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Current Medicinal Chemistry

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ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

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Review Article

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*

Volume 29, Issue 13, 2022

Published on: 09 July, 2021

Page: [2261 - 2273] Pages: 13

DOI: 10.2174/0929867328666210709110721

Price: $65

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.

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