Structural Basis for Inhibition of Mutant EGFR with Lazertinib (YH25448).
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DOI: 10.1021/acsmedchemlett.2c00213
Abstract: Lazertinib (YH25448) is a novel third-generation tyrosine kinase inhibitor (TKI) developed as a treatment for EGFR mutant non-small cell lung cancer. To better understand the nature of lazertinib inhibition, we determined crystal structures of lazertinib… read more here.
Keywords: lazertinib yh25448; lazertinib; inhibition; chemistry ... See more keywords
Structure-activity exploration of a small-molecule allosteric inhibitor of T790M/L858R double mutant EGFR
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DOI: 10.1080/14756366.2022.2145284
Abstract: Abstract EGFR is a protein kinase whose aberrant activity is frequently involved in the development of non-small lung cancer (NSCLC) drug resistant forms. The allosteric inhibition of this enzyme is currently one among the most… read more here.
Keywords: structure activity; allosteric inhibitor; mutant egfr; egfr ... See more keywords
Comparative effectiveness of concurrent chemoradiotherapy versus EGFR‐tyrosine kinase inhibitors for the treatment of clinical stage IIIb lung adenocarcinoma patients with mutant EGFR
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DOI: 10.1111/1759-7714.12847
Abstract: The standard of care for fit locally advanced non‐small cell lung cancer (NSCLC) patients is concurrent chemoradiotherapy (CCRT). However, in a subset of patients with lung adenocarcinoma with mutant EGFR (LA‐mEGFR), the role of EGFR‐tyrosine… read more here.
Keywords: concurrent chemoradiotherapy; lung adenocarcinoma; kinase inhibitors; mutant egfr ... See more keywords
Development and Optimization of Osimertinib-loaded Biodegradable Polymeric Nanoparticles Enhance In-vitro Cytotoxicity in Mutant EGFR NSCLC Cell Models and In-vivo Tumor Reduction in H1975 Xenograft Mice Models
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DOI: 10.1208/s12249-022-02314-9
Abstract: Osimertinib (OMB), a third-generation EGFR inhibitor, specifically and irreversibly inhibits EGFRT790M mutant form. Nevertheless, its clinical use is limited due to poor solubility, low absorption, and oral bioavailability. To overcome the low therapeutic capabilities of… read more here.
Keywords: omb chs; omb; mutant egfr; h1975 ... See more keywords
Dual effects of a CpG-DNAzyme targeting mutant EGFR transcripts in lung cancer cells: TLR9 activation and EGFR downregulation
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DOI: 10.5483/bmbrep.2018.51.1.163
Abstract: Non-small-cell lung cancer (NSCLC) is commonly caused by a mutation in the epidermal growth factor receptor (EGFR) and subsequent aberrant EGFR signaling with uncontrolled kinase activity. A deletion mutation in EGFR exon 19 is frequently… read more here.
Keywords: egfr; egfr downregulation; mutant egfr; lung cancer ... See more keywords