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AssigneesThe Regents of the University of Colorado, a body corporate, Yale University
InventorsDylan Taatjes, Alanna Schepartz Shrader
Estimating the term…
The invention includes novel systems, methods, and compositions to inhibit TF function by disrupting the TF-Mediator interaction. In this preferred aspect, functional mimics of TF activation domains may be rationally designed to block TF-Mediator binding and selectively inhibited TF-dependent transcription and may further incorporate a penta-arg motif for enhanced cell penetration. In one preferred embodiment of the invention novel stapled mimetic peptides of p53 activation domains incorporating a penta-arg motif were rationally designed to block p53 function by disrupting the p53-Mediator interaction. Additional aspects of the invention include methods of treating cancer in a subject, and other diseases related to the activity of the TFs, such as p53, and the Mediator complex, and its downstream TF-dependent transcription.
A bivalent peptide comprising a mimetic of a first activation domain of a DNA-binding transcription factor (TF) coupled with a second activation domain of said TF, wherein said bivalent peptide inhibits the interaction of the TF and the Mediator complex.
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13-83. (canceled)
A cell penetrating bivalent peptide comprising a mimetic of a first activation domain of a DNA-binding transcription factor (TF) coupled with a second activation domain of said TF, wherein at least one of the first and/or said second activation domains have a penta-arg motif, and wherein said bivalent peptide inhibits the interaction of the TF and the Mediator complex.
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95-97. (canceled)
A bivalent peptide that competitively inhibits the interaction of p53 and the Mediator complex according to amino acid sequence SEQ ID NO. 14.
Dependencies are inferred from the claim text.