Casein kinase 2 (CK2) inhibitor is an early development stage small molecule inhibitor project. Polaris is developing a small molecule inhibitor of CK2 for use as an anticancer agent.
Recent evidence has demonstrated that the protein kinase CK2α is important for the growth and survival of cancer cells and consequently is a significant novel target for anticancer chemotherapy. Its activity is involved in the promotion of angiogenesis by the regulation of HIF-1α, a transcription factor that is critical for neovascularization in tumors and response of cancer cells to hypoxic conditions.
CK2α has been shown to be elevated in a wide variety of cancers and to be correlated with aggressive tumor growth. Abolition of the CK2α enzyme's activity through genetic and/or small molecule inhibitor approaches causes cancer cells to enter apoptosis and die.
Polaris has designed novel structural classes of inhibitors for CK2α using a structure-based drug design approach. These novel classes of CK2α inhibitors are being tested in animal models for efficacy, and initial patent applications have been filed worldwide.
Polaris' US Protein Kinase Inhibitors patent (No.7,517,882) was issued April 14, 2009.