Study summary · research use only
Inhibitor of ghrelin receptor reverses gefitinib resistance in lung cancer
Plain-language summary
Paraphrased from the published abstract below — not a verdict on whether anything works.
In this in vitro study using human-derived lung cancer cell lines (HCC827/GR and H1650; species not specified beyond human cell lines), the authors examined whether the ghrelin receptor antagonist D-lys-3-GHRP-6 affects gefitinib resistance. GHSR was found to be overexpressed in HCC827/GR cells compared with parental cells, along with increased p-AKT and p-ERK1/2; D-lys-3-GHRP-6 treatment was associated with decreased p-AKT and p-ERK1/2 expression in HCC827/GR cells. In both H1650 and HCC827/GR cells, combining D-lys-3-GHRP-6 with gefitinib was associated with reduced cell proliferation and Bcl2 protein level, and increased apoptosis and cleaved-caspase3 protein level, compared with control, with no significant difference observed between the control and gefitinib-alone groups.
Abstract
Gefitinib is the first-generation EGFR tyrosine kinase inhibitor (EGFR-TKI), which is used in the treatment of NCSLC patients through interrupting EGFR signaling pathway. Although gefitinib prolongs patients' progression-free survival (PFS), acquired resistance occurs in advanced NSCLC patients. In this study, we mainly investigated the effects of antagonist for ghrelin-R (D-lys-3-GHRP-6) on conquering acquired gefitinib resistance in human lung cancer cells. We found that GHSR was overexpressed in our established HCC827/GR cells compared with parental cells, accompanied with increase of p-AKT and p-ERK1/2. Treatment of D-lys-3-GHRP-6 significantly decreased p-AKT and p-ERK1/2 expression in HCC827/GR cells. H1650 cells and HCC827/GR cells were treated with control, gefitinib, D-lys-3-GHRP-6 and D-lys-3-GHRP-6 + gefitinib, respectively. In H1650 and HCC827/GR cells, combination of D-lys-3-GHRP-6 and gefitinib significantly inhibited cell proliferation and Bcl2 protein level, induced the cell apoptosis and cleaved-caspase3 protein level compared with control group, while there was no significant difference between control and gefitinib group.
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