Longdaysin inhibits Wnt/β-catenin signaling and exhibits antitumor activity against breast cancer

OncoTargets and Therapy
Yanpeng XiongDesheng Lu

Abstract

CK1 is involved in regulating Wnt/β-catenin signaling and represents a promising target for the treatment of breast cancer. A purine derivative longdaysin has recently been identified as a novel modulator of cellular circadian rhythms through targeting the protein kinases CK1δ, CK1α, and ERK2. However, the antitumor activity of longdaysin and its underlying mechanisms remain unclear. The inhibitory effect of longdaysin on Wnt/β-catenin signaling was investigated using the SuperTOPFlash reporter system. The levels of phosphorylated LRP6, total LRP6, DVL2, active β-catenin, and total β-catenin were examined by Western blot. The expression of Wnt target genes was determined using real-time PCR. The ability of colony formation of breast cancer cells was measured by colony formation assay. The effects of longdaysin on cancer cell migration and invasion were assessed using transwell assays. The effect of longdaysin on cancer stem cells was tested by sphere formation assay. The in vivo antitumor effect of longdaysin was evaluated using MDA-MB-231 breast cancer xenografts. Longdaysin suppressed Wnt/β-catenin signaling through inhibition of CK1δ and CK1ε in HEK293T cells. In breast cancer Hs578T and MDA-MB-231 cells, micromolar concentr...Continue Reading

Citations

Dec 25, 2019·Journal of Experimental & Clinical Cancer Research : CR·Yangyang DongJing Jia
Sep 19, 2020·FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology·Xiaopeng SongLi Gao
Aug 22, 2020·Cancer Management and Research·Xiaolan WenWen Zhang
Jun 3, 2020·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·Ling WangDesheng Lu
Apr 14, 2021·Oncogene·Francesca BattaglinHeinz-Josef Lenz
Jul 4, 2021·Journal of Cellular and Molecular Medicine·Guanzheng LiuRutong Yu

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Methods Mentioned

BETA
nuclear translocation
xenografts
Transfection
PCR
xenograft

Software Mentioned

GraphPad Prism

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