Journal
ARCHIVES OF PHARMACAL RESEARCH
Volume 35, Issue 8, Pages 1293-1296Publisher
PHARMACEUTICAL SOC KOREA
DOI: 10.1007/s12272-012-0800-9
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Funding
- KRICT's project [SI-1205]
- Ministry of Knowledge Economy, Republic of Korea
- National Research Council of Science & Technology (NST), Republic of Korea [SI-1205] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
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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-1 alpha 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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