Discovery of holoenzyme-disrupting chemicals as substrate-selective CK2 inhibitors

CK2 is a constitutively active protein kinase overexpressed in numerous malignancies. Interaction between CK2α and CK2β subunits is essential for substrate selectivity. The CK2α/CK2β interface has been previously targeted by peptides to achieve functional effects; however, no small molecules modulat...

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Veröffentlicht in:	Scientific reports 2019-11, Vol.9 (1), p.15893-16, Article 15893
Hauptverfasser:	Kufareva, Irina, Bestgen, Benoit, Brear, Paul, Prudent, Renaud, Laudet, Béatrice, Moucadel, Virginie, Ettaoussi, Mohamed, Sautel, Celine F., Krimm, Isabelle, Engel, Matthias, Filhol, Odile, Borgne, Marc Le, Lomberget, Thierry, Cochet, Claude, Abagyan, Ruben
Format:	Artikel
Sprache:	eng
Schlagworte:	119/118 13/51 13/62 13/95 140/131 631/154/555 631/154/556 631/92/275 692/4017 692/4028/67/1059/602 82/6 96/34 96/98 Adenosine Triphosphate - metabolism Apoptosis Binding Sites Biochemistry, Molecular Biology Breast cancer Casein Kinase II - antagonists & inhibitors Casein Kinase II - metabolism Catalytic Domain Cell Line, Tumor Cell Movement - drug effects Cell Proliferation - drug effects Chemical Sciences Computer applications Crystallography Crystallography, X-Ray Fumigation Holoenzymes - chemistry Holoenzymes - metabolism Humanities and Social Sciences Humans Inhibitors Kinases Kinetics Life Sciences Medication Medicinal Chemistry Molecular Docking Simulation multidisciplinary NMR Nuclear magnetic resonance Peptides Peptides - chemistry Peptides - metabolism Pharmaceutical sciences Pharmacology Phosphorylation Protein kinase Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - metabolism Protein Kinase Inhibitors - pharmacology Protein structure Protein Subunits - antagonists & inhibitors Protein Subunits - metabolism Science Science (multidisciplinary) Structural Biology Substrate Specificity Substrates Surface Plasmon Resonance
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