Canonical WNT (Wingless/integrase 1) signaling is an important developmental pathway that has attracted increased attention for anti-cancer drug discovery. Researchers at the University of Arizona are investigating utility for the compounds herein for the treatment of colorectal cancer as well as potential disease modifying agents for the treatment of osteoarthritis of the knee. Therapeutic opportunities exist for several malignancies and for neurodegenerative diseases. Background: Several WNT inhibitor molecules are in clinical trials with differing mechanisms of action including porcupine and tankyrase inhibitors. Recently, numerous new biological processes and targets related to the WNT pathway have been discovered. Among these targets, the tyrosine and serine/threonine kinase CLKS have been reported to modulate pre-mRNA splicing and as such modulate WNT activity. There are a reported five CLK inhibitors (often denoted CLK2 inhibitors) in clinical trials for different malignancies and regeneration studies. These small molecules could play a crucial role in the delivery of anti-cancer drugs due to their ability to inhibit cell growth. By just inhibiting CLK pathways the WNT pathway gene expression will be reduced, showing that they play a role with one another. Applications:
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