期刊
CELL CHEMICAL BIOLOGY
卷 28, 期 4, 页码 546-+出版社
CELL PRESS
DOI: 10.1016/j.chembiol.2020.12.013
关键词
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资金
- AbbVie [1097737]
- Bayer Pharma AG
- Boehringer Ingelheim
- Canada Foundation for Innovation
- Eshelman Institute for Innovation
- Genome Canada
- Genentech
- Innovative Medicines Initiative (EU/EFPIA) (ULTRA-DD grant) [115766]
- Janssen
- Merck KGaA Darmstadt Germany
- MSD
- Novartis Pharma AG
- Ontario Ministry of Economic Development and Innovation
- Pfizer
- Sao Paulo Research Foundation-FAPESP
- Takeda
- Wellcome [106169/ZZ14/Z]
- NC Biotech Center Institutional Support Grant [2018-IDG-1030]
- NIH [1U24DK116204]
- DOD ALSRP award [AL190107]
- NC Policy Collaboratory at UNC-CH
- NC Coronavirus Relief Fund
- Canadian Institutes of Health Research [37854]
- Natural Sciences and Engineering Research Council of Canada [RGPIN/04186-2014]
A highly potent and cell-active CK2 chemical probe with exclusive selectivity for both human CK2 isoforms was designed, but did not show broad antiproliferative effects in >90% of >140 cell lines tested.
Building on the pyrazolopyrimidine CK2 (casein kinase 2) inhibitor scaffold, we designed a small targeted library. Through comprehensive evaluation of inhibitor selectivity, we identified inhibitor 24 (SGC-CK2-1) as a highly potent and cell-active CK2 chemical probe with exclusive selectivity for both human CK2 isoforms. Remarkably, despite years of research pointing to CK2 as a key driver in cancer, our chemical probe did not elicit a broad antiproliferative phenotype in >90% of >140 cell lines when tested in doseresponse. While many publications have reported CK2 functions, CK2 biology is complex and an available high-quality chemical tool such as SGC-CK2-1 will be indispensable in deciphering the relationships between CK2 function and phenotypes.
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