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

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

  • Bioorg Med Chem Lett. 2013 Oct 15;23(20):5578-85. doi: 10.1016/j.bmcl.2013.08.046.
Anne-Sophie Huart 1,  Barbara Saxty,  Andy Merritt,  Marta Nekulova,  Stephen Lewis,  Yide Huang,  Borivoj Vojtesek,  Catherine Kettleborough,  Ted R Hupp
Affiliations

Affiliation

  • 1 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.
PMID: 24007918 DOI: 10.1016/j.bmcl.2013.08.046
Abstract

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.

Keywords

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

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