885223-63-2Relevant articles and documents
HPK1 ANTAGONISTS AND USES THEREOF
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Paragraph 1296; 1297, (2021/03/19)
The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of HPK1, and the treatment of HPK1-mediated disorders.
Identification of novel 7-amino-5-methyl-1,6-naphthyridin-2(1H)-one derivatives as potent PI3K/mTOR dual inhibitors
Lin, Songwen,Han, Fangbin,Liu, Peng,Tao, Jing,Zhong, Xuechao,Liu, Xiujie,Yi, Chongqin,Xu, Heng
supporting information, p. 790 - 793 (2014/02/14)
Inhibition of the phosphoinositide 3-kinase (PI3K)/AKT/mammalian target of rapamycin (mTOR) signaling pathway is one of the most intensively studied approaches to cancer therapy. Rational design led to the identification of novel 7-amino-5-methyl-1,6-naph
A Casein kinase 1/Checkpoint kinase 1 pyrazolo-pyridine protein kinase inhibitor as novel activator of the p53 pathway
Huart, Anne-Sophie,Saxty, Barbara,Merritt, Andy,Nekulova, Marta,Lewis, Stephen,Huang, Yide,Vojtesek, Borivoj,Kettleborough, Catherine,Hupp, Ted R.
supporting information, p. 5578 - 5585 (2013/10/01)
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.