Abstract
The central role of cyclin-dependent kinases (CDKs) in cell cycle regulation makes them a promising target for discovering small inhibitory molecules that can modify the degree of cell proliferation. The three-dimensional structure of CDK2 provides a structural foundation for understanding the mechanisms of activation and inhibition of CDK2 and for the discovery of inhibitors. In this article five structures of human CDK2 are summarised: apoprotein, ATP complex, olomoucine complex, isopentenyladenine complex, and des-chloro-flavopiridol complex.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, Non-P.H.S.
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Adenine / analogs & derivatives
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Adenine / pharmacology
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Adenosine Triphosphate / chemistry
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Animals
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Binding Sites
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CDC2-CDC28 Kinases*
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Cell Cycle
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Crystallography, X-Ray
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Cyclin-Dependent Kinase 2
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Cyclin-Dependent Kinases / antagonists & inhibitors*
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Cyclin-Dependent Kinases / chemistry*
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Enzyme Activation
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Enzyme Inhibitors / pharmacology
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Flavonoids / pharmacology
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Humans
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Isopentenyladenosine
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Kinetin
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Ligands
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Macromolecular Substances
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Models, Molecular
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Piperidines / pharmacology
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Protein Conformation
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Protein Serine-Threonine Kinases / antagonists & inhibitors*
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Protein Serine-Threonine Kinases / chemistry*
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Purines / pharmacology
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Recombinant Proteins / antagonists & inhibitors
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Recombinant Proteins / chemistry
Substances
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Enzyme Inhibitors
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Flavonoids
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Ligands
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Macromolecular Substances
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Piperidines
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Purines
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Recombinant Proteins
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N(6)-(delta(2)-isopentenyl)adenine
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alvocidib
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olomoucine
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Isopentenyladenosine
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Adenosine Triphosphate
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Protein Serine-Threonine Kinases
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CDC2-CDC28 Kinases
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CDK2 protein, human
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Cyclin-Dependent Kinase 2
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Cyclin-Dependent Kinases
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Adenine
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Kinetin