期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 23, 期 20, 页码 5578-5585出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.08.046
关键词
Kinase inhibitor; p53 Pathway activation; Casein kinase 1; Checkpoint kinase 1
资金
- Cancer Research UK [C483/A10706]
- GACR [P301/11/1678, P206/12/G151]
- RECAMO [CZ.1.05/2.1.00/03.0101]
- MH CZ - DRO (MMCI) [00209805]
- MRC [MC_G1000806] Funding Source: UKRI
- Medical Research Council [MC_G1000806] Funding Source: researchfish
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. (C) 2013 Elsevier Ltd. All rights reserved.
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