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Author Spotlight: Exploring Salidroside's Molecular Mechanisms in Breast Cancer Treatment
Published on: June 9, 2023
SIK2 maintains breast cancer stemness by phosphorylating LRP6 and activating Wnt/β-catenin signaling
Zhuoxian Rong1,2,3,4,5, Lu Zhang1,2, Zhi Li1,2,3,4,5
1Xiangya Cancer Center, Xiangya Hospital, Central South University, Changsha, 410008, China.
Abstract:
Breast cancer stem cells (BCSCs) are the main drivers of recurrence and metastasis. However, commonly used drugs rarely target BCSCs. Via screenings, we found that Salt-inducible kinase 2 (SIK2) participated in breast cancer (BC) stemness maintenance and zebrafish embryos development. SIK2 was upregulated in recurrence samples. Knockdown of SIK2 expression reduced the proportion of BCSCs and the tumor initiation of BC cells. Mechanistically, SIK2, phosphorylated by CK1α, directly phosphorylated LRP6 in a SIK2 kinase activity-dependent manner, leading to Wnt/β-catenin signaling pathway activation. ARN-3236 and HG-9-91-01, inhibitors of SIK2, inhibited LRP6 phosphorylation and β-catenin accumulation and disturbed stemness maintenance. In addition, the SIK2-activated Wnt/β-catenin signaling led to induction of IDH1 expression, causing metabolic reprogramming in BC cells. These findings demonstrate a novel mechanism whereby Wnt/β-catenin signaling pathway is regulated by different kinases in response to metabolic requirement of CSCs, and suggest that SIK2 inhibition may potentially be a strategy for eliminating BCSCs.
Insights
Salt-inducible kinase 2 (SIK2) drives breast cancer stemness and Wnt/β-catenin activation. Inhibiting SIK2 reduces cancer recurrence and metastasis, offering a new therapeutic strategy for breast cancer.
Area of Science:
- Oncology
- Molecular Biology
- Cell Biology
Background:
- Breast cancer stem cells (BCSCs) drive tumor recurrence and metastasis.
- Current therapies are ineffective against BCSCs.
- Identifying novel targets for BCSCs is crucial for improving treatment outcomes.
Purpose of the Study:
- To investigate the role of Salt-inducible kinase 2 (SIK2) in maintaining breast cancer stemness.
- To elucidate the molecular mechanism by which SIK2 regulates BCSCs.
- To evaluate SIK2 inhibitors as a potential therapeutic strategy against breast cancer.
Main Methods:
- High-throughput screening to identify SIK2 involvement in breast cancer stemness.
- SIK2 knockdown experiments in breast cancer cells.
- Western blotting to assess protein phosphorylation and signaling pathway activation (Wnt/β-catenin).
- Treatment with SIK2 inhibitors (ARN-3236 and HG-9-91-01).
- Analysis of IDH1 expression and metabolic reprogramming.
Main Results:
- SIK2 is upregulated in recurrent breast cancer samples and promotes stemness.
- SIK2 knockdown reduces the proportion of BCSCs and tumor initiation.
- SIK2 directly phosphorylates LRP6, activating the Wnt/β-catenin pathway.
- SIK2 inhibitors block LRP6 phosphorylation, reduce β-catenin, and impair stemness.
- SIK2-activated Wnt/β-catenin signaling induces IDH1, leading to metabolic reprogramming.
Conclusions:
- SIK2 is a key regulator of breast cancer stemness via Wnt/β-catenin pathway activation.
- SIK2 inhibition disrupts CSC maintenance and metabolic reprogramming.
- Targeting SIK2 represents a promising therapeutic approach for eliminating BCSCs and preventing recurrence.
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