Polaris uses rational structure-based drug design to develop novel structural classes of small molecule inhibitors of Casein kinase 2 (CK2). This is an early stage project which Polaris is pursuing for use as an anticancer agent. These novel classes of CK2α inhibitors are being tested in animal models for efficacy, and initial patent applications have been filed worldwide.
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.