LncRNA HCP5 remodels G6PD dual post-translational modification to mediate metabolic adaptations driving osimertinib resistance in lung adenocarcinoma

INTRODUCTION: Osimertinib represents the standard treatment for EGFR-mutant lung adenocarcinoma (LUAD); however, acquired resistance limits its clinical efficacy. Elucidating the underlying mechanisms of resistance is crucial for developing novel therapeutic strategies. OBJECTIVES: This study aimed to investigate the role of the long non-coding RNA HCP5 in mediating resistance to osimertinib. METHODS: HCP5 was identified via bioinformatics analysis of GEO datasets. Its expression was evaluated in patient-derived tumor tissues and serum using fluorescence in situ hybridization and RT-qPCR. Osimertinib-resistant cell models were established. Functional assays included HCP5 modulation, metabolomics, and mechanistic studies such as RNA immunoprecipitation, co-immunoprecipitation, and ubiquitination/acetylation assays. In vivo validation utilized a xenograft model and an orthotopic lung transplantation tumor model. RESULTS: Integrated bioinformatics analysis identified HCP5 as the only lncRNA consistently overexpressed in TKI-resistant LUAD cells. Clinically, HCP5 was markedly elevated in both serum and tumor tissues of osimertinib-resistant patients, and correlated with poorer progression-free survival. Functionally, HCP5 overexpression increased osimertinib IC50 by over 10-fold, while its knockdown restored sensitivity. Mechanistically, HCP5 physically interacts with G6PD, shielding it from VHL-mediated ubiquitination to enhance its protein stability. Simultaneously, HCP5 recruits SIRT2 to promote G6PD deacetylation, dimerization, and enzymatic activation, thereby driving pentose phosphate pathway (PPP) metabolic reprogramming. In vivo, HCP5 overexpression compromised osimertinib's antitumor effect, which was rescued by co-treatment with the PPP inhibitor 6-aminonicotinamide. CONCLUSIONS: HCP5 drives osimertinib resistance through dual post-translational regulation of G6PD-blocking ubiquitination and promoting deacetylation-leading to metabolic adaptation. Targeting the HCP5-G6PD axis is a potential treatment strategy to overcome osimertinib resistance in LUAD.

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Journal
Journal of Advanced Research
Published
2026-04-01
DOI
https://doi.org/10.1016/j.jare.2026.04.017
Primary Topic
Cancer-related molecular mechanisms research
Type
article
Field-Weighted Citation Impact
0.00

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article

LncRNA HCP5 remodels G6PD dual post-translational modification to mediate metabolic adaptations driving osimertinib resistance in lung adenocarcinoma

YueJun Chen, Yiping Liu, Wei Xu, Ping Xu et al.
Journal of Advanced Research
Cancer-related molecular mechanisms research
article

LncRNA HCP5 remodels G6PD dual post-translational modification to mediate metabolic adaptations driving osimertinib resistance in lung adenocarcinoma

YueJun Chen, Yiping Liu, Wei Xu, Ping Xu, Ziyao Wang, Zheng Li, Li Fang, Xi Chen, Desong Yang, Qianqian Zhang
article en

Abstract

INTRODUCTION: Osimertinib represents the standard treatment for EGFR-mutant lung adenocarcinoma (LUAD); however, acquired resistance limits its clinical efficacy. Elucidating the underlying mechanisms of resistance is crucial for developing novel therapeutic strategies. OBJECTIVES: This study aimed to investigate the role of the long non-coding RNA HCP5 in mediating resistance to osimertinib. METHODS: HCP5 was identified via bioinformatics analysis of GEO datasets. Its expression was evaluated in patient-derived tumor tissues and serum using fluorescence in situ hybridization and RT-qPCR. Osimertinib-resistant cell models were established. Functional assays included HCP5 modulation, metabolomics, and mechanistic studies such as RNA immunoprecipitation, co-immunoprecipitation, and ubiquitination/acetylation assays. In vivo validation utilized a xenograft model and an orthotopic lung transplantation tumor model. RESULTS: Integrated bioinformatics analysis identified HCP5 as the only lncRNA consistently overexpressed in TKI-resistant LUAD cells. Clinically, HCP5 was markedly elevated in both serum and tumor tissues of osimertinib-resistant patients, and correlated with poorer progression-free survival. Functionally, HCP5 overexpression increased osimertinib IC50 by over 10-fold, while its knockdown restored sensitivity. Mechanistically, HCP5 physically interacts with G6PD, shielding it from VHL-mediated ubiquitination to enhance its protein stability. Simultaneously, HCP5 recruits SIRT2 to promote G6PD deacetylation, dimerization, and enzymatic activation, thereby driving pentose phosphate pathway (PPP) metabolic reprogramming. In vivo, HCP5 overexpression compromised osimertinib's antitumor effect, which was rescued by co-treatment with the PPP inhibitor 6-aminonicotinamide. CONCLUSIONS: HCP5 drives osimertinib resistance through dual post-translational regulation of G6PD-blocking ubiquitination and promoting deacetylation-leading to metabolic adaptation. Targeting the HCP5-G6PD axis is a potential treatment strategy to overcome osimertinib resistance in LUAD.

Journal of Advanced Research
Central South University (CN), Ministry of Education (SA), Hunan Cancer Hospital (CN), Peking University Shenzhen Hospital (CN), Ministry of Education (ET), Shenzhen Second People's Hospital (CN)
Central South University, Natural Science Foundation of Guangdong Province, Science, Technology and Innovation Commission of Shenzhen Municipality, Higher Education Discipline Innovation Project, Science and Technology Program of Hunan Province, Health and Family Planning Commission of Hunan Province, Overseas Expertise Introduction Project for Discipline Innovation
Zero hunger
Openalex Percentile: Top 20%
Cancer-related molecular mechanisms research
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