MEK Inhibition Suppresses Growth of Atypical Teratoid/Rhabdoid Tumors

J Neuropathol Exp Neurol. 2020 Jul 1;79(7):746-753. doi: 10.1093/jnen/nlaa042.

Abstract

Atypical teratoid/rhabdoid (AT/RT) tumors are the most common malignant brain tumor of infancy and have a poor prognosis. We have previously identified very high expression of LIN28A and/or LIN28B in AT/RT tumors and showed that AT/RT have corresponding increased expression of the mitogen-activated protein (MAP) kinase pathway. Binimetinib is a novel inhibitor of mitogen-activated protein kinase (MAP2K1 or MEK), and is currently in pediatric phase II clinical trials for low-grade glioma. We hypothesized that binimetinib would inhibit growth of AT/RT cells by suppressing the MAP kinase pathway. Binimetinib inhibited AT/RT growth at nanomolar concentrations. Binimetinib decreased cell proliferation and induced apoptosis in AT/RT cells and significantly reduced AT/RT tumor growth in flank xenografts. Our data suggest that MAP kinase pathway inhibition could offer a potential avenue for treating these highly aggressive tumors.

Keywords: INI1; MEK162; Malignant rhabdoid tumor; Pediatric brain tumor; RAS.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Benzimidazoles / pharmacology*
  • Benzimidazoles / therapeutic use
  • Brain Neoplasms / drug therapy*
  • Brain Neoplasms / enzymology
  • Brain Neoplasms / pathology
  • Cell Line, Tumor
  • Cell Proliferation / drug effects*
  • Cell Proliferation / physiology
  • Humans
  • MAP Kinase Signaling System / drug effects*
  • MAP Kinase Signaling System / physiology
  • Mice
  • Rhabdoid Tumor / drug therapy*
  • Rhabdoid Tumor / enzymology
  • Rhabdoid Tumor / pathology
  • Teratoma / drug therapy*
  • Teratoma / enzymology
  • Teratoma / pathology
  • Xenograft Model Antitumor Assays / methods

Substances

  • Benzimidazoles
  • binimetinib