Peptides and Peptidomimetics with Structural Similarity to Human p53 that Activate p53 Function
AssigneesBayer Aktiengesellschaft, The Wistar Institute
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 of select tumor-derived p53 mutants. Pharmaceutical compositions of the compounds of the invention and methods of using these compositions therapeutically are also provided.
Claims4
A peptidomimetic of a peptide which competes with an endogenous p53 negative regulatory region for binding with a negative regulatory region NRR1 comprising residues 361-383 of p53 or NRR2 comprising residues 300-321 of p53, said peptidomimetic containing at least four sequential amino acids from a negative regulatory region which maps to residues 361-383 (SEQ ID NO. 2) of p53, said peptide not being a subfragment of human p53, wherein said peptide activates, in a p53 DNA binding assay, DNA binding of wild-type p53 or a p53 mutant.
Dependencies are inferred from the claim text.