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Research Progress of DCLK1 Inhibitors as Cancer Therapeutics

Author(s):

Linna Cheng, Shenzhen Huang, Lijuan Chen, Xiaoyan Dong, Lei Zhang, Chengye Wu, Kaihong Ye, Fengmin Shao*, Zunmin Zhu* and Rick F. Thorne*   Pages 1 - 13 ( 13 )

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.

Keywords:

DCLK1, kinase inhibitor, cancer stem cell marker, structural biology, cancer biomarker, DCX.

Affiliation:

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, Henan Eye Institute, Henan Eye Hospital and Henan Key Laboratory of Ophthalmology and Visual Science, Henan Provincial People's Hospital, Zhengzhou University People’s Hospital, Henan University People's Hospital, Zhengzhou, Henan, 450003, Department of Medical Imaging, Henan Provincial People’s Hospital, Zhengzhou University People’s Hospital, Henan University People's Hospital, Zhengzhou, Henan, 450003, 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, 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, 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, Translational Research Institute, Henan Provincial People’s Hospital, Academy of Medical Science, Zhengzhou University, No.7, WeiWu Road, Zhengzhou, 450003, Henan, Translational Research Institute, Henan Provincial People’s Hospital, Academy of Medical Science, Zhengzhou University, No.7, WeiWu Road, Zhengzhou, 450003, Henan, 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, Translational Research Institute, Henan Provincial People’s Hospital, Academy of Medical Science, Zhengzhou University, No.7, WeiWu Road, Zhengzhou, 450003, Henan



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