Journal: Genes & Diseases

Article Title: PDK1 elevation was induced by epigenetic modifications of KDM3A and METTL16 to mediate TKI resistance and cancer development

doi: 10.1016/j.gendis.2025.101947

Figure Lengend Snippet: PDK1 inhibitor JX06 and gefitinib synergistically induced cell apoptosis in gefitinib-resistant lung cancer cells. (A) The protein expression levels of PDK were reduced upon the treatment of PDK1 inhibitor JX06 in PC-9 and PC-9/G cells. (B) B2B and PC-9/G cells were treated with different concentrations of JX06 for 48 h. The cell viabilities were determined by CCK-8. (C – E) The synergy effect between JX06 and gefitinib was determined and analyzed with CompuSyn software. (F) The apoptosis rates were analyzed with flow cytometry after the combined treatment of gefitinib and JX06. (G) The TUNEL assay was performed with the indicated treatment in PC-9/G cells. (H) The cells treated as described were stained with the JC-1 probe and detected using a fluorescence microscope. Red fluorescence indicates the aggregation form of JC-1, showing increased mitochondrial membrane potential (ΔΨm). Green fluorescence indicates the monomeric form of JC-1, which indicates reduced mitochondrial membrane potential (ΔΨm). Data were statistically analyzed with Student’s t -test, and values were shown as mean ± standard deviation. ∗ P < 0.05 and ∗∗ P < 0.01.

Article Snippet: Gefitinib and JX06 were purchased from MedChemExpress (Shanghai, China).

Techniques: Expressing, CCK-8 Assay, Software, Flow Cytometry, TUNEL Assay, Staining, Fluorescence, Microscopy, Membrane, Standard Deviation

Journal: Genes & Diseases

Article Title: PDK1 elevation was induced by epigenetic modifications of KDM3A and METTL16 to mediate TKI resistance and cancer development

doi: 10.1016/j.gendis.2025.101947

Figure Lengend Snippet: Dual-treatment of JX06 and gefitinib significantly inhibited tumor growth in vivo . The PC-9/G cells (5 × 10 6 cells) were inoculated subcutaneously on the back of nude mice. When the tumor reached approximately 5 × 5 mm 2 , the nude mice were randomly divided into four groups ( n = 5 per group) and treated with saline, gefitinib (25 mg/kg), JX06 (30 mg/kg), or gefitinib (25 mg/kg) plus JX06 (30 mg/kg). (A – C) Tumor volumes and weights were analyzed, and dual-treatment of JX06 and gefitinib significantly inhibited tumor volumes and tumor weights. (D) Animal weights between the four groups did not show any significant difference. (E) Representative images of immunohistochemical staining of Ki67 and CD31 in paraffin-embedded xenograft tumor tissues, and the expression levels of Ki67 and CD31 were quantified for six microscopic fields of the tumor samples. Data were statistically analyzed with Student’s t -test, and values were shown as mean ± standard deviation. ∗ P < 0.05 and ∗∗ P < 0.01.

Article Snippet: Gefitinib and JX06 were purchased from MedChemExpress (Shanghai, China).

Techniques: In Vivo, Saline, Immunohistochemical staining, Staining, Expressing, Standard Deviation