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.

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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