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Comment
. 2023 Nov 1;83(21):3498-3500.
doi: 10.1158/0008-5472.CAN-23-2921.

Targeting WNT/β-Catenin via Modulating EZH2 Function: A New Chapter in the Treatment of β-Catenin Mutant Hepatocellular Carcinoma?

Man Hsin Hung  1 , Xin Wei Wang  1   2
Affiliations
Comment

Targeting WNT/β-Catenin via Modulating EZH2 Function: A New Chapter in the Treatment of β-Catenin Mutant Hepatocellular Carcinoma?

Man Hsin Hung et al. Cancer Res. .

Abstract

In a recent study, Rialdi and colleagues identified a specific vulnerability in β-catenin mutant hepatocellular carcinoma (HCC) via EZH2-mediated suppression of WNT signaling and revealed the selective anti-HCC activity of WNTinib, a chemical derivative of regorafenib and sorafenib in targeting this vulnerability. Their discoveries highlight the role of EZH2 in modulating WNT signaling and suggest an implication of WNTinihb as a small-molecule inhibitor for the treatment of HCC with activated WNT/β-catenin.

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  • WNTinib is a multi-kinase inhibitor with specificity against β-catenin mutant hepatocellular carcinoma.
    Rialdi A, Duffy M, Scopton AP, Fonseca F, Zhao JN, Schwarz M, Molina-Sanchez P, Mzoughi S, Arceci E, Abril-Fornaguera J, Meadows A, Ruiz de Galarreta M, Torre D, Reyes K, Lim YT, Rosemann F, Khan ZM, Mohammed K, Wang X, Yu X, Lakshmanan M, Rajarethinam R, Tan SY, Jin J, Villanueva A, Michailidis E, De Jong YP, Rice CM, Marazzi I, Hasson D, Llovet JM, Sobota RM, Lujambio A, Guccione E, Dar AC. Rialdi A, et al. Nat Cancer. 2023 Aug;4(8):1157-1175. doi: 10.1038/s43018-023-00609-9. Epub 2023 Aug 3. Nat Cancer. 2023. PMID: 37537299 Free PMC article.

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