Cancer stemness kinase (CSK)

Cancer stemness kinase (CSK) refers to a specialized class of serine/threonine kinases that are essential for the maintenance, self-renewal, and survival of cancer stem cells (CSCs). These kinases regulate the activity of key transcription factors, such as Nanog, Sox2, and Oct4, which govern the stemness phenotype of tumor cells and contribute to their ability to resist conventional therapies. CSCs are a subpopulation of cells within a tumor responsible for treatment resistance, metastasis, and disease recurrence. By inhibiting these kinases, therapeutic agents like amcasertib (BBI-503) disrupt the signaling pathways required for CSC survival, leading to the exhaustion of the stem cell population and sensitization of the tumor to standard treatments. Amcasertib is an orally bioavailable small molecule that has been investigated in clinical trials for various advanced solid tumors, demonstrating the potential to downregulate stemness-related gene expression and inhibit tumor self-renewal.

Other names

Cancer stem cell pathway serine/threonine kinaseCSC kinaseStemness-maintaining kinaseNanog-regulating kinaseDual specificity tyrosine-phosphorylation-regulated kinase 1A (DYRK1A)Dual specificity tyrosine-phosphorylation-regulated kinase 1B (DYRK1B)

Amcasertib is a small molecule inhibitor that targets cancer stemness kinases, suppressing the expression and activity of stemness-related transcription factors like Nanog, which leads to the depletion of the cancer stem cell population and inhibition of tumor self-renewal.