Unexpected Binding Mode of a Potent Indeno[1,2-b]indole-Type Inhibitor of Protein Kinase CK2 Revealed by Complex Structures with the Catalytic Subunit CK2α and Its Paralog CK2α′

Unexpected Binding Mode of a Potent Indeno[1,2-b]indole-Type Inhibitor of Protein Kinase CK2 Revealed by Complex Structures with the Catalytic Subunit CK2α and Its Paralog CK2α′

Protein kinase CK2, a member of the eukaryotic protein kinase superfamily, is associated with cancer and other human pathologies and thus an attractive drug target. The indeno[1,2-b]indole scaffold is a novel lead structure to develop ATP-competitive CK2 inhibitors. Some indeno[1,2-b]indole-based CK...

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Bibliographic Details
Main Authors: Jennifer Hochscherf, Dirk Lindenblatt, Benedict Witulski, Robin Birus, Dagmar Aichele, Christelle Marminon, Zouhair Bouaziz, Marc Le Borgne, Joachim Jose, Karsten Niefind
Format: Article
Language:English
Published: MDPI AG 2017-12-01
Series:Pharmaceuticals
Subjects:
protein kinase CK2
casein kinase 2
paralogous isoforms CK2α and CK2α′
indeno[1,2-b]indole scaffold
membrane permeability
ATP-competitive inhibitors
dual inhibitors
Online Access:https://www.mdpi.com/1424-8247/10/4/98

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https://www.mdpi.com/1424-8247/10/4/98

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