Evans Blue Acts as a Selective Inhibitor of <scp>CaMKII</scp>‐α to Impede the Progression of <scp>TCL</scp> Identified by <scp>HTS</scp>

T-cell lymphoma (TCL) poses a significant challenge in clinical oncology, characterized by its aggressive behavior and resistance to conventional therapies. Despite considerable research efforts, the prognosis for TCL patients remains poor, primarily due to the lack of effective therapeutic strategies that can inhibit tumor progression and metastasis. In this study, we identified CaMKII-α as a potential therapeutic target for TCL. To explore its role in TCL pathogenesis, we investigated its effects on TCL cell lines. Protein expression levels within the PI3K-AKT signaling pathway were assessed using western blot analysis. Through siRNA-mediated gene silencing, we downregulated CaMKII-α expression and monitored TCL cell proliferation. Furthermore, we identified Evans Blue (IC<sub>50</sub> = 197.1 nM) as a selective small-molecule inhibitor of CaMKII-α through high-throughput screening (HTS). Evans Blue demonstrated significant tumor-suppressive effects, potentially inhibiting TCL cell proliferation via regulation of the PI3K-AKT signaling pathway. Notably, the antitumor effect of Evans Blue was comparable to that observed with genetic CaMKII-α ablation, highlighting its potential as a novel therapeutic strategy for the treatment of TCL.

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Publication Details

Journal
Cancer Science
Published
2025-04-04
DOI
https://doi.org/10.1111/cas.70051
Primary Topic
Ubiquitin and proteasome pathways
Type
article
Field-Weighted Citation Impact
0.00

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article

Evans Blue Acts as a Selective Inhibitor of CaMKII‐α to Impede the Progression of TCL Identified by HTS

Lansong Li, Jianru Tian, Hui Jiang, Aiqin Zhang et al.
Cancer Science
Ubiquitin and proteasome pathways
article

Evans Blue Acts as a Selective Inhibitor of CaMKII‐α to Impede the Progression of TCL Identified by HTS

Lansong Li, Jianru Tian, Hui Jiang, Aiqin Zhang, Hong Liu, Ruqi Liang
article en

Abstract

T-cell lymphoma (TCL) poses a significant challenge in clinical oncology, characterized by its aggressive behavior and resistance to conventional therapies. Despite considerable research efforts, the prognosis for TCL patients remains poor, primarily due to the lack of effective therapeutic strategies that can inhibit tumor progression and metastasis. In this study, we identified CaMKII-α as a potential therapeutic target for TCL. To explore its role in TCL pathogenesis, we investigated its effects on TCL cell lines. Protein expression levels within the PI3K-AKT signaling pathway were assessed using western blot analysis. Through siRNA-mediated gene silencing, we downregulated CaMKII-α expression and monitored TCL cell proliferation. Furthermore, we identified Evans Blue (IC<sub>50</sub> = 197.1 nM) as a selective small-molecule inhibitor of CaMKII-α through high-throughput screening (HTS). Evans Blue demonstrated significant tumor-suppressive effects, potentially inhibiting TCL cell proliferation via regulation of the PI3K-AKT signaling pathway. Notably, the antitumor effect of Evans Blue was comparable to that observed with genetic CaMKII-α ablation, highlighting its potential as a novel therapeutic strategy for the treatment of TCL.

Cancer ScienceVol. 116(7)
Taiyuan University of Technology (CN)
National Science Foundation, Taiyuan University of Technology
No poverty
Openalex Percentile: Top 94%
Ubiquitin and proteasome pathways
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