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Updated: Oct 29, 2025

Methods for Evaluating the Role of c-Fos and Dusp1 in Oncogene Dependence
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Research Progress of DCLK1 Inhibitors as Cancer Therapeutics

Linna Cheng1, Shenzhen Huang2, Lijuan Chen3

  • 1Institute 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.

Current Medicinal Chemistry
|July 13, 2021
PubMed

Insights

Doublecortin-like kinase 1 (DCLK1) is a stem cell marker promoting regeneration and cancer. Targeting DCLK1 offers a promising strategy for inhibiting cancer growth by exploiting its specific expression in tumors.

Area of Science:

  • Gastrointestinal stem cell biology
  • Cancer biology
  • Molecular oncology

Background:

  • Doublecortin-like kinase 1 (DCLK1) is identified as a key stem cell marker in gastrointestinal tissues.
  • DCLK1 expression is linked to tissue regeneration and cancer stem cell populations in mouse models.
  • Specific DCLK1 isoforms are overexpressed in various cancers, presenting a therapeutic vulnerability.

Purpose of the Study:

  • To review the evidence supporting Doublecortin-like kinase 1 (DCLK1) as a potential cancer therapeutic target.
  • To examine the isoform-specific expression and mutational landscape of DCLK1 in human cancers.
  • To discuss the progress and challenges in developing small molecule inhibitors against DCLK1.

Main Methods:

  • Literature review of studies on DCLK1 in gastrointestinal tissues and cancer.
  • Analysis of DCLK1 isoform expression patterns in normal versus cancerous human tissues.
  • Examination of DCLK1 mutational status across different cancer types.
  • Review of current small molecule inhibitor development for DCLK1.

Main Results:

  • DCLK1 marks stem cells involved in tissue regeneration and cancer stem cell activity.
  • Aberrant expression of specific DCLK1 isoforms is a hallmark of many human cancers.
  • DCLK1 presents a targetable vulnerability due to its differential expression in cancer cells.

Conclusions:

  • DCLK1 is a compelling target for cancer therapy due to its role in stemness and cancer-specific expression.
  • Targeting DCLK1 kinase activity or expression holds potential for inhibiting cancer progression.
  • Development of DCLK1 inhibitors is advancing, though challenges remain in clinical translation.
Keywords:
DCLK1DCXcancer biomarkercancer stem cell markerkinase inhibitorstructural biology

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