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US 9,789,121 B2Granted
Small molecules that replace or agonize p53 function
AssigneeBuck Institute
InventorsShahrooz Rabizadeh, Kayvan R. Niazi, Dale E. Bredesen
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Abstract
This invention provides a novel screening system for identifying p53 mimetics/agonists. Also provided are small organic molecules that act as effective p53 mimetics/agonists.
Claims4
A kit comprising a compound of Formula I and a cell for screening for agents that promote cell death in a p53 naive cell, wherein said cell is an HEK293T cell containing a nucleic acid construct comprising a promoter element comprising at least a portion of SEQ ID NO:
- 1, wherein the promoter element is operably coupled to a reporter, wherein the compound of Formula I is a p53 mimetic and has a structure according to Formula I and wherein the compound of Formula I is present in an amount effective to induce or increase transcription of said reporter,
- wherein R1 and R4 are independently selected from the group consisting of an amino group, a cyano group, a nitro group, a carboxyl group, halo, hydroxyl, SO2, C1-6 alkyl, C1-6haloalkyl, C1-8 alkoxyl, C1-11 alkoxyalkyl, C1-6 alkylamino, and C1-6 aminoalkyl;
- R2 and R3 are independently selected from the group consisting of CH and N;
- R5 is CH2 or O;
- R6 and R7 are independently halogen;
- R8 is selected from the group consisting of NO2, OH, and COOH;
- and
- R9 is selected from the group consisting of H, CH3.
5 more elements
Dependencies are inferred from the claim text.