Bioorganic & medicinal chemistry letters
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Bioorg. Med. Chem. Lett. · May 2010
Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta.
CK1 and gamma-secretase are interesting targets for therapeutic intervention in the treatment of cancer and Alzheimer's disease. The CK1 inhibitor IC261 was reported to inhibit gamma-secretase activity. ⋯ The most active compounds were investigated on CK1delta activity. These findings exclude a direct influence of CK1delta on gamma-secretase, because any change in the substitution pattern of IC261 diminished CK1 inhibition, whereas gamma-secretase inhibition is still exerted by several analogues.