Research Progress of DCLK1 Inhibitors as Cancer Therapeutics.

Doublecortin-like kinase 1 (DCLK1) has emerged over the last decade as a unique stem cell marker within gastrointestinal tissues. Evidence from mouse models shows that high Dclk1 expression denotes a population of cells that promote tissue regeneration and serve as potential cancer stem cells. Moreover, since specific DCLK1 isoforms are overexpressed in many cancers and not normal cells, targeting the expression or kinase activity of DCLK1 can inhibit cancer cell growth. Here we review the evidence for DCLK1 as a prospective cancer target, including its isoform-specific expression and mutational status in human cancers. We further discuss the challenges and current progress in the development of small-molecule inhibitors of DCLK1.