Inhibitor Selectivity for Cyclin‐Dependent Kinase 7: A Structural, Thermodynamic, and Modelling Study

Deregulation of the cell cycle by mechanisms that lead to elevated activities of cyclin‐dependent kinases (CDK) is a feature of many human diseases, cancer in particular. We identified small‐molecule inhibitors that selectively inhibit CDK7, the kinase that phosphorylates cell‐cycle CDKs to promote...

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Veröffentlicht in:	ChemMedChem 2017-03, Vol.12 (5), p.372-380
Hauptverfasser:	Hazel, Pascale, Kroll, Sebastian H. B., Bondke, Alexander, Barbazanges, Marion, Patel, Hetal, Fuchter, Matthew J., Coombes, R Charles, Ali, Simak, Barrett, Anthony G. M., Freemont, Paul S.
Format:	Artikel
Sprache:	eng
Schlagworte:	Amino Acid Sequence Binding Sites Calorimetry cancer CDK7 Cyclin-Dependent Kinase 2 - antagonists & inhibitors Cyclin-Dependent Kinase 2 - genetics Cyclin-Dependent Kinase 2 - metabolism Cyclin-Dependent Kinase-Activating Kinase Cyclin-Dependent Kinases - antagonists & inhibitors Cyclin-Dependent Kinases - genetics Cyclin-Dependent Kinases - metabolism drug discovery Humans isothermal titration calorimetry Molecular Dynamics Simulation Molecular Sequence Data Mutagenesis, Site-Directed Protein Binding Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - metabolism protein kinases Protein Structure, Tertiary Recombinant Proteins - biosynthesis Recombinant Proteins - chemistry Recombinant Proteins - isolation & purification Sequence Alignment Thermodynamics
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