EGFR inhibitors
In Silico Pharmacokinetics Studies for Quinazolines Proposed as EGFR Inhibitors
... highly active [30]), which are selected and colored in red Figure 2(a). Among these compounds, some can be identified as potentially having favorable pharmacokinetics properties by calculating the corresponding Log P. ...
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QSAR based model for discriminating EGFR inhibitors and non-inhibitors using Random forest
... in EGFR inhibitors like gefitinib, EKB-569, lapatinib and act as linkers have high frequency of occurrence (Figure ...known EGFR inhibitors gefitinib, ...
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Low EGFR/MET ratio is associated with resistance to EGFR inhibitors in non-small cell lung cancer
... with EGFR wild- type genotype who experienced a prolonged clinical response (006-004) exhibited high EGFR/MET ...two EGFR-mutant patients who did not respond to EGFR TKIs (006-032 and 006-044) ...
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Berberine inhibits EGFR signaling and enhances the antitumor effects of EGFR inhibitors in gastric cancer
... Berberine was tested for its ability to enhance the antitumor effects of EGFR inhibitors in gastric cancer. We used erlotinib and cetuximab in SGC7901, BGC823 cell culture experiments by MTT assays. ...
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Radiotherapy plus EGFR inhibitors: synergistic modalities
... targeting EGFR in combination with radiation. Until now, cetuximab, an anti-EGFR monoclonal antibody, is the only targeted agent that has been shown to improve overall survival in combination with radiation ...
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Clinical Effects of EGFR Inhibitors on EGFR exon19 and 21 Mutationsin Lung Cancer
... shows EGFR inhibitors for the treatment of EGFR exon 19 and 21 exon safety of mutations in lung cancer patients, the incidence of adverse reactions with li-li guo (Guo Lili, 2014) ...of EGFR ...
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Adaptive and Acquired Resistance to EGFR Inhibitors Converge on the MAPK Pathway
... of EGFR TKIs [18, ...pathway inhibitors are undergoing clinical ...with EGFR inhibitors and MET or MAPK kinase inhibitors should be considered for NSCLC patients bearing EGFR ...
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The activation of EGFR promotes myocardial tumor necrosis factor-α production and cardiac failure in endotoxemia
... of EGFR activation on the generation of TNF-α and the occurrence of cardiac dysfuncetion during sepsis, PD168393 and erlotinib (both are EGFR inhibitors) were applied to decreased the production of ...
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EGFR tyrosine kinase inhibitors promote pro-caspase-8 dimerization that sensitizes cancer cells to DNA-damaging therapy
... the EGFR inhibitor and DNA-damaging ...that EGFR inhibitors promoted pro-caspase-8 homodimerization by inhibiting ERK pathway signaling, while doxorubicin promoted ...of EGFR tyrosine kinase ...
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Mechanisms of resistance to EGFR-targeted drugs: lung cancer
... the EGFR T790M gatekeeper mutation and tried to answer the question of whether resistance depends on selection of pre-existing clones or on acquisition of validated genetic resistance mechanisms after a period of ...
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Gillis_unc_0153D_16817.pdf
... first-generation EGFR inhibitor resistance due to secondary EGFR mutations or bypass track ...potent inhibitors of EGFR, such as the FDA-approved second-generation EGFR inhibitor, ...
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Nuclear localization of epidermal growth factor receptor (EGFR) in ameloblastomas
... with EGFR-inhibitors is currently in clinical practice, having demonstrated important anti- tumor activity in patients with head and neck squamous cell carcinoma, metastatic colorectal cancer, lung cancer ...
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Orthogonal targeting of EGFRvIII expressing glioblastomas through simultaneous EGFR and PLK1 inhibition
... to EGFR inhibitors, suggesting these resistant clones retain oncogenic stress that required PLK1 ...of EGFR inhibitors in the Ink4a/ Arf(-/-) EGFRvIII model, durable response was not achieved ...
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Anti-EGFR monoclonal antibodies and EGFR tyrosine kinase inhibitors as combination therapy for triple-negative breast cancer
... targeting EGFR rely on the use of monoclonal antibodies (mAbs) and small molecule EGFR tyrosine kinase inhibitors ...and EGFR-TKIs competitively block the binding of adenosine 5′ triphosphate ...
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Molecular mechanisms of resistance in epidermal growth factor receptor-mutant lung adenocarcinomas
... of EGFR inhibitors effective against T790M has recently ...These inhibitors, for example WZ4002, AZD9291 or CO-1686, have been specifically designed to inhibit EGFR-T790M and are different to ...
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Genomic markers of panitumumab resistance including ERBB2/ HER2 in a phase II study of KRAS wild-type (wt) metastatic colorectal cancer (mCRC).
... Colorectal cancer (CRC) has high rates of metastasis and recurrence [1, 2]. Therapy for advanced disease includes epidermal growth factor receptor (EGFR)-inhibitors, including cetuximab and panitumumab, ...
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Favorable pleiotropic effects of sodium glucose cotransporter 2 inhibitors: head-to-head comparisons with dipeptidyl peptidase-4 inhibitors in type 2 diabetes patients
... SGLT2 inhibitors is associated with better cardio- vascular outcomes than DPP4 inhibitors ...SGLT2 inhibitors compared to DPP4 inhibitors [7, 8, ...SGLT2 inhibitors were associated with ...
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<p>Dual Targeting of the Epidermal Growth Factor Receptor Using Combination of Nimotuzumab and Erlotinib in Advanced Non-Small-Cell Lung Cancer with Leptomeningeal Metastases: A Report of Three Cases</p>
... combining EGFR targeting with the tyrosine kinase inhibitor ge fi tinib and monoclonal antibody cetuximab has been ...of EGFR with nimotuzumab plus ge fi tinib was not associated with better outcomes than ge ...
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Novel agents and strategies for overcoming EGFR TKIs resistance
... includes EGFR/HER1, ERBB2/HER2, ERBB3/HER3 and ERBB4/HER4. Somatic EGFR mutations result in con- formational changes and the activation of downstream sig- ...first-generation EGFR TKIs that ...
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Genomic profiling toward precision medicine in non-small cell lung cancer: getting beyond EGFR
... While success has been demonstrated in LAC patients with mutated EGFR or gene rearrangements in ALK, therapeutic resistance is pervasive in these subgroups. More importantly, the majority of NSCLC patients do not ...
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