Protein kinase CK2 inhibition is associated with the destabilization of HIF-1α in human cancer cells

Highlights • We have identified a novel highly potent protein kinase CK2 inhibitor. • Necrotic cell death has been observed in tumour-bearing mice upon treatment with the inhibitor. • The compound interferes with the stable expression of HIF-1a under hypoxia in different cancer cell lines. • Elucida...

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Veröffentlicht in:	Cancer letters 2015-01, Vol.356 (2), p.751-761
Hauptverfasser:	Guerra, Barbara, Rasmussen, Tine D.L, Schnitzler, Alexander, Jensen, Hans H, Boldyreff, Brigitte S, Miyata, Yoshihiko, Marcussen, Niels, Niefind, Karsten, Issinger, Olaf-Georg
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Benzoates - pharmacology Blotting, Western Casein Kinase II - antagonists & inhibitors Cell Cycle - drug effects Cell Proliferation - drug effects Combinatorial Chemistry Techniques Female Fluorenes - pharmacology Fluorescent Antibody Technique Hematology, Oncology and Palliative Medicine HIF-1α Humans Hypoxia-Inducible Factor 1, alpha Subunit - chemistry Hypoxia-Inducible Factor 1, alpha Subunit - metabolism Immunoenzyme Techniques Kinase inhibitors Luciferases - metabolism Mice Mice, Nude Murine xenograft Neoplasms - drug therapy Neoplasms - enzymology Neoplasms - pathology Phosphorylation - drug effects Protein Conformation - drug effects Protein kinase CK2 Protein Kinase Inhibitors - pharmacology Signal Transduction - drug effects Tumor Cells, Cultured Xenograft Model Antitumor Assays
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Zusammenfassung:	Highlights • We have identified a novel highly potent protein kinase CK2 inhibitor. • Necrotic cell death has been observed in tumour-bearing mice upon treatment with the inhibitor. • The compound interferes with the stable expression of HIF-1a under hypoxia in different cancer cell lines. • Elucidation of the CK2 structure in the presence of the compound reveals unique binding properties not reported before.
ISSN:	0304-3835 1872-7980
DOI:	10.1016/j.canlet.2014.10.026