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Druggability of the CK2 inhibitor CX-4945 as an anticancer drug and beyond

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Abstract

Casein kinase 2 (CK2) is involved in multiple cellular processes such as proliferation, apoptosis, and cell cycle. In particular, its over-expression in human cancers is associated with angiogenesis and tumor progression. As a first orally bioavailable small molecule inhibitor of CK2, CX-4945 exerts anti-proliferative activity in human cancer cells by inhibiting the cell cycle and the PI3K/Akt signaling pathway. Additionally, CX-4945 reduces angiogenesis via blockade of hypoxia-inducible factor-1α transcription and suppresses the inflammatory interleukin-6 production in human breast cancer cells. These effects are supported by results from mouse xenograft model investigations. Here, we discuss the druggability of CX-4945 and its potential to be developed as an anti-cancer drug in clinical trials.

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Correspondence to Seong Hwan Kim.

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Edited by Donghak Kim, Department of Biological Sciences, Konkuk University, Seoul 143-701, Korea Tel: 82-2-450-3366 E-mail: donghak@konkuk.ac.kr

Seong Hwan Kim Principle Researcher Laboratory of Translational Therapeutics, Pharmacology Research Center, Korea Research Institute of Chemical Technology 1991∼1995 Sungkyunkwan University, Biochemistry, BA 1997∼1999 Sungkyunkwan University, Biochemistry, MS 1999∼2002 University of Vienna, Austria, Biochemistry, PhD Main Research Areas Cancer Biology (Autophagy, EMT, Metastasis, First-in-Class Target study) Bone Biology for Developing Anti-Osteoporotic Drugs

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Kim, J., Kim, S.H. Druggability of the CK2 inhibitor CX-4945 as an anticancer drug and beyond. Arch. Pharm. Res. 35, 1293–1296 (2012). https://doi.org/10.1007/s12272-012-0800-9

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