The oncogenic neurotrophin receptor tropomyosin-related kinase variant, TrkAIII
Antonietta Rosella Farina1, Lucia Cappabianca1, Pierdomenico Ruggeri1
1Department of Applied Clinical and Biotechnological Sciences, University of L'Aquila, L'Aquila, Italy.
Abstract:
Oncogenes derived from the neurotrophin receptor tropomyosin-related kinase TrkA act as drivers in sub-populations of a wide-range of human cancers. This, combined with a recent report that both adult and childhood cancers driven by novel oncogenic TrkA chimeric-fusions exhibit profound, long-lived therapeutic responses to the Trk inhibitor Larotrectinib, highlights the need to improve clinical detection of TrkA oncogene-driven cancers in order to maximise this novel therapeutic potential. Cancers potentially driven by TrkA oncogenes include a proportion of paediatric neuroblastomas (NBs) that express the alternative TrkA splice variant TrkAIII, which exhibits exon 6, 7 and 9 skipping and oncogenic-activity that depends upon deletion of the extracellular D4 Ig-like domain. In contrast to fully spliced TrkA, which exhibits tumour suppressor activity in NB and associates with good prognosis, TrkAIII associates with advanced stage metastatic disease, post therapeutic relapse and worse prognosis, induces malignant transformation of NIH-3T3 cells and exhibits oncogenic activity in NB models. TrkAIII induction in NB cells is stress-regulated by conditions that mimic hypoxia or perturbate the ER with potential to change TrkA tumour-suppressing signals into oncogenic TrkAIII signals within the stressful tumour microenvironment. In contrast to cell surface TrkA, TrkAIII re-localises to intracellular pre-Golgi membranes, centrosomes and mitochondria, within which it exhibits spontaneous ligand-independent activation, triggering a variety of mechanisms that promote tumorigenicity and malignant behaviour, which impact the majority of cancer hallmarks. In this review, we present updates on TrkAIII detection and association with human malignancies, the multiple ways TrkAIII exerts oncogenic activity and potential therapeutic approaches for TrkAIII expressing cancers, with particular reference to NB.
Insights
Oncogenic TrkAIII, a variant of the TrkA receptor, drives various cancers, including neuroblastoma. Detecting TrkAIII is crucial for effective treatment with Trk inhibitors like Larotrectinib.
Area of Science:
- Oncology
- Molecular Biology
- Cancer Genetics
Background:
- Tropomyosin-related kinase (Trk) A oncogenes drive subsets of human cancers.
- TrkA alterations, particularly chimeric-fusions, respond well to Trk inhibitor therapy.
- TrkAIII, an oncogenic splice variant, is implicated in aggressive cancers, including pediatric neuroblastoma (NB).
Purpose of the Study:
- To review advances in detecting TrkAIII-driven cancers.
- To explore the oncogenic mechanisms of TrkAIII.
- To discuss therapeutic strategies for TrkAIII-positive malignancies, focusing on NB.
Main Methods:
- Literature review of TrkAIII in human cancers.
- Analysis of TrkAIII's oncogenic activity and cellular localization.
- Discussion of therapeutic targets and inhibitors.
Main Results:
- TrkAIII expression correlates with advanced NB, metastasis, and poor prognosis.
- TrkAIII exhibits ligand-independent activation and promotes tumorigenesis.
- TrkAIII re-localizes to intracellular compartments, distinct from cell surface TrkA.
Conclusions:
- Improved detection of TrkAIII-driven cancers is essential for maximizing therapeutic responses.
- TrkAIII's unique oncogenic pathways offer potential therapeutic vulnerabilities.
- Targeting TrkAIII presents a promising strategy for treating specific aggressive cancers.
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