发明名称 |
BCL6 INHIBITORS AS ANTICANCER AGENTS |
摘要 |
The invention provides compositions and methods for blocking the BCL6 BTB domain with small molecule, non-peptide compounds as disclosed and claimed herein. BCL6 is a transcriptional repressor of the BTB-POZ (brie a brae, tramtrack, broad complex/pox virus zincfinger) family of proteins. It is required for normal development of germinal center (GC) B-cells and is also the most commonly involvedoncogene in diffuse large B-celllymphomas (DLBCLs), and constitutive expression of BCL6 in GC B-cells causes DLBCL in mice. |
申请公布号 |
US2016166549(A1) |
申请公布日期 |
2016.06.16 |
申请号 |
US201414899083 |
申请日期 |
2014.06.16 |
申请人 |
Cornell University ;University of Maryland, Baltimore |
发明人 |
Melnick Ari;Cerchietti Leandro Carlos A.;Cardenas Mariano G.;Xue Fengtian;MacKerell Alexander D. |
分类号 |
A61K31/427;A61K45/06 |
主分类号 |
A61K31/427 |
代理机构 |
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代理人 |
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主权项 |
1. A method of disrupting BCL6 BTB domain interactions with corepressors, in B-cells, comprising exposing the B cells to an effective concentration of a compound that blocks the lateral groove of BCL6. |
地址 |
Ithaca NY US |