KRAS Inhibitor Resistance Confers a Targetable Vulnerability to Ferroptosis in Pancreatic Ductal Adenocarcinoma

KRAS inhibitors represent a promising therapeutic frontier in pancreatic ductal adenocarcinoma (PDAC) treatment. However, the clinical benefit of KRAS inhibitors in PDAC is limited by the frequent emergence of resistance. Here, we demonstrated that acquisition of resistance to KRAS inhibitors rendered PDAC cells hypersensitive to ferroptosis. Untargeted lipidomic profiling revealed that resistant cells underwent extensive lipid metabolic reprogramming characterized by selective enrichment of polyunsaturated fatty acid-containing phosphatidylcholines (PC-PUFAs) and a concomitant reduction in monounsaturated fatty acid-containing species (PC-MUFAs). The orphan nuclear receptor NR2F2 was a critical determinant of ferroptosis sensitivity in resistant cells. NR2F2 expression was markedly elevated upon acquisition of resistance, accompanied by substantial changes in its occupancy at regulatory elements of key lipid metabolic genes. By altering chromatin accessibility, NR2F2 drove PUFA biosynthesis and phospholipid remodeling, creating a ferroptosis-prone lipid state. Collectively, these findings establish NR2F2-driven lipid metabolic rewiring as an intrinsic ferroptosis liability in KRAS inhibitor-resistant PDAC and reveal ferroptosis induction as a therapeutic strategy to overcome resistance to KRAS-targeted therapies.

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Publication Details

Journal
Cancer Research
Published
2026-11-03
DOI
https://doi.org/10.1158/0008-5472.can-26-1490
Primary Topic
Ferroptosis and cancer prognosis
Type
article
Field-Weighted Citation Impact
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article

KRAS Inhibitor Resistance Confers a Targetable Vulnerability to Ferroptosis in Pancreatic Ductal Adenocarcinoma

Sihan Huo, Hua Wang, Ying Zhao, Jingfeng Tang et al.
Cancer Research
Ferroptosis and cancer prognosis
article

KRAS Inhibitor Resistance Confers a Targetable Vulnerability to Ferroptosis in Pancreatic Ductal Adenocarcinoma

Sihan Huo, Hua Wang, Ying Zhao, Jingfeng Tang, Yueran Zhang, Minghe Fan, Wenqin Hao, Ziyang Zhang, Tong Liu, Lina Wang, Yuyao Guo, Ruoxuan Wang, Xiangying Fu, Hailong Zhao
article en

Abstract

KRAS inhibitors represent a promising therapeutic frontier in pancreatic ductal adenocarcinoma (PDAC) treatment. However, the clinical benefit of KRAS inhibitors in PDAC is limited by the frequent emergence of resistance. Here, we demonstrated that acquisition of resistance to KRAS inhibitors rendered PDAC cells hypersensitive to ferroptosis. Untargeted lipidomic profiling revealed that resistant cells underwent extensive lipid metabolic reprogramming characterized by selective enrichment of polyunsaturated fatty acid-containing phosphatidylcholines (PC-PUFAs) and a concomitant reduction in monounsaturated fatty acid-containing species (PC-MUFAs). The orphan nuclear receptor NR2F2 was a critical determinant of ferroptosis sensitivity in resistant cells. NR2F2 expression was markedly elevated upon acquisition of resistance, accompanied by substantial changes in its occupancy at regulatory elements of key lipid metabolic genes. By altering chromatin accessibility, NR2F2 drove PUFA biosynthesis and phospholipid remodeling, creating a ferroptosis-prone lipid state. Collectively, these findings establish NR2F2-driven lipid metabolic rewiring as an intrinsic ferroptosis liability in KRAS inhibitor-resistant PDAC and reveal ferroptosis induction as a therapeutic strategy to overcome resistance to KRAS-targeted therapies.

Cancer Research
Peking University (CN), Peking University Third Hospital (CN), Hubei University of Technology (CN)
Openalex Percentile: Top 13%
Ferroptosis and cancer prognosis
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