Universität zu Köln

Guerra, Barbara ORCID: 0000-0003-1136-2413, Rasmussen, Tine D. L., Schnitzler, Alexander, Jensen, Hans H., Boldyreff, Brigitte S., Miyata, Yoshihiko, Marcussen, Niels, Niefind, Karsten ORCID: 0000-0002-0183-6315 and Issinger, Olaf-Georg (2015). Protein kinase CK2 inhibition is associated with the destabilization of HIF-1 alpha in human cancer cells. Cancer Lett., 356 (2). S. 751 - 762. CLARE: ELSEVIER IRELAND LTD. ISSN 1872-7980

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Abstract

Screening for protein kinase CK2 inhibitors of the structural diversity compound library (DTP NCl/NIH) led to the discovery of 4-[(E)-(fluoren-9-ylidenehydrazinylidene)-methyl]benzoic acid (E9). E9 induces apoptotic cell death in various cancer cell lines and upon hypoxia, the compound suppresses CK2-catalyzed HSP90/Cdc37 phosphorylation and induces HIF-1 alpha degradation. Furthermore, E9 exerts a strong anti-tumour activity by inducing necrosis in murine xenograft models underlining its potential to be used for cancer treatment in future clinical studies. Crystal structure analysis of human and maize CK2 alpha in complex with E9 reveals unique binding properties of the inhibitor to the enzyme, accounting for its affinity and selectivity. (C) 2014 Elsevier Ireland Ltd. All rights reserved.

Item Type:	Journal Article
Creators:	Creators Email ORCID ORCID Put Code Guerra, Barbara UNSPECIFIED orcid.org/0000-0003-1136-2413 UNSPECIFIED Rasmussen, Tine D. L. UNSPECIFIED UNSPECIFIED UNSPECIFIED Schnitzler, Alexander UNSPECIFIED UNSPECIFIED UNSPECIFIED Jensen, Hans H. UNSPECIFIED UNSPECIFIED UNSPECIFIED Boldyreff, Brigitte S. UNSPECIFIED UNSPECIFIED UNSPECIFIED Miyata, Yoshihiko UNSPECIFIED UNSPECIFIED UNSPECIFIED Marcussen, Niels UNSPECIFIED UNSPECIFIED UNSPECIFIED Niefind, Karsten UNSPECIFIED orcid.org/0000-0002-0183-6315 UNSPECIFIED Issinger, Olaf-Georg UNSPECIFIED UNSPECIFIED UNSPECIFIED
URN:	urn:nbn:de:hbz:38-414291
DOI:	10.1016/j.canlet.2014.10.026
Journal or Publication Title:	Cancer Lett.
Volume:	356
Number:	2
Page Range:	S. 751 - 762
Date:	2015
Publisher:	ELSEVIER IRELAND LTD
Place of Publication:	CLARE
ISSN:	1872-7980
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 REGULATORY BETA-SUBUNIT; CATALYTIC-SUBUNIT; CRYSTAL-STRUCTURE; HIF-1 ALPHA; HYPOXIA; DRUG; HSP90; ACTIVATION; CHAPERONE; INSIGHTS Multiple languages Oncology Multiple languages
Refereed:	Yes
URI:	http://kups.ub.uni-koeln.de/id/eprint/41429