Activation of Nerve Growth Factor signaling limits the response to lenvatinib in hepatocellular carcinoma
Minghao Xu1, Yimin Zheng1, Longtao Zhao1
1Department of Liver Surgery and Transplantation, Liver Cancer Institute, Zhongshan Hospital, Fudan University, Shanghai, China.
Abstract:
Resistance to lenvatinib remains a major barrier in the treatment of advanced hepatocellular carcinoma (HCC), underscoring the urgent need to elucidate the underlying mechanisms and identify actionable therapeutic targets. In this study, we identified a neurosecretory factor derived from HCC cells, Nerve Growth Factor (NGF), as a critical mediator of lenvatinib resistance. Utilizing an innovative in vivo-in vitro cross-circulated strategy, we established a phenotypically stable lenvatinib-resistant HCC cell line (LenR-cells). Through proteomic screening of conditioned media and subsequent functional validation, we demonstrated that NGF secretion progressively increases with the acquisition of resistance. Mechanistically, we uncovered that the SRPK1-SRSF1 axis drives enhanced NGF production by regulating alternative splicing of its precursor transcript, specifically promoting the expression of a shorter, translationally efficient isoform (proNGF-B). Elevated NGF subsequently activates the non-canonical MAPK pathway (MEK5-ERK5) via its high-affinity receptor TrkA, thereby sustaining tumor cell viability and proliferation under sustained tyrosine kinase inhibitor pressure. Critically, pharmacological co-targeting of TrkA with the clinically approved inhibitor larotrectinib restored lenvatinib sensitivity in both patient-derived organoids and xenograft models, producing marked synergistic anti-tumor effects without evidence of exacerbated toxicity. Clinical analyses of two independent patient cohorts further confirmed that elevated NGF expression is significantly associated with poor response to lenvatinib, shorter recurrence-free survival, and worse overall survival. Our findings unveil a critical and previously underappreciated role for tumor-derived NGF in orchestrating adaptive signaling through a precise post-transcriptional regulatory circuit and propose a readily translatable, biomarker-guided combination strategy to overcome lenvatinib resistance in HCC.
Insights
Nerve Growth Factor (NGF) drives lenvatinib resistance in liver cancer by activating the MEK5-ERK5 pathway. Targeting NGF
Area of Science:
- Oncology
- Molecular Biology
- Drug Resistance Mechanisms
Background:
- Lenvatinib resistance is a significant challenge in advanced hepatocellular carcinoma (HCC) treatment.
- Identifying mechanisms of resistance is crucial for developing effective therapeutic strategies.
Purpose of the Study:
- To investigate the role of neurosecretory factors in lenvatinib resistance in HCC.
- To identify novel therapeutic targets to overcome lenvatinib resistance.
Main Methods:
- Established a lenvatinib-resistant HCC cell line (LenR-cells) using an in vivo-in vitro cross-circulated strategy.
- Utilized proteomic screening and functional validation to identify key mediators.
- Investigated the SRPK1-SRSF1 axis and its role in Nerve Growth Factor (NGF) production.
- Examined the MEK5-ERK5 pathway activation by NGF via the TrkA receptor.
- Evaluated combination therapy with TrkA inhibitor (larotrectinib) and lenvatinib in patient-derived organoids and xenograft models.
- Analyzed clinical data from two independent HCC patient cohorts.
Main Results:
- Nerve Growth Factor (NGF) secretion increases with lenvatinib resistance.
- The SRPK1-SRSF1 axis promotes NGF production through alternative splicing.
- Elevated NGF activates the MEK5-ERK5 pathway, sustaining tumor cell viability.
- Co-targeting TrkA with larotrectinib restored lenvatinib sensitivity and showed synergistic anti-tumor effects.
- High NGF expression correlated with poor lenvatinib response, shorter recurrence-free survival, and worse overall survival in HCC patients.
Conclusions:
- Tumor-derived NGF is a critical mediator of lenvatinib resistance in HCC.
- A post-transcriptional regulatory circuit involving the SRPK1-SRSF1 axis drives NGF production.
- Combination therapy targeting TrkA offers a promising strategy to overcome lenvatinib resistance.
- NGF can serve as a predictive biomarker for lenvatinib treatment response.
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