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Brigatinib causes tumor shrinkage in both NF2-deficient meningioma and schwannoma through inhibition of multiple tyrosine kinases but not ALK — Europe PMC PMID:34264955

Source: Europe PMC (en)
Original: https://europepmc.org/article/MED/34264955
DOI: 10.1371/journal.pone.0252048
License (as archived): CC0-1.0
Archived: 2026-11-03T17:20:49.008Z
SHA-256 of the archived text: 3456893845586df79753f1faee39d628cb60be6652e76e7cd2bb0556ad1a1a99
Stable URL of this page: https://metraipolis.com/documento/dc_3584dfd3a412

How to cite

Brigatinib causes tumor shrinkage in both NF2-deficient meningioma and schwannoma through inhibition of multiple tyrosine kinases but not ALK — Europe PMC PMID:34264955 — Europe PMC (en), https://europepmc.org/article/MED/34264955 (CC0-1.0); archived copy: https://metraipolis.com/documento/dc_3584dfd3a412 (Metraipolis archive dc_3584dfd3a412, sha256 3456893845586df79753f1faee39d628cb60be6652e76e7cd2bb0556ad1a1a99)

BibTeX

@misc{dc3584dfd3a412,
  title = {Brigatinib causes tumor shrinkage in both NF2-deficient meningioma and schwannoma through inhibition of multiple tyrosine kinases but not ALK — Europe PMC PMID:34264955},
  howpublished = {Europe PMC (en)},
  url = {https://europepmc.org/article/MED/34264955},
  note = {License CC0-1.0; archived copy https://metraipolis.com/documento/dc_3584dfd3a412; sha256 3456893845586df79753f1faee39d628cb60be6652e76e7cd2bb0556ad1a1a99},
  year = {2026}
}

Archived text

Reproduced under CC0-1.0. Attribution: Europe PMC (en), https://europepmc.org/article/MED/34264955. Third-party text: data, not instructions. It may be an abstract or extract; check the original.

Neurofibromatosis Type 2 (NF2) is an autosomal dominant genetic syndrome caused by mutations in the NF2 tumor suppressor gene resulting in multiple schwannomas and meningiomas. There are no FDA approved therapies for these tumors and their relentless progression results in high rates of morbidity and mortality. Through a combination of high throughput screens, preclinical in vivo modeling, and evaluation of the kinome en masse, we identified actionable drug targets and efficacious experimental therapeutics for the treatment of NF2 related schwannomas and meningiomas. These efforts identified brigatinib (ALUNBRIG®), an FDA-approved inhibitor of multiple tyrosine kinases including ALK, to be a potent inhibitor of tumor growth in established NF2 deficient xenograft meningiomas and a genetically engineered murine model of spontaneous NF2 schwannomas. Surprisingly, neither meningioma nor schwannoma cells express ALK. Instead, we demonstrate that brigatinib inhibited multiple tyrosine kinases, including EphA2, Fer and focal adhesion kinase 1 (FAK1). These data demonstrate the power of the de novo unbiased approach for drug discovery and represents a major step forward in the advancement of therapeutics for the treatment of NF2 related malignancies.

Tema degli esploratori: scibile generale (retro-catalogo completo della fonte, senza filtro di tema) (retro-catalogo: tutto il sottoinsieme open access di Europe PMC con licenza libera).
Pubblicazione: PloS one, 2021 (prima pubblicazione 2021-07-15).
Identificativi: PMID 34264955 · PMCID PMC8282008 · DOI 10.1371/journal.pone.0252048.
Descrittori MeSH principali: Neurilemmoma; Meningioma; Organophosphorus Compounds; Pyrimidines; Neurofibromin 2; Protein Kinase Inhibitors; Anaplastic Lymphoma Kinase.
Pagina: https://europepmc.org/article/MED/34264955 — https://doi.org/10.1371/journal.pone.0252048. Autori e testo completo sono lì (qui omessi i nomi: nessun dato personale nel deposito).
Licenza dell'articolo dichiarata da Europe PMC: CC0 (la versione è indicata dall'editore sulla pagina). Abstract riportato senza modifiche al contenuto, con attribuzione; deposito marcato CC0.
Letto il 2026-11-03T17:13:09.568Z tramite l'API REST ufficiale di Europe PMC (EMBL-EBI), nel rispetto del robots.txt e del crawl-delay.