Development of IWP-related compounds as selective wt/mutCK1d/e inhibitors, characterization in vitro and in vivo in animal models for their use in new anticancer concepts

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The aims of the present application are development and optimization of novel Casein Kinase 1 (CK1) d/e isoform/mutant-specific inhibitors, and their biological characterization in vitro, including tumor cultures, and in vivo using animal models. CK1 isoforms are known for being key regulators of diverse cellular processes. Alterations in the activity and expression of CK1d/e isoforms are linked to the development of several diseases, including neurodegenerative disorders and cancer. This evidence makes CK1isoforms attractive and promising therapeutic drug targets. The discovery and analysis of novel treatments, including active small molecule inhibitors, is of fundamental importance for cancer research and could be integrated into innovative cancer therapy concepts. Potential new compounds could prove beneficial in the case of aggressive tumor entities with high resistance to chemo/radiotherapy and high mutational rates, like triple negative breast cancer, where the reduced effectiveness of conventional treatments is responsible for high mortality rates. We expect to identify novel small molecule inhibitors with therapeutic potential which could contribute to a significant improvement in current treatment concepts for aggressive tumor entities.