wherein said peptide activates DNA binding of wild-type p53 or a p53 mutant containing a single amino acid substitution, said mutant selected from the group consisting of p53-ser239, p53-his273, p53-gln248, p53-trp282, and p53-cys273, in a p53 DNA binding assay.
Dependencies are inferred from the claim text.