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Therapeutic targeting of casein kinase 1deta in breast cancer

A casein kinase, breast cancer technology, applied in the determination/inspection of microorganisms, medical preparations containing active ingredients, drug combinations, etc., can solve problems such as contribution knowledge and obstacles

Inactive Publication Date: 2018-08-21
THE SCRIPPS RES INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the contribution of these kinases to human cancer is poorly understood, and the non-selectivity of previously reported CK1δ / CK1ε inhibitors has hindered the approval of these kinases as anticancer targets (9, 13-15)

Method used

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  • Therapeutic targeting of casein kinase 1deta in breast cancer
  • Therapeutic targeting of casein kinase 1deta in breast cancer
  • Therapeutic targeting of casein kinase 1deta in breast cancer

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Embodiment

[0095] Research design

[0096] This study aims to assess the involvement of CK1δ and CK1ε in human breast cancer and investigate the efficacy of an in-house, highly specific dual CK1δ / CK1ε inhibitor in a preclinical model of human breast cancer. Using five human orthotopic breast xenograft models, pharmacological and genetic studies validate targeting CK1δ in breast cancer subpopulations that overexpress this kinase. Power analysis indicated that n was required to be at least 7 or greater based on the difference in tumor volume between groups and the standard deviation of tumor volume within each group (90% confidence). Therefore, experiments included 7-12 tumor-bearing mice per experimental or control (vehicle) group, where mice were randomized prior to treatment to determine random sampling such that the median tumor size was the same between groups. All tumor sizes were measured throughout the experiment and plotted without excluding any samples. For survival analysis,...

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Abstract

The invention provides a method of inhibiting casein kinase 1 DETA (CK1 DETA), comprising contacting the CK1 DETA 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 CK1 delta 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 CK1 DETA and BETA-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.

Description

[0001] Cross References to Related Applications [0002] This application claims priority to US Provisional Application Serial No. 62 / 240,689, filed October 13, 2015, the disclosure of which is incorporated by reference in its entirety. [0003] Statement of Government Support [0004] This invention was made with Government support under CA175094 by the National Institutes of Health. The government has certain rights in this invention. Background technique [0005] Breast cancer accounts for nearly a quarter of all cancer diagnoses and is the leading cause of cancer-related mortality in women worldwide (1,2). Currently, treatment selection for breast cancer is based on pathological information and histological grade, as well as the expression status of estrogen (ER), progesterone (PR), and epidermal growth factor 2 (HER2 / neu) receptors, in which blocking receptor function Targeted therapy has resulted in improvements in overall survival (1,3). In fact, the expression of E...

Claims

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Application Information

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IPC IPC(8): C07D473/32C07D473/16
CPCA61P35/00A61K31/5377C12Q1/6886C12Q2600/136
Inventor 威廉·R·劳什德里克·R·达克特约翰·L·克利夫兰劳拉·H·罗森伯格
Owner THE SCRIPPS RES INST
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