Inhibition of γ-secretase by the CK1 inhibitor IC261 does not depend on CK1δ

…, K Baumann, R Schubenel, E Winkler, H Steiner…

Index: Hoettecke, Nicole; Liebeck, Miriam; Baumann, Karlheinz; Schubenel, Robert; Winkler, Edith; Steiner, Harald; Schmidt, Boris Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 9 p. 2958 - 2963

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Citation Number: 11

Abstract

CK1 and γ-secretase are interesting targets for therapeutic intervention in the treatment of cancer and Alzheimer's disease. The CK1 inhibitor IC261 was reported to inhibit γ-secretase activity. The question is: Does CK1 inhibition directly influence γ-secretase activity? Therefore we analyzed the SAR of 15 analogues and their impact on γ-secretase activity. The most active compounds were investigated on CK1δ activity. These findings exclude a ...

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