Title:Research Progress of DCLK1 Inhibitors as Cancer Therapeutics
Volume: 29
Issue: 13
Author(s): Linna Cheng, Shenzhen Huang, Lijuan Chen, Xiaoyan Dong, Lei Zhang, Chengye Wu, Kaihong Ye, Fengmin Shao*, Zunmin Zhu*Rick F. Thorne*
Affiliation:
- Translational Research Institute, Henan Provincial People’s Hospital,
Academy of Medical Science, Zhengzhou University, No.7, WeiWu Road, Zhengzhou, 450003, Henan, China
- Institute of Hematology, Henan Key Laboratory of Stem Cell Differentiation and Modification, Henan Provincial
People's Hospital, Zhengzhou University People’s Hospital, Henan University People’s Hospital,
Zhengzhou, Henan, 450003, China
- Translational Research Institute, Henan Provincial People’s Hospital,
Academy of Medical Science, Zhengzhou University, No.7, WeiWu Road, Zhengzhou, 450003, Henan, China
Keywords:
DCLK1, kinase inhibitor, cancer stem cell marker, structural biology, cancer biomarker, DCX.
Abstract: 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.