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Cyclin-dependent kinases as targets for cancer therapy
Update on Cancer Therapeutics, 2003Cell cycle perturbations are commonly observed in human malignancies. Exploiting this finding is the rationale for the development of CDK inhibitors as anti-tumor agents. Single-agent evaluation of several CDKIs has demonstrated limited clinical activity.
Gary K. Schwartz, Manish A. Shah
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Targets of cyclin-dependent protein kinases
Current Opinion in Cell Biology, 1993Our current understanding of the eukaryotic cell cycle attributes a key regulatory role to cyclin-dependent protein kinases. It is important, therefore, to identify the physiological substrates of these kinases, and to understand how the phosphorylation of such proteins promotes cell cycle progression.
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Smad3 phosphorylation by cyclin-dependent kinases
Cytokine & Growth Factor Reviews, 2006Smad3, a key mediator for TGF-beta antiproliferative responses, is phosphorylated by both CDK4 and CDK2 in vivo and in vitro. Except for the Rb family members, Smad3 is the only CDK4 substrate demonstrated so far. CDK phosphorylation of Smad3 inhibits its transcriptional activity and antiproliferative function.
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The dynamics of cyclin dependent kinase structure
Current Opinion in Cell Biology, 1996In the past year, several new crystal structures have provided exciting insights into the conformational changes underlying the regulation of cyclin-dependent kinases. We now understand the structural basis of many of the mechanisms by which cyclin-dependent kinases are regulated, including activation by cyclin binding and phosphorylation, inhibition ...
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Measuring Cyclin-Dependent Kinase Activity
2004The activity of cyclin-dependent kinases (CDKs) lies at the heart of cell cycle and checkpoint control. These complexes have been called the "cell cycle engine," as it is their enzymatic activity that pushes the cells through the cell-division cycle.
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Cyclin-dependent protein serine/threonine kinase inhibitors as anticancer drugs.
Pharmacological Research, 2019R. Roskoski
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Deletions of the cyclin-dependent kinase-4 inhibitor gene in multiple human cancers
Nature, 1994T. Nobori+5 more
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Cyclin dependent kinase (CDK) inhibitors as anticancer drugs.
Bioorganic & Medicinal Chemistry Letters, 2015Concha Sánchez-Martínez+3 more
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