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

…, S Lewis, Y Huang, B Vojtesek, C Kettleborough…

Index: Huart, Anne-Sophie; Saxty, Barbara; Merritt, Andy; Nekulova, Marta; Lewis, Stephen; Huang, Yide; Vojtesek, Borivoj; Kettleborough, Catherine; Hupp, Ted R. Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 20 p. 5578 - 5585

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Citation Number: 4

Abstract

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 ...