- 专利标题: Therapeutic targeting of casein kinase 1δ in breast cancer
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申请号: US15768257申请日: 2016-10-05
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公开(公告)号: US10603322B2公开(公告)日: 2020-03-31
- 发明人: William R. Roush , Derek R. Duckett , John L. Cleveland , Laura H. Rosenberg
- 申请人: The Scripps Research Institute
- 申请人地址: US CA La Jolla
- 专利权人: The Scripps Research Institute
- 当前专利权人: The Scripps Research Institute
- 当前专利权人地址: US CA La Jolla
- 代理商 Hugh Wang; Thomas Fitting
- 国际申请: PCT/US2016/055436 WO 20161005
- 国际公布: WO2017/066055 WO 20170420
- 主分类号: A61K31/5377
- IPC分类号: A61K31/5377 ; A61P35/00 ; C12Q1/6886
摘要:
The invention provides a method of inhibiting casein kinase 1δ (CK1δ), comprising contacting the CK1δ with a compound of formula (I), as defined herein; such as compound SR-3029. We demonstrate that CSNK1D is amplified and/or overexpressed in human breast tumors and that CK1δ can be medically targeted in human breast cancer subtypes overexpressing this kinase. The invention further provides a method of treating cancer, such as a breast cancer, melanoma, glioblastoma, medulloblastoma, renal, bladder or colon cancer, or a cancer that metastasizes to the brain, lung, or bone provided that both elevated CK1δ and β-catenin dependence are involved in those metastatic diseases. The cancer can be a breast cancer of the triple negative subclass of breast cancers (TNBC), or can be an HER+ breast cancer.
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