1. Academic Validation
  2. ORY-1001 Suppresses Cell Growth and Induces Apoptosis in Lung Cancer Through Triggering HK2 Mediated Warburg Effect

ORY-1001 Suppresses Cell Growth and Induces Apoptosis in Lung Cancer Through Triggering HK2 Mediated Warburg Effect

  • Front Pharmacol. 2018 Dec 4:9:1411. doi: 10.3389/fphar.2018.01411.
Zhaoliang Lu 1 Yanke Guo 1 Xiaoya Zhang 1 Jing Li 2 Leilei Li 1 Shuai Zhang 3 4 Changliang Shan 1 2
Affiliations

Affiliations

  • 1 The First Affiliated Hospital, Biomedical Translational Research Institute, Jinan University, Guangzhou, China.
  • 2 State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin, China.
  • 3 School of Integrative Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin, China.
  • 4 Department of Medical Biochemistry and Molecular Biology, School of Medicine, Jinan University, Guangzhou, China.
Abstract

ORY-1001, an inhibitor of covalent lysine (K)-specific demethylase 1A (KDM1A), has been used as a therapy for the treatment of acute leukemia. However, the underlying mechanisms of Anticancer are still not fully elucidated. Here, we report that KDM1A is highly expressed in lung cancers, where it appears to drive aggressive growth. Furthermore, lung Cancer patients with higher KDM1A levels have worse survival outcomes than patients with lower KDM1A levels. Interestingly, ORY-1001significantly inhibited the cell proliferation, colony formation, cell cycle, and induced Apoptosis, by regulating the Warburg effect through controlling Hexokinases 2 (HK2) expression. In summary, these results indicate that ORY-1001 could inhibit the growth of lung Cancer cells via regulating the Warburg effect by controlling HK2.

Keywords

Hexokinases 2; Warburg effect; cell proliferation; lung cancer; lysine (K)-specific demethylase 1A.

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