The T790M "gatekeeper" mutation in EGFR mediates resistance to low concentrations of an irreversible EGFR inhibitor.

PubWeight™: 2.58‹?› | Rank: Top 1%

🔗 View Article (PMID 18413800)

Published in Mol Cancer Ther on April 01, 2008

Authors

Nadia Godin-Heymann1, Lindsey Ulkus, Brian W Brannigan, Ultan McDermott, Jennifer Lamb, Shyamala Maheswaran, Jeffrey Settleman, Daniel A Haber

Author Affiliations

1: Massachusetts General Hospital Cancer Center and Harvard Medical School, 149 13th Street, Charlestown, MA 02129, USA.

Articles citing this

Dissecting therapeutic resistance to RAF inhibition in melanoma by tumor genomic profiling. J Clin Oncol (2011) 8.37

Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature (2009) 7.05

Rational, biologically based treatment of EGFR-mutant non-small-cell lung cancer. Nat Rev Cancer (2010) 5.82

Optimization of dosing for EGFR-mutant non-small cell lung cancer with evolutionary cancer modeling. Sci Transl Med (2011) 4.91

Acquired resistance to EGFR tyrosine kinase inhibitors in EGFR-mutant lung cancer: distinct natural history of patients with tumors harboring the T790M mutation. Clin Cancer Res (2010) 3.68

Factors underlying sensitivity of cancers to small-molecule kinase inhibitors. Nat Rev Drug Discov (2009) 3.64

Acquired resistance to epidermal growth factor receptor tyrosine kinase inhibitors in non-small-cell lung cancers dependent on the epidermal growth factor receptor pathway. Clin Lung Cancer (2009) 3.37

BRAF gene amplification can promote acquired resistance to MEK inhibitors in cancer cells harboring the BRAF V600E mutation. Sci Signal (2010) 3.25

The quest to overcome resistance to EGFR-targeted therapies in cancer. Nat Med (2013) 3.20

Dual targeting of EGFR can overcome a major drug resistance mutation in mouse models of EGFR mutant lung cancer. J Clin Invest (2009) 3.14

Acquired EGFR C797S mutation mediates resistance to AZD9291 in non-small cell lung cancer harboring EGFR T790M. Nat Med (2015) 2.88

KIT kinase mutants show unique mechanisms of drug resistance to imatinib and sunitinib in gastrointestinal stromal tumor patients. Proc Natl Acad Sci U S A (2009) 2.84

Reactivation of ERK signaling causes resistance to EGFR kinase inhibitors. Cancer Discov (2012) 2.47

A Landscape of Pharmacogenomic Interactions in Cancer. Cell (2016) 2.07

Effects of erlotinib in EGFR mutated non-small cell lung cancers with resistance to gefitinib. Clin Cancer Res (2008) 2.00

Noncovalent wild-type-sparing inhibitors of EGFR T790M. Cancer Discov (2012) 1.86

Dual MET-EGFR combinatorial inhibition against T790M-EGFR-mediated erlotinib-resistant lung cancer. Br J Cancer (2008) 1.83

Resistance to irreversible EGF receptor tyrosine kinase inhibitors through a multistep mechanism involving the IGF1R pathway. Cancer Res (2012) 1.66

The molecular pathology of breast cancer progression. J Pathol (2010) 1.65

The Allelic Context of the C797S Mutation Acquired upon Treatment with Third-Generation EGFR Inhibitors Impacts Sensitivity to Subsequent Treatment Strategies. Clin Cancer Res (2015) 1.61

Molecular mechanisms of acquired resistance to tyrosine kinase targeted therapy. Mol Cancer (2010) 1.56

Potential therapeutic strategies to overcome acquired resistance to BRAF or MEK inhibitors in BRAF mutant cancers. Oncotarget (2011) 1.55

HOXB9, a gene overexpressed in breast cancer, promotes tumorigenicity and lung metastasis. Proc Natl Acad Sci U S A (2009) 1.45

The challenge of developing robust drugs to overcome resistance. Drug Discov Today (2011) 1.43

EGFR Mutations and Resistance to Irreversible Pyrimidine-Based EGFR Inhibitors. Clin Cancer Res (2015) 1.28

Biomarkers That Currently Affect Clinical Practice in Lung Cancer: EGFR, ALK, MET, ROS-1, and KRAS. Front Oncol (2014) 1.20

The role of HER2 in early breast cancer metastasis and the origins of resistance to HER2-targeted therapies. Exp Mol Pathol (2009) 1.18

EGFR-mutant lung adenocarcinomas treated first-line with the novel EGFR inhibitor, XL647, can subsequently retain moderate sensitivity to erlotinib. J Thorac Oncol (2012) 1.18

Tyrosine phosphoproteomics identifies both codrivers and cotargeting strategies for T790M-related EGFR-TKI resistance in non-small cell lung cancer. Clin Cancer Res (2014) 1.07

Adaptive stress signaling in targeted cancer therapy resistance. Oncogene (2015) 1.07

Computational modeling of allosteric communication reveals organizing principles of mutation-induced signaling in ABL and EGFR kinases. PLoS Comput Biol (2011) 1.06

Genomic and proteomic biomarkers for cancer: a multitude of opportunities. Biochim Biophys Acta (2009) 1.03

Strategies for overcoming resistance to EGFR family tyrosine kinase inhibitors. Cancer Treat Rev (2011) 0.96

Biochemical mechanisms of resistance to small-molecule protein kinase inhibitors. ACS Chem Biol (2010) 0.94

Next-generation sequencing. Breast Cancer Res (2009) 0.94

Optimizing the sequence of anti-EGFR-targeted therapy in EGFR-mutant lung cancer. Mol Cancer Ther (2014) 0.93

EGFR C797S mutation mediates resistance to third-generation inhibitors in T790M-positive non-small cell lung cancer. J Hematol Oncol (2016) 0.90

AST1306, a novel irreversible inhibitor of the epidermal growth factor receptor 1 and 2, exhibits antitumor activity both in vitro and in vivo. PLoS One (2011) 0.85

Second-generation epidermal growth factor receptor tyrosine kinase inhibitors in lung cancers. J Natl Compr Canc Netw (2013) 0.83

Targeted inhibition of kinases in cancer therapy. Mt Sinai J Med (2010) 0.82

Winning the arms race by improving drug discovery against mutating targets. ACS Chem Biol (2011) 0.81

Second generation tyrosine kinase inhibitors for the treatment of metastatic non-small-cell lung cancer. Transl Respir Med (2014) 0.81

Enhanced dimerization drives ligand-independent activity of mutant epidermal growth factor receptor in lung cancer. Mol Biol Cell (2015) 0.81

Emerging Agents and New Mutations in EGFR-Mutant Lung Cancer. Clin Cancer Res (2015) 0.80

Tyrosine kinase inhibitors in lung cancer. Hematol Oncol Clin North Am (2012) 0.80

Integrating complex genomic datasets and tumour cell sensitivity profiles to address a 'simple' question: which patients should get this drug? BMC Med (2009) 0.79

In silico identification of EGFR-T790M inhibitors with novel scaffolds: start with extraction of common features. Drug Des Devel Ther (2013) 0.79

Intermittent high-dose treatment with erlotinib enhances therapeutic efficacy in EGFR-mutant lung cancer. Oncotarget (2015) 0.79

Activation of the IGF1R pathway potentially mediates acquired resistance to mutant-selective 3rd-generation EGF receptor tyrosine kinase inhibitors in advanced non-small cell lung cancer. Oncotarget (2016) 0.78

Biomarkers of erlotinib response in non-small cell lung cancer tumors that do not harbor the more common epidermal growth factor receptor mutations. Int J Clin Exp Pathol (2015) 0.77

AKT-STAT3 Pathway as a Downstream Target of EGFR Signaling to Regulate PD-L1 Expression on NSCLC cells. J Cancer (2016) 0.76

Interleukin-1 beta transactivates epidermal growth factor receptor via the CXCL1-CXCR2 axis in oral cancer. Oncotarget (2015) 0.76

Low EGFR/MET ratio is associated with resistance to EGFR inhibitors in non-small cell lung cancer. Oncotarget (2015) 0.76

Clonal Evolutionary Analysis during HER2 Blockade in HER2-Positive Inflammatory Breast Cancer: A Phase II Open-Label Clinical Trial of Afatinib +/- Vinorelbine. PLoS Med (2016) 0.75

Epidermal Growth Factor Receptor (EGFR) Pathway Biomarkers in the Randomized Phase III Trial of Erlotinib Versus Observation in Ovarian Cancer Patients with No Evidence of Disease Progression after First-Line Platinum-Based Chemotherapy. Target Oncol (2015) 0.75

A platinum-based hybrid drug design approach to circumvent acquired resistance to molecular targeted tyrosine kinase inhibitors. Sci Rep (2016) 0.75

The Mitogen-Activated Protein Kinase Pathway Facilitates Resistance to the Src Inhibitor Dasatinib in Thyroid Cancer. Mol Cancer Ther (2016) 0.75

Distribution bias analysis of germline and somatic single-nucleotide variations that impact protein functional site and neighboring amino acids. Sci Rep (2017) 0.75

Interleukin-6 identified as an important factor in hypoxia- and aldehyde dehydrogenase-based gefitinib adaptive resistance in non-small cell lung cancer cells. Oncol Lett (2017) 0.75

Articles by these authors

Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib. N Engl J Med (2004) 71.08

Anaplastic lymphoma kinase inhibition in non-small-cell lung cancer. N Engl J Med (2010) 36.78

Signatures of mutational processes in human cancer. Nature (2013) 21.63

Guidelines for the use and interpretation of assays for monitoring autophagy in higher eukaryotes. Autophagy (2007) 20.92

Isolation of rare circulating tumour cells in cancer patients by microchip technology. Nature (2007) 19.33

Systematic identification of genomic markers of drug sensitivity in cancer cells. Nature (2012) 15.91

Clinical features and outcome of patients with non-small-cell lung cancer who harbor EML4-ALK. J Clin Oncol (2009) 15.23

Epidermal growth factor receptor mutations in lung cancer. Nat Rev Cancer (2007) 14.84

Detection of mutations in EGFR in circulating lung-cancer cells. N Engl J Med (2008) 13.54

Gefitinib-sensitizing EGFR mutations in lung cancer activate anti-apoptotic pathways. Science (2004) 11.58

A chromatin-mediated reversible drug-tolerant state in cancer cell subpopulations. Cell (2010) 11.20

Circulating breast tumor cells exhibit dynamic changes in epithelial and mesenchymal composition. Science (2013) 10.87

First-line gefitinib in patients with advanced non-small-cell lung cancer harboring somatic EGFR mutations. J Clin Oncol (2008) 9.43

Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. Proc Natl Acad Sci U S A (2007) 8.23

A two-gene expression ratio predicts clinical outcome in breast cancer patients treated with tamoxifen. Cancer Cell (2004) 8.06

Transforming properties of YAP, a candidate oncogene on the chromosome 11q22 amplicon. Proc Natl Acad Sci U S A (2006) 8.01

Isolation of circulating tumor cells using a microvortex-generating herringbone-chip. Proc Natl Acad Sci U S A (2010) 7.77

Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib. Proc Natl Acad Sci U S A (2005) 6.82

Genomic alterations of anaplastic lymphoma kinase may sensitize tumors to anaplastic lymphoma kinase inhibitors. Cancer Res (2008) 6.71

Circulating tumor cells: approaches to isolation and characterization. J Cell Biol (2011) 6.54

Rapid targeted mutational analysis of human tumours: a clinical platform to guide personalized cancer medicine. EMBO Mol Med (2010) 6.38

Elevated CRAF as a potential mechanism of acquired resistance to BRAF inhibition in melanoma. Cancer Res (2008) 6.05

Molecular predictors of response to epidermal growth factor receptor antagonists in non-small-cell lung cancer. J Clin Oncol (2007) 5.55

Amplification of MET may identify a subset of cancers with extreme sensitivity to the selective tyrosine kinase inhibitor PHA-665752. Proc Natl Acad Sci U S A (2006) 5.23

Dual role for argonautes in microRNA processing and posttranscriptional regulation of microRNA expression. Cell (2007) 5.19

Differential effects of oncogenic K-Ras and N-Ras on proliferation, differentiation and tumor progression in the colon. Nat Genet (2008) 5.07

Inertial focusing for tumor antigen-dependent and -independent sorting of rare circulating tumor cells. Sci Transl Med (2013) 4.74

EGFR-mediated re-activation of MAPK signaling contributes to insensitivity of BRAF mutant colorectal cancers to RAF inhibition with vemurafenib. Cancer Discov (2012) 4.72

A recurrent mutation in PALB2 in Finnish cancer families. Nature (2007) 4.64

Genomics of Drug Sensitivity in Cancer (GDSC): a resource for therapeutic biomarker discovery in cancer cells. Nucleic Acids Res (2012) 4.34

p120-catenin and p190RhoGAP regulate cell-cell adhesion by coordinating antagonism between Rac and Rho. Cell (2006) 4.24

Exon 19 deletion mutations of epidermal growth factor receptor are associated with prolonged survival in non-small cell lung cancer patients treated with gefitinib or erlotinib. Clin Cancer Res (2006) 4.11

Oncogene addiction: setting the stage for molecularly targeted cancer therapy. Genes Dev (2007) 4.11

Epidermal growth factor receptor mutations and gene amplification in non-small-cell lung cancer: molecular analysis of the IDEAL/INTACT gefitinib trials. J Clin Oncol (2005) 4.04

MED12 controls the response to multiple cancer drugs through regulation of TGF-β receptor signaling. Cell (2012) 4.01

Inherited susceptibility to lung cancer may be associated with the T790M drug resistance mutation in EGFR. Nat Genet (2005) 4.00

An X chromosome gene, WTX, is commonly inactivated in Wilms tumor. Science (2007) 4.00

Isolation and characterization of circulating tumor cells from patients with localized and metastatic prostate cancer. Sci Transl Med (2010) 3.90

A common signaling cascade may underlie "addiction" to the Src, BCR-ABL, and EGF receptor oncogenes. Cancer Cell (2006) 3.78

Aberrant overexpression of satellite repeats in pancreatic and other epithelial cancers. Science (2011) 3.77

SCF(FBW7) regulates cellular apoptosis by targeting MCL1 for ubiquitylation and destruction. Nature (2011) 3.69

Acquired resistance to tyrosine kinase inhibitors during cancer therapy. Curr Opin Genet Dev (2008) 3.67

RNA sequencing of pancreatic circulating tumour cells implicates WNT signalling in metastasis. Nature (2012) 3.40

Synthetic lethal interaction of combined BCL-XL and MEK inhibition promotes tumor regressions in KRAS mutant cancer models. Cancer Cell (2012) 3.39

Modulation of Rho GTPase signaling regulates a switch between adipogenesis and myogenesis. Cell (2003) 3.36

Cell line-based platforms to evaluate the therapeutic efficacy of candidate anticancer agents. Nat Rev Cancer (2010) 3.33

REDD1, a developmentally regulated transcriptional target of p63 and p53, links p63 to regulation of reactive oxygen species. Mol Cell (2002) 3.29

MET amplification identifies a small and aggressive subgroup of esophagogastric adenocarcinoma with evidence of responsiveness to crizotinib. J Clin Oncol (2011) 3.27

YAP-dependent induction of amphiregulin identifies a non-cell-autonomous component of the Hippo pathway. Nat Cell Biol (2009) 3.26

BRAF gene amplification can promote acquired resistance to MEK inhibitors in cancer cells harboring the BRAF V600E mutation. Sci Signal (2010) 3.25

Targeting MYCN in neuroblastoma by BET bromodomain inhibition. Cancer Discov (2013) 3.11

Oncogenic activity of epidermal growth factor receptor kinase mutant alleles is enhanced by the T790M drug resistance mutation. Cancer Res (2007) 2.78

Androgen receptor signaling in circulating tumor cells as a marker of hormonally responsive prostate cancer. Cancer Discov (2012) 2.76

Androgen deprivation causes epithelial-mesenchymal transition in the prostate: implications for androgen-deprivation therapy. Cancer Res (2011) 2.71

Transitions between epithelial and mesenchymal states in development and disease. Semin Cell Dev Biol (2008) 2.69

Negative regulation of YAP by LATS1 underscores evolutionary conservation of the Drosophila Hippo pathway. Cancer Res (2008) 2.63