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Targeting Cyclin-Dependent Kinases and Cell Cycle Progression in Human Cancers.
Seminars in Oncology, 2015Uncontrolled cell division is a defining characteristic of cancer cells. Cyclin-dependent kinases (Cdks) are critical regulators of cell cycle progression. Deregulated Cdk activities as a result of gene amplification, translocation, or point mutations of
L. Santo, K. Siu, N. Raje
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Inhibitors of cyclin-dependent kinase and cancer
Journal of Molecular Medicine, 1995Recent research has yielded a dramatic increase in the number of connections between oncogenesis and the proteins which regulate the cell cycle. Three classes of protein which inhibit the activity of cyclin-dependent kinases (CDKs) have emerged as potential targets for oncogenic inactivation.
Andrew S. Kraft, Joseph R. Biggs
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Designing Inhibitors of Cyclin-Dependent Kinases
Annual Review of Pharmacology and Toxicology, 2002Cyclin-dependent kinases (cdks) play a pivotal role in controlling progression through the cell cycle. The complex mechanisms that control cdks have been elucidated and, in the case of cdk2, explained with reference to X-ray crystal structures of the catalytically active and inactive kinase.
Bernard T. Golding +2 more
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Distinct roles for cyclin-dependent kinases in cell cycle control.
Science, 1993The key cell-cycle regulator Cdc2 belongs to a family of cyclin-dependent kinases in higher eukaryotes. Dominant-negative mutations were used to address the requirement for kinases of this family in progression through the human cell cycle.
S. V. D. Heuvel, E. Harlow
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Cyclin dependent kinase activating kinases
Current Opinion in Cell Biology, 1996The cyclin dependent kinase activating kinase (CAK) has roles in both cell cycle regulation and transcription. CAK assembly is regulated either by additional protein binding or by phosphorylation. A recent comparison of this kinase from two yeast species shows that different proteins perform distinct roles and that the most studied CAK may function ...
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Targets of the cyclin-dependent kinase Cdk1
Nature, 2003The events of cell reproduction are governed by oscillations in the activities of cyclin-dependent kinases (Cdks). Cdks control the cell cycle by catalysing the transfer of phosphate from ATP to specific protein substrates. Despite their importance in cell-cycle control, few Cdk substrates have been identified.
Jeffrey A. Ubersax +12 more
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Cyclin-Dependent Kinase Inhibition by Flavoalkaloids
Mini-Reviews in Medicinal Chemistry, 2012Chromone alkaloids and flavoalkaloids are an important group of natural products possessing promising medicinal properties. A chromone alkaloid rohitukine is a major bioactive chemical constituent of plant Dysoxylum binectariferum (Meliaceae) Hook. which is phylogenetically related to the Ayurvedic plant, D. malabaricum Bedd.
Shreyans K. Jain +2 more
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Quinazolines as cyclin dependent kinase inhibitors
Bioorganic & Medicinal Chemistry Letters, 2001Quinazolines have been identified as inhibitors of CDK4/D1 and CDK2/E. Aspects of the SAR were investigated using solution-phase, parallel synthesis. An X-ray crystal structure was obtained of quinazoline 51 bound in CDK2 and key interactions within the ATP binding pocket are defined.
Haiying Chen +14 more
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Identification of substrates for cyclin dependent kinases
Advances in Enzyme Regulation, 2010Protein phosphorylation is a key regulatory mechanism for cell cycle control in eukaryotes. From yeast to humans, cell cycle progression and cell division require the activation of a group of serine– threonine protein kinases called cyclin dependent kinases (CDKs) (Morgan, 1997), which initiate and coordinate these processes by orderly phosphorylation ...
Krupa Deshmukh +4 more
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