Targeting GCN5-mediated ERK lactylation: A promising drug development frontier in cancer therapy

• GCN5 mediates ERK K231 lactylation linking glycolysis to oncogenic MAPK signaling. • Targeting GCN5 lactylation offers a strategy to overcome resistance to MEK or ERK inhibitors. • Modulating lactylation reshapes the tumor immune microenvironment and enhances T cell function. • Inhibiting site-specific lactylation is a precise strategy for glycolytic RAS ERK driven cancers.

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Publication Details

Journal
Biomedicine & Pharmacotherapy
Published
2026-02-21
DOI
https://doi.org/10.1016/j.biopha.2026.119128
Primary Topic
Melanoma and MAPK Pathways
Type
article
Field-Weighted Citation Impact
0.00
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article

Targeting GCN5-mediated ERK lactylation: A promising drug development frontier in cancer therapy

Yen‐Dun Tony Tzeng, Chia‐Jung Li, An-Jen Chiang
Biomedicine & Pharmacotherapy
Melanoma and MAPK Pathways
article

Targeting GCN5-mediated ERK lactylation: A promising drug development frontier in cancer therapy

Yen‐Dun Tony Tzeng, Chia‐Jung Li, An-Jen Chiang
article en

Abstract

• GCN5 mediates ERK K231 lactylation linking glycolysis to oncogenic MAPK signaling. • Targeting GCN5 lactylation offers a strategy to overcome resistance to MEK or ERK inhibitors. • Modulating lactylation reshapes the tumor immune microenvironment and enhances T cell function. • Inhibiting site-specific lactylation is a precise strategy for glycolytic RAS ERK driven cancers.

Biomedicine & PharmacotherapyVol. 196
National Sun Yat-sen University (TW), Kaohsiung Veterans General Hospital (TW)
Good health and well-being
Openalex Percentile: Top 46%
Melanoma and MAPK Pathways
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