Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10587588 | Bioorganic & Medicinal Chemistry Letters | 2013 | 8 Pages |
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.
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Authors
Anne-Sophie Huart, Barbara Saxty, Andy Merritt, Marta Nekulova, Stephen Lewis, Yide Huang, Borivoj Vojtesek, Catherine Kettleborough, Ted R. Hupp,