Stemness serine-threonine kinases

Stemness serine-threonine kinases represent a functional group of enzymes that are critical for the maintenance, self-renewal, and survival of cancer stem cells (CSCs). This group includes several distinct kinases such as STK33, STK17A, NEK2, HASPIN, DYRK1A, DYRK1B, AURKA, AURKB, and PLK1, which collectively modulate the activity of master pluripotency transcription factors, most notably Nanog, Oct4, and Sox2. By phosphorylating these factors or their upstream regulators, such as beta-catenin, these kinases promote a stem-like phenotype that allows cancer cells to resist standard chemotherapy and radiation, undergo epithelial-mesenchymal transition (EMT), and drive tumor recurrence and metastasis. Targeting this group of kinases is a therapeutic strategy aimed at eradicating the CSC population, which is often the root cause of treatment failure in advanced malignancies. Amcasertib (BBI-503) is the lead clinical-stage small molecule inhibitor designed to target these kinases, demonstrating the potential to disrupt the survival pathways of tumor-initiating cells across various solid tumors.

Other names

Cancer stemness kinasesStemness kinasesCSC kinasesCancer stem cell kinases

Inhibition of multiple serine-threonine kinases that regulate the expression, stability, and transcriptional activity of cancer stem cell pluripotency factors such as Nanog, Oct4, and Sox2.