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 certain DCLK1 isoforms are overexpressed in many cancers and not normal cells, targeting the expression or kinase activity of DCLK1 has the potential to 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.

Automated summary

DCLK1 has emerged as a unique stem cell marker in gastrointestinal tissues, promoting tissue regeneration and serving as potential cancer stem cells. Targeting the expression or kinase activity of DCLK1, which is overexpressed in many cancers, has the potential to inhibit cancer cell growth. This review summarizes the evidence for DCLK1 as a prospective cancer target and discusses the challenges and progress in developing small molecule inhibitors of DCLK1.