Therapeutic targeting of proteolytic cleavage of the mixed lineage leukemia gene product (MLL1) by taspase1 using kinase inhibitors

    公开(公告)号:US11071727B2

    公开(公告)日:2021-07-27

    申请号:US16257581

    申请日:2019-01-25

    IPC分类号: A61K31/4375 A61P35/02

    摘要: Disclosed are methods and pharmaceutical compositions for treating a cancer in a subject in need thereof, the cancer characterized by proteolytic cleavage by taspase1 of the mixed-lineage leukemia 1 gene product (MLL1), the method comprising administering to the subject a therapeutic agent that inhibits cleavage by taspase1 of MLL1. Suitable therapeutic agents may include agents that inhibit the kinase activity of casein kinase II (CKII). Cancer treated by the disclosed methods and pharmaceutical compositions may include leukemia such as Acute Lymphoblastic Leukemia (ALL) and/or Acute Myeloid Leukemia (AML) and in particular, leukemia characterized by rearrangements in MLL1.

    THERAPEUTIC TARGETING OF THE BAP1 COMPLEX IN CANCER

    公开(公告)号:US20210060001A1

    公开(公告)日:2021-03-04

    申请号:US16931942

    申请日:2020-07-17

    摘要: Disclosed are methods for methods, compounds, and compositions for treating cancers characterized by therapeutic targeting of the BAP1 histone H2A deubiquitinase (DUB) complex, otherwise referred to herein as the BAP1 complex. In particular, the methods, compounds, and compositions disclosed herein relate to the use of therapeutic agents that inhibit the biological activity of the BAP1 complex for treating cancers such as myeloid neoplasms.