Mechanisms of Resistance to EGFR Inhibition Reveal Metabolic Vulnerabilities in Human GBM.
Details
Serval ID
serval:BIB_B63D76C24EA8
Type
Article: article from journal or magazin.
Collection
Publications
Institution
Title
Mechanisms of Resistance to EGFR Inhibition Reveal Metabolic Vulnerabilities in Human GBM.
Journal
Molecular cancer therapeutics
ISSN
1538-8514 (Electronic)
ISSN-L
1535-7163
Publication state
Published
Issued date
09/2019
Peer-reviewed
Oui
Volume
18
Number
9
Pages
1565-1576
Language
english
Notes
Publication types: Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't
Publication Status: ppublish
Publication Status: ppublish
Abstract
Amplification of the epidermal growth factor receptor gene (EGFR) represents one of the most commonly observed genetic lesions in glioblastoma (GBM); however, therapies targeting this signaling pathway have failed clinically. Here, using human tumors, primary patient-derived xenografts (PDX), and a murine model for GBM, we demonstrate that EGFR inhibition leads to increased invasion of tumor cells. Further, EGFR inhibitor-treated GBM demonstrates altered oxidative stress, with increased lipid peroxidation, and generation of toxic lipid peroxidation products. A tumor cell subpopulation with elevated aldehyde dehydrogenase (ALDH) levels was determined to comprise a significant proportion of the invasive cells observed in EGFR inhibitor-treated GBM. Our analysis of the ALDH1A1 protein in newly diagnosed GBM revealed detectable ALDH1A1 expression in 69% (35/51) of the cases, but in relatively low percentages of tumor cells. Analysis of paired human GBM before and after EGFR inhibitor therapy showed an increase in ALDH1A1 expression in EGFR-amplified tumors (P < 0.05, n = 13 tumor pairs), and in murine GBM ALDH1A1-high clones were more resistant to EGFR inhibition than ALDH1A1-low clones. Our data identify ALDH levels as a biomarker of GBM cells with high invasive potential, altered oxidative stress, and resistance to EGFR inhibition, and reveal a therapeutic target whose inhibition should limit GBM invasion.
Keywords
Aldehyde Dehydrogenase 1/metabolism, Animals, Brain Neoplasms/drug therapy, Brain Neoplasms/metabolism, Brain Neoplasms/pathology, Cell Line, Tumor, Cell Proliferation/drug effects, Dasatinib/pharmacology, Drug Resistance, Neoplasm/drug effects, ErbB Receptors/antagonists & inhibitors, ErbB Receptors/metabolism, Erlotinib Hydrochloride/pharmacology, Glioblastoma/drug therapy, Glioblastoma/metabolism, Glioblastoma/pathology, Humans, Mice, Oxidative Stress/drug effects, Protein Kinase Inhibitors/pharmacology, Retinal Dehydrogenase/metabolism, Xenograft Model Antitumor Assays/methods
Pubmed
Web of science
Create date
08/07/2019 12:50
Last modification date
21/04/2021 5:34