Protein kinase CK2 regulates CDC25B phosphatase activity

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چکیده

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Protein kinase CK2.

Protein kinase CK2 is a ubiquitous protein kinase responsible for the phosphorylation of Ser and Thr residues specified by acidic side chains in many proteins, including several key enzymes, growth factor receptors, transcription factors and cytoskeletal proteins. The holoenzyme is composed of two catalytic and two regulatory subunits, the latter having antagonistic roles. CK2 is constitutively...

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Inhibition of CDC25B Phosphatase Through Disruption of Protein–Protein Interaction

CDC25 phosphatases are key cell cycle regulators and represent very attractive but challenging targets for anticancer drug discovery. Here, we explored whether fragment-based screening represents a valid approach to identify inhibitors of CDC25B. This resulted in identification of 2-fluoro-4-hydroxybenzonitrile, which directly binds to the catalytic domain of CDC25B. Interestingly, NMR data and...

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INTRODUCTION Due to its physiological role into promoting cell survival and its dysregulation in most cancer cells, protein kinase CK2 is a relevant physiopathological target for development of chemical inhibitors. We report the discovery of azonaphthalene derivatives, as a new family of highly specific CK2 inhibitors. First, we demonstrated that CK2 inhibition (IC50= 0.4 µM) was highly specifi...

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The New Role for an Old Kinase: Protein Kinase CK2 Regulates Metal Ion Transport

The pleiotropic serine/threonine protein kinase CK2 was the first kinase discovered. It is renowned for its role in cell proliferation and anti-apoptosis. The complexity of this kinase is well reflected by the findings of past decades in terms of its heterotetrameric structure, subcellular location, constitutive activity and the extensive catalogue of substrates. With the advent of non-biased h...

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ژورنال

عنوان ژورنال: Oncogene

سال: 2003

ISSN: 0950-9232,1476-5594

DOI: 10.1038/sj.onc.1206107