IP Library › Granted Patent US 9,737,546
Granted Patent B2
US 9,737,546 · App. 14/910,976 · Granted Aug 22, 2017

Small molecules to enhance P53 activity

Inventors: Rommie E. Amaro (San Clemente, CA); Roberta Baronio (Oxford, GB); Ozlem Demir (San Diego, CA); Peter Kaiser (Irvine, CA); Richard H. Lathrop (Irvine, CA); Seyedey-Faezeh Salehi-Amin (Pasadena, CA); Christopher D. Wassman (San Francisco, CA)
Assignee: The Regents of the University of California
A61K31/538A61K31/416A61K31/4155A61K31/4184A61K31/429A61K31/44A61K31/47A61K31/472A61K31/4704A61K45/06C07D213/75C07D215/38C07D217/24C07D231/54C07D265/36C07D405/04C07D513/04
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Quick Facts
Patent No.
US 9,737,546
App. No.
14/910,976
Granted
Aug 22, 2017
Kind
B2
Abstract

A method of enhancing p53 activity of a p53 mutant polypeptide is provided. The method includes interacting a compound to an open L1/S3 binding site of the p53 mutant polypeptide, where the p53 activity of the p53 mutant polypeptide is enhanced in the presence of the compound. Compounds were identified from databases of compounds for virtual drug screening. Methods of screening for compounds that enhance p53 activity by binding to the open L1/S3 binding site, and methods of treatment using the identified compounds, are also provided.

Claims (4)

1. A method of enhancing p53 activity of a p53 mutant polypeptide, comprising directly interacting the p53 mutant polypeptide with at least one compound, or a tautomer or pharmaceutically acceptable salt thereof, wherein the at least one compound is selected from the group consisting of:

and a combination thereof,

wherein X − is a counterion, and the p53 activity of the p53 mutant polypeptide is enhanced in the presence of the at least one compound as compared to its absence.

2. The method of claim 1 , wherein the at least one compound is one of the following compounds, or a combination thereof:

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 28, 2016
From: AMARO, ROMMIE E.; BARONIO, ROBERTA; DEMIR, OZLEM; KAISER, PETER; LATHROP, RICHARD H.; SALEHI-AMIRI, SEYEDEH-FAEZEH; WASSMAN, CHRISTOPHER D.
To: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
Reel/Frame 038555/0492 →
Continuity (2)
Provisional Application 61864441 · Aug 9, 2013
Related Publication 20160193214A1 · Jul 7, 2016