2015
DOI: 10.18632/oncotarget.3380
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Targeting the degradation of AXL receptor tyrosine kinase to overcome resistance in gefitinib-resistant non-small cell lung cancer

Abstract: Acquired resistance to epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs), such as gefitinib, remains a major problem in non-small cell lung cancer (NSCLC) treatment. Increased activation of AXL has been identified as a novel mechanism for acquired resistance to EGFR-TKIs in NSCLC treatment. However, the cause of uncontrolled AXL expression is not fully understood. Here, we first demonstrate that AXL is overexpressed in an acquired gefitinib-resistant cell line (H292-Gef) as a result of sl… Show more

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Cited by 66 publications
(83 citation statements)
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“…4a), an antitumor agent that effectively inhibits the proliferation of NSCLC cells and exhibits synergistic effect when combined with gefitinib272831. Treatment with 10 nM YD for 24 h dramatically increased SerpinB2 expression in H292-Gef cells (Fig.…”
Section: Resultsmentioning
confidence: 97%
“…4a), an antitumor agent that effectively inhibits the proliferation of NSCLC cells and exhibits synergistic effect when combined with gefitinib272831. Treatment with 10 nM YD for 24 h dramatically increased SerpinB2 expression in H292-Gef cells (Fig.…”
Section: Resultsmentioning
confidence: 97%
“…Then, these mice were treated with vehicle or LDN-193189 (4 mg/kg for PC9-Gef, 5 mg/kg for H1993-Gef) for 3 weeks (5 days on, 2 days off). Tumor volumes were determined using digital calipers using the formula (L × W × M × π)/6 as described previously 27 . The body weight of each mouse was also monitored for toxicity analyses.…”
Section: Methodsmentioning
confidence: 99%
“…Receptor ubiquitination mediated by the Casitas B-lineage lymphoma (Cbl) E3 ubiquitin ligases can regulate the abundance of AXL in several cells (39, 40). Likewise, increased AXL half-life by impaired degradation of the receptor can occur in lung cancer cell lines, resulting in the net increase of AXL levels (41). …”
Section: Introductionmentioning
confidence: 99%