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. Moreo...

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Published inCurrent medicinal chemistry Vol. 29; no. 13; p. 2261
Main Authors Cheng, Linna, Huang, Shenzhen, Chen, Lijuan, Dong, Xiaoyan, Zhang, Lei, Wu, Chengye, Ye, Kaihong, Shao, Fengmin, Zhu, Zunmin, Thorne, Rick F
Format Journal Article
LanguageEnglish
Published United Arab Emirates 01.01.2022
Subjects
DCX
kinase inhibitor
structural biology
cancer stem cell marker
cancer biomarker
DCLK1
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Summary: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.
ISSN:1875-533X
DOI:10.2174/0929867328666210709110721