Universität zu Köln

Lindenblatt, Dirk ORCID: 0000-0002-5561-1082, Nickelsen, Anna, Applegate, Violetta M., Jose, Joachim and Niefind, Karsten ORCID: 0000-0002-0183-6315 (2020). Structural and Mechanistic Basis of the Inhibitory Potency of Selected 2-Aminothiazole Compounds on Protein Kinase CK2. J. Med. Chem., 63 (14). S. 7766 - 7773. WASHINGTON: AMER CHEMICAL SOC. ISSN 1520-4804

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Abstract

Selective inhibitors of protein kinase CK2 with significant cytotoxicity on tumor cells based on a 2-aminothiazole scaffold were described recently. Here, these studies are supplemented with representative CK2 alpha/CK2 alpha' complex structures. They reveal that the 2-aminothiazole- based inhibitors occupy the ATP cavity, whereas preliminary data had indicated an allosteric binding site. The crystal structure findings are corroborated by subsequent enzyme kinetic studies; their atomic-resolution quality provides the basis for future optimization of these promising CK2 inhibitors.

Item Type:	Journal Article
Creators:	Creators Email ORCID ORCID Put Code Lindenblatt, Dirk UNSPECIFIED orcid.org/0000-0002-5561-1082 UNSPECIFIED Nickelsen, Anna UNSPECIFIED UNSPECIFIED UNSPECIFIED Applegate, Violetta M. UNSPECIFIED UNSPECIFIED UNSPECIFIED Jose, Joachim UNSPECIFIED UNSPECIFIED UNSPECIFIED Niefind, Karsten UNSPECIFIED orcid.org/0000-0002-0183-6315 UNSPECIFIED
URN:	urn:nbn:de:hbz:38-325800
DOI:	10.1021/acs.jmedchem.0c00587
Journal or Publication Title:	J. Med. Chem.
Volume:	63
Number:	14
Page Range:	S. 7766 - 7773
Date:	2020
Publisher:	AMER CHEMICAL SOC
Place of Publication:	WASHINGTON
ISSN:	1520-4804
Language:	English
Faculty:	Faculty of Mathematics and Natural Sciences
Divisions:	Faculty of Mathematics and Natural Sciences > Department of Chemistry > Institute of Biochemistry
Subjects:	no entry
Uncontrolled Keywords:	Keywords Language CRYSTAL-STRUCTURE; SUBUNIT; BINDING; CK2-ALPHA'; ASSAY Multiple languages Chemistry, Medicinal Multiple languages
Refereed:	Yes
URI:	http://kups.ub.uni-koeln.de/id/eprint/32580