Title:Research Progress of DCLK1 Inhibitors as Cancer Therapeutics
Volume: 29
Issue: 13
关键词:
DCLK1,激酶抑制剂,癌症干细胞标志物,结构生物学,癌症生物标志物,DCX。
摘要: 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.