发明名称 |
Modulators of DNA cytosine-5 methyltransferase and methods for use thereof |
摘要 |
A synthetic oligonucleotide comprising a C-5 methylcytosine and which recognizes and binds an allosteric site on DNA methyltransferase thereby inhibiting DNA methyltransferase activity is disclosed. Also disclosed is a composition comprising a synthetic oligonucleotide of the invention. The composition is useful for inhibiting DNA methyltransferase activity, thereby inhibiting the methylation of DNA. The composition can be a pharmaceutical composition useful for treating disorders associated with methylation defects, such as cancer and certain developmental disorders. Also disclosed is a method of inhibiting methylation of DNA. The method involves contacting a DCMTase with a synthetic oligonucleotide of the invention in the presence of the DNA, thereby resulting in an enzyme/synthetic oligonucleotide complex. The presence of the complex prevents catalysis, thereby inhibiting DNA methyltransferase activity. Also disclosed is a method of treating a disorder of cell proliferation or development by administering to a subject a synthetic oligonucleotide of the invention. The inhibition of DNA methyltransferase prevents the methylation of DNA thereby treating the disorder of cell proliferation or development.
|
申请公布号 |
US7138384(B1) |
申请公布日期 |
2006.11.21 |
申请号 |
US20000485071 |
申请日期 |
2000.02.03 |
申请人 |
THE REGENTS OF THE UNIVERSITY OF CALIFORNIA |
发明人 |
REICH NORBERT O.;FLYNN JAMES |
分类号 |
A01N43/04;A61K31/70;A61K38/00;C12N15/113 |
主分类号 |
A01N43/04 |
代理机构 |
|
代理人 |
|
主权项 |
|
地址 |
|