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:
CreatorsEmailORCIDORCID Put Code
Lindenblatt, DirkUNSPECIFIEDorcid.org/0000-0002-5561-1082UNSPECIFIED
Nickelsen, AnnaUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Applegate, Violetta M.UNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Jose, JoachimUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Niefind, KarstenUNSPECIFIEDorcid.org/0000-0002-0183-6315UNSPECIFIED
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: Unspecified
Divisions: Unspecified
Subjects: no entry
Uncontrolled Keywords:
KeywordsLanguage
CRYSTAL-STRUCTURE; SUBUNIT; BINDING; CK2-ALPHA'; ASSAYMultiple languages
Chemistry, MedicinalMultiple languages
URI: http://kups.ub.uni-koeln.de/id/eprint/32580

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