Overcoming Acquired Resistance to AZD9291, A Third-Generation EGFR Inhibitor, through Modulation of MEK/ERK-Dependent Bim and Mcl-1 Degradation

scientific article published in August 2017

Overcoming Acquired Resistance to AZD9291, A Third-Generation EGFR Inhibitor, through Modulation of MEK/ERK-Dependent Bim and Mcl-1 Degradation is …
instance of (P31):
scholarly articleQ13442814

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P356DOI10.1158/1078-0432.CCR-17-1574
P932PMC publication ID5668147
P698PubMed publication ID28765329

P2093author name stringShi-Yong Sun
Shuo Zhang
Taofeek K Owonikoko
Mingwei Chen
Hui Ren
Emily Anderson
Liang Deng
Guojing Zhang
Suresh S Ramalingam
Grant Wu
Puyu Shi
You-Take Oh
Benjamin Legendre
Guoqing Qian
P2860cites workMET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signalingQ27851406
AZD9291 in EGFR inhibitor-resistant non-small-cell lung cancerQ27853158
Rociletinib in EGFR-mutated non-small-cell lung cancerQ27853159
Acquired EGFR C797S mutation mediates resistance to AZD9291 in non-small cell lung cancer harboring EGFR T790M.Q27853162
Gefitinib-induced killing of NSCLC cell lines expressing mutant EGFR requires BIM and can be enhanced by BH3 mimeticsQ28469345
Thr 163 phosphorylation causes Mcl-1 stabilization when degradation is independent of the adjacent GSK3-targeted phosphodegron, promoting drug resistance in cancerQ28484291
BIM mediates EGFR tyrosine kinase inhibitor-induced apoptosis in lung cancers with oncogenic EGFR mutationsQ28756824
Third-Generation Tyrosine Kinase Inhibitors Targeting Epidermal Growth Factor Receptor Mutations in Non-Small Cell Lung CancerQ33740707
Caspase-8 in apoptosis: the beginning of "the end"?Q34143631
Induction of BIM is essential for apoptosis triggered by EGFR kinase inhibitors in mutant EGFR-dependent lung adenocarcinomasQ36026392
The Allelic Context of the C797S Mutation Acquired upon Treatment with Third-Generation EGFR Inhibitors Impacts Sensitivity to Subsequent Treatment StrategiesQ36104980
EGFR Mutations and Resistance to Irreversible Pyrimidine-Based EGFR InhibitorsQ36687288
Combined EGFR/MEK Inhibition Prevents the Emergence of Resistance in EGFR-Mutant Lung CancerQ36775204
Circulating tumour DNA profiling reveals heterogeneity of EGFR inhibitor resistance mechanisms in lung cancer patients.Q37000646
Down-regulation of myeloid cell leukemia-1 through inhibiting Erk/Pin 1 pathway by sorafenib facilitates chemosensitization in breast cancerQ37177949
Overcoming mTOR inhibition-induced paradoxical activation of survival signaling pathways enhances mTOR inhibitors' anticancer efficacyQ37389181
Acquired resistance to epidermal growth factor receptor tyrosine kinase inhibitors in EGFR-mutant non-small cell lung cancer: a new era begins.Q38119594
Clinical approaches to treat patients with non-small cell lung cancer and epidermal growth factor receptor tyrosine kinase inhibitor acquired resistance.Q38504491
Fighting cancer drug resistance: Opportunities and challenges for mutation-specific EGFR inhibitors.Q38506135
Third-generation epidermal growth factor receptor tyrosine kinase inhibitors in advanced nonsmall cell lung cancerQ38684074
Met gene amplification and protein hyperactivation is a mechanism of resistance to both first and third generation EGFR inhibitors in lung cancer treatmentQ38756221
Acquired Resistance to the Mutant-Selective EGFR Inhibitor AZD9291 Is Associated with Increased Dependence on RAS Signaling in Preclinical ModelsQ38887681
The PI3 kinase inhibitor NVP-BKM120 induces GSK3/FBXW7-dependent Mcl-1 degradation, contributing to induction of apoptosis and enhancement of TRAIL-induced apoptosisQ39170414
Elevated expression of eukaryotic translation initiation factor 4E is associated with proliferation, invasion and acquired resistance to erlotinib in lung cancerQ39413724
FAS and NF-κB signalling modulate dependence of lung cancers on mutant EGFR.Q39571776
Heterogeneous mechanisms of primary and acquired resistance to third-generation EGFR inhibitorsQ39716418
Death receptor regulation and celecoxib-induced apoptosis in human lung cancer cells.Q40486081
MCL1 is phosphorylated in the PEST region and stabilized upon ERK activation in viable cells, and at additional sites with cytotoxic okadaic acid or taxolQ40537978
Extracellular signal-regulated kinases 1/2 are serum-stimulated "Bim(EL) kinases" that bind to the BH3-only protein Bim(EL) causing its phosphorylation and turnoverQ40606380
Phosphorylation of Bim-EL by Erk1/2 on serine 69 promotes its degradation via the proteasome pathway and regulates its proapoptotic function.Q40626751
Activation of the ERK1/2 signaling pathway promotes phosphorylation and proteasome-dependent degradation of the BH3-only protein, Bim.Q40662652
Mechanisms of apoptosis induced by the synthetic retinoid CD437 in human non-small cell lung carcinoma cellsQ40954596
Reciprocal and complementary role of MET amplification and EGFR T790M mutation in acquired resistance to kinase inhibitors in lung cancerQ42815191
High MET amplification level as a resistance mechanism to osimertinib (AZD9291) in a patient that symptomatically responded to crizotinib treatment post-osimertinib progressionQ44828642
Differential effects of synthetic nuclear retinoid receptor-selective retinoids on the growth of human non-small cell lung carcinoma cellsQ73838303
Regulatory phosphorylation of Bim: sorting out the ERK from the JNKQ81833475
P433issue21
P407language of work or nameEnglishQ1860
P304page(s)6567-6579
P577publication date2017-08-01
P1433published inClinical Cancer ResearchQ332253
P1476titleOvercoming Acquired Resistance to AZD9291, A Third-Generation EGFR Inhibitor, through Modulation of MEK/ERK-Dependent Bim and Mcl-1 Degradation
P478volume23

Reverse relations

cites work (P2860)
Q52594173Acquired resistance to AZD9291 as an upfront treatment is dependent on ERK signaling in a preclinical model.
Q96129358Clonal Evolution and Heterogeneity of Osimertinib Acquired Resistance Mechanisms in EGFR Mutant Lung Cancer
Q91742514Concurrent inhibition of ErbB family and MEK/ERK kinases to suppress non-small cell lung cancer proliferation
Q92898855DYRK1A inhibition suppresses STAT3/EGFR/Met signalling and sensitizes EGFR wild-type NSCLC cells to AZD9291
Q89818780Deguelin suppresses non-small cell lung cancer by inhibiting EGFR signaling and promoting GSK3β/FBW7-mediated Mcl-1 destabilization
Q60044511Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia
Q91844724ERK inhibition effectively overcomes acquired resistance of epidermal growth factor receptor-mutant non-small cell lung cancer cells to osimertinib
Q64089193Emerging therapies for non-small cell lung cancer
Q91812931Formononetin inhibits tumor growth by suppression of EGFR-Akt-Mcl-1 axis in non-small cell lung cancer
Q91937343Impact of MET alterations on targeted therapy with EGFR-tyrosine kinase inhibitors for EGFR-mutant lung cancer
Q92060167Inhibition of EGFR Signaling and Activation of Mitochondrial Apoptosis Contribute to Tanshinone IIA-Mediated Tumor Suppression in Non-Small Cell Lung Cancer Cells
Q96122560MEK or ERK inhibition effectively abrogates emergence of acquired osimertinib resistance in the treatment of epidermal growth factor receptor-mutant lung cancers
Q92942818MET inhibitors for targeted therapy of EGFR TKI-resistant lung cancer
Q99210175Marked synergy by vertical inhibition of EGFR signaling in NSCLC spheroids shows SOS1 is a therapeutic target in EGFR-mutated cancer
Q60929137Overcoming Resistance to AC0010, a Third Generation of EGFR Inhibitor, by Targeting c-MET and BCL-2
Q89461554Overcoming acquired resistance of EGFR-mutant NSCLC cells to the third generation EGFR inhibitor, osimertinib, with the natural product honokiol
Q93062391Overcoming acquired resistance of epidermal growth factor receptor-mutant non-small cell lung cancer cells to osimertinib by combining osimertinib with the histone deacetylase inhibitor panobinostat (LBH589)
Q47450308Pharmacokinetic drug evaluation of osimertinib for the treatment of non-small cell lung cancer.
Q90590454Targeting apoptosis in cancer therapy
Q91254638Targeting the EMT transcription factor TWIST1 overcomes resistance to EGFR inhibitors in EGFR-mutant non-small-cell lung cancer
Q64112445The Third-Generation EGFR Inhibitor, Osimertinib, Promotes c-FLIP Degradation, Enhancing Apoptosis Including TRAIL-Induced Apoptosis in NSCLC Cells with Activating EGFR Mutations
Q64115764The anti-tumor growth effect of a novel agent DMAMCL in rhabdomyosarcoma in vitro and in vivo
Q55223055The continued EGFR-TKI with cytotoxic chemotherapy at progression-poison or medicine?
Q50047476The irreversible ERBB1/2/4 inhibitor neratinib interacts with the BCL-2 inhibitor venetoclax to kill mammary cancer cells.
Q49887956Third generation EGFR TKIs: current data and future directions
Q50104127Treatment of EGFR T790M-Positive Non-Small Cell Lung Cancer

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