title: Impact of H3K27 Demethylase Inhibitor GSKJ4 on NSCLC Cells Alone and in Combination with Metformin.
abstract: GSKJ4, an H3K27 demethylase inhibitor, reportedly exhibits antitumor activity against specific cancers harboring genetic alterations in genes encoding chromatin modulators. However, its potential as an anticancer agent against human cancers not associated with such genetic alterations, including non-small cell lung cancer (NSCLC), remains unknown.
  
  
  
  The effect of GSKJ4 on the growth of three NSCLC cell lines and normal lung fibroblasts was investigated using the WST-8, dye exclusion, and colony formation assays.
  
  
  
  GSKJ4, alone and in combination with an anti-diabetic drug metformin, induced cell death and inhibited the growth of NSCLC cell lines efficiently at concentrations non-toxic to normal cells, irrespective of their genetic backgrounds (mutations in the KRAS, TP53 and EGFR genes) and also of their resistance to cisplatin and paclitaxel.
  
  
  
  GSKJ4, being a promising anticancer agent for NSCLC, may be effective against a wider spectrum of cancers than previously thought.
authors: Department of Molecular Cancer Science, Yamagata University School of Medicine, Yamagata, Japan.|Second Department of Surgery, Yamagata University School of Medicine, Yamagata, Japan.
authors: Hikaru
authors: H
authors: Watarai
authors: Department of Molecular Cancer Science, Yamagata University School of Medicine, Yamagata, Japan ckitanak@med.id.yamagata-u.ac.jp m-okada@med.id.yamagata-u.ac.jp.
authors: Masashi
authors: M
authors: Okada
authors: Department of Molecular Cancer Science, Yamagata University School of Medicine, Yamagata, Japan.
authors: Kenta
authors: K
authors: Kuramoto
authors: Department of Molecular Cancer Science, Yamagata University School of Medicine, Yamagata, Japan.|Department of Obstetrics and Gynecology, Yamagata University School of Medicine, Yamagata, Japan.
authors: Hiroyuki
authors: H
authors: Takeda
authors: Department of Molecular Cancer Science, Yamagata University School of Medicine, Yamagata, Japan.|Department of Clinical Oncology, Yamagata University School of Medicine, Yamagata, Japan.
authors: Hirotsugu
authors: H
authors: Sakaki
authors: Department of Molecular Cancer Science, Yamagata University School of Medicine, Yamagata, Japan.|Department of Obstetrics and Gynecology, Yamagata University School of Medicine, Yamagata, Japan.
authors: Shuhei
authors: S
authors: Suzuki
authors: Department of Molecular Cancer Science, Yamagata University School of Medicine, Yamagata, Japan.|Research Institute for Promotion of Medical Sciences, Yamagata University Faculty of Medicine, Yamagata, Japan.
authors: Shizuka
authors: S
authors: Seino
authors: Second Department of Surgery, Yamagata University School of Medicine, Yamagata, Japan.
authors: Hiroyuki
authors: H
authors: Oizumi
authors: Second Department of Surgery, Yamagata University School of Medicine, Yamagata, Japan.
authors: Mitsuaki
authors: M
authors: Sadahiro
authors: Department of Molecular Cancer Science, Yamagata University School of Medicine, Yamagata, Japan ckitanak@med.id.yamagata-u.ac.jp m-okada@med.id.yamagata-u.ac.jp.|Research Institute for Promotion of Medical Sciences, Yamagata University Faculty of Medicine, Yamagata, Japan.
authors: Chifumi
authors: C
authors: Kitanaka
mesh_terms: D001552:Benzazepines / Q000494:pharmacology*; D002289:Carcinoma, Non-Small-Cell Lung / Q000473:pathology*; D045744:Cell Line, Tumor; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D006801:Humans; D008175:Lung Neoplasms / Q000473:pathology*; D008687:Metformin / Q000494:pharmacology*; D011743:Pyrimidines / Q000494:pharmacology*
chemical_list: D001552:Benzazepines; D004791:Enzyme Inhibitors; C000593030:GSK-J4; D011743:Pyrimidines; D008687:Metformin
keywords: Epigenetic; chemotherapy; clonogenic survival; global histone modification