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Bioorg Med Chem Lett. 2013 Oct 15;23(20):5578-85. doi: 10.1016/j.bmcl.2013.08.046. Epub 2013 Aug 16.

A Casein kinase 1/Checkpoint kinase 1 pyrazolo-pyridine protein kinase inhibitor as novel activator of the p53 pathway.

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p53 Signal Transduction Group, University of Edinburgh Cancer Research Centre in the Institute of Genetics and Molecular Medicine, Crewe Road South, Edinburgh EH4 2XR, United Kingdom.


Reactivation of the wild-type p53 pathway is one key goal aimed at developing targeted therapeutics in the cancer research field. Although most p53 protein kinases form 'p53-activating' signals, there are few kinases whose action can contribute to the inhibition of p53, as Casein kinase 1 (CK1) and Checkpoint kinase 1 (CHK1). Here we report on a pyrazolo-pyridine analogue showing activity against both CK1 and CHK1 kinases that lead to p53 pathway stabilisation, thus having pharmacological similarities to the p53-activator Nutlin-3. These data demonstrate the emerging potential utility of multivalent kinase inhibitors.


Casein kinase 1; Checkpoint kinase 1; Kinase inhibitor; p53 Pathway activation

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