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RAC1 directly phosphorylates both PKM2 and FBP1 to promote radioresistance in hepatocellular carcinoma.

Molecular therapy : the journal of the American Society of Gene Therapy 2026 Vol.34(2) p. 1201-1214

Jiang Y, Zhou K, Wei X, Feng J, Zhou B, Liu C, Sun J, Zhu H, Liu Z, Yuan N, Li Y, Meng X, Cao J, Jiao Y, Cheng S

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Radiotherapy (RT) is a promising treatment for hepatocellular carcinoma (HCC), but resistance limits its efficacy.

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BibTeX ↓ RIS ↓
APA Jiang Y, Zhou K, et al. (2026). RAC1 directly phosphorylates both PKM2 and FBP1 to promote radioresistance in hepatocellular carcinoma.. Molecular therapy : the journal of the American Society of Gene Therapy, 34(2), 1201-1214. https://doi.org/10.1016/j.ymthe.2025.10.049
MLA Jiang Y, et al.. "RAC1 directly phosphorylates both PKM2 and FBP1 to promote radioresistance in hepatocellular carcinoma.." Molecular therapy : the journal of the American Society of Gene Therapy, vol. 34, no. 2, 2026, pp. 1201-1214.
PMID 41204670

Abstract

Radiotherapy (RT) is a promising treatment for hepatocellular carcinoma (HCC), but resistance limits its efficacy. This study reveals that Rac family small GTPase 1 (RAC1) is overexpressed in radioresistant HCC patients and promotes resistance by directly phosphorylating pyruvate kinase M2 (PKM2) and fructose-1,6-bisphosphatase 1 (FBP1), leading to enhanced glycolytic flux. Introducing mutations in PKM2 (S172A) and FBP1 (T309A) effectively inhibits tumor growth. Additionally, combining RT with the US Food and Drug Administration-approved drug foscarnet sodium, which inhibits RAC1 activity, significantly improves therapeutic outcomes in vivo. These findings identify RAC1 as a key regulator of radioresistance and a potential therapeutic target in HCC.

MeSH Terms

Carcinoma, Hepatocellular; Humans; Liver Neoplasms; Animals; rac1 GTP-Binding Protein; Radiation Tolerance; Mice; Membrane Proteins; Thyroid Hormone-Binding Proteins; Thyroid Hormones; Phosphorylation; Fructose-Bisphosphatase; Cell Line, Tumor; Carrier Proteins; Xenograft Model Antitumor Assays; Gene Expression Regulation, Neoplastic

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