| 发明名称 |
SMALL MOLECULES TO ENHANCE P53 ACTIVITY |
| 摘要 |
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. |
| 申请公布号 |
US2016193214(A1) |
申请公布日期 |
2016.07.07 |
| 申请号 |
US201414910976 |
申请日期 |
2014.08.09 |
| 申请人 |
THE REGENTS OF THE UNIVERSITY OF CALIFORNIA |
发明人 |
Amaro Rommie E.;Baronio Roberta;Demir Ozten;Kaiser Peter;Lathrop Richard H.;Salehi-Amin Seyedeh-Feezeh;Wassman Christopher D. |
| 分类号 |
A61K31/538;A61K45/06;C07D217/24;A61K31/4155;C07D405/04;A61K31/416;C07D231/54;A61K31/429;C07D513/04;A61K31/4704;C07D215/38;C07D265/36;A61K31/44;C07D213/75;A61K31/472 |
主分类号 |
A61K31/538 |
| 代理机构 |
|
代理人 |
|
| 主权项 |
1. A method of enhancing p53 activity of a p53 mutant polypeptide, comprising interacting the p53 mutant polypeptide with at least one compound of the following compounds, or a tautomer, derivative or pharmaceutically acceptable salt thereof, or a combination thereof: wherein the p53 activity of the p53 mutant polypeptide is enhanced in the presence of the at least one compound as compared to its absence. |
| 地址 |
Oakland CA US |
