Discovery of a rare GKAP1-NTRK2 fusion in a pediatric low-grade glioma, leading to targeted treatment with TRK-inhibitor larotrectinib

Cancer Biol Ther. 2021 Mar 4;22(3):184-195. doi: 10.1080/15384047.2021.1899573. Epub 2021 Apr 5.

Abstract

Here we report a case of an 11-year-old girl with an inoperable tumor in the optic chiasm/hypothalamus, who experienced several tumor progressions despite three lines of chemotherapy treatment. Routine clinical examination classified the tumor as a BRAF-negative pilocytic astrocytoma. Copy-number variation profiling of fresh frozen tumor material identified two duplications in 9q21.32-33 leading to breakpoints within the GKAP1 and NTRK2 genes. RT-PCR Sanger sequencing revealed a GKAP1-NTRK2 exon 10-16 in-frame fusion, generating a putative fusion protein of 658 amino acids with a retained tyrosine kinase (TK) domain. Functional analysis by transient transfection of HEK293 cells showed the GKAP1-NTRK2 fusion protein to be activated through phosphorylation of the TK domain (Tyr705). Subsequently, downstream mediators of the MAPK- and PI3K-signaling pathways were upregulated in GKAP1-NTRK2 cells compared to NTRK2 wild-type; phosphorylated (p)ERK (3.6-fold), pAKT (1.8- fold), and pS6 ribosomal protein (1.4-fold). Following these findings, the patient was enrolled in a clinical trial and treated with the specific TRK-inhibitor larotrectinib, resulting in the arrest of tumor growth. The patient's condition is currently stable and the quality of life has improved significantly. Our findings highlight the value of comprehensive clinical molecular screening of BRAF-negative pediatric low-grade gliomas, to reveal rare fusions serving as targets for precision therapy.

Keywords: GKAP1; NTRK2; TRKB; fusion gene; larotrectinib; pLGG; pediatric brain tumor; precision medicine.

Publication types

  • Case Reports
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adaptor Proteins, Signal Transducing / genetics
  • Brain Neoplasms / drug therapy*
  • Brain Neoplasms / genetics*
  • Brain Neoplasms / metabolism
  • Child
  • Female
  • Glioma / drug therapy*
  • Glioma / genetics
  • Glioma / metabolism
  • Humans
  • Hypothalamic Diseases
  • Membrane Glycoproteins / genetics
  • Neoplasm Grading
  • Oncogene Proteins, Fusion / genetics*
  • Oncogene Proteins, Fusion / metabolism
  • Optic Chiasm / pathology
  • Protein Kinase Inhibitors / therapeutic use*
  • Pyrazoles / therapeutic use*
  • Pyrimidines / therapeutic use*
  • Receptor, trkB / genetics

Substances

  • Adaptor Proteins, Signal Transducing
  • Membrane Glycoproteins
  • Oncogene Proteins, Fusion
  • Protein Kinase Inhibitors
  • Pyrazoles
  • Pyrimidines
  • Receptor, trkB
  • tropomyosin-related kinase-B, human
  • larotrectinib

Grants and funding

This work was supported by the Swedish Cancer Society (www.cancerfonden.se, grant number 2018/825 to FA and grant number 2018/652 to JN), the Swedish Childhood Cancer Foundation (www.barncancerfonden.se, grant number PR2017-0029 to FA, and PR2019-0079 to KE), and the ALF-agreement (www.researchweb.org/is/alfgbg, Sahlgrenska Universitetssjukhuset ALFGBG-716231 to FA and Sahlgrenska Universitetssjukhuset ALFGBG-719301 to JN).