ArticleMolecular medicine reports2015
LW6, a hypoxia-inducible factor 1 inhibitor, selectively induces apoptosis in hypoxic cells through depolarization of mitochondria in A549 human lung cancer cells.
Article in Molecular medicine reports, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed, 35 citations in OpenAlex.
- Sodium Sulfite as an Oxygen-Depletion-Based Chemical Model of Tumor Hypoxia In Vitro.Applied biochemistry and biotechnology · 2026Article
- Myofibroblast- specific autophagy drives cyst growth in autosomal dominant polycystic kidney disease.Cell communication and signaling : CCS · 2026Article
- Effect of HIF-1α inhibitor LW6 on chondrogenic properties of mesenchymal stromal cells and chondrocytes in cell sheets under physioxia.Journal of biological engineering · 2026Article
- BCL2-Associated Transcription Factor 1 Promotes SRC/Hypoxia-Inducible Factor 1 Subunit α-Mediated Cancer Stemness in Radioresistant Triple-Negative Breast Cancer.Oncology research · 2026Article
- Hypoxia Inhibitor Improves Iodine Uptake Disorder in Thyroid Cancer Through the hsa_circ_0023990/miR-448/DNMT1/NIS Axis.Cancer science · 2025Article
- Hypoxia Regulates the Proliferation and Apoptosis of Coronary Artery Smooth Muscle Cells Through HIF-1α Mediated Autophagy in Yak.Biomolecules · 2025Article
- The hypoxic microenvironment ofFrontiers in immunology · 2025Article
- Hypoxia drives estrogen receptor β-mediated cell growth via transcription activation in non-small cell lung cancer.Journal of molecular medicine (Berlin, Germany) · 2024Article
- Resistance to Gemcitabine in Pancreatic Ductal Adenocarcinoma: A Physiopathologic and Pharmacologic Review.Cancers · 2022Review
- Hypoxia-inducible factor 1-alpha is a driving mechanism linking chronic obstructive pulmonary disease to lung cancer.Frontiers in oncology · 2022Review
- Screening of radiotracer for diagnosis of colorectal cancer liver metastasis based on MACC1-SPON2.Abdominal radiology (New York) · 2021Article
- Antioxidative Stress: Inhibiting Reactive Oxygen Species Production as a Cause of Radioresistance and Chemoresistance.Oxidative medicine and cellular longevity · 2021Review
- DNA damage response signaling pathways and targets for radiotherapy sensitization in cancer.Signal transduction and targeted therapy · 2020Review
- Immunogenomic Profiling and Classification of Prostate Cancer Based on HIF-1 Signaling Pathway.Frontiers in oncology · 2020Article
- Activation of TWIST Transcription by Chromatin Remodeling Protein BRG1 Contributes to Liver Fibrosis in Mice.Frontiers in cell and developmental biology · 2020Article
- Metformin and LW6 impairs pancreatic cancer cells and reduces nuclear localization of YAP1.Journal of Cancer · 2020Article
- Development of a Ternary Solid Dispersion Formulation of LW6 to Improve the In Vivo Activity as a BCRP Inhibitor: Preparation and In Vitro/In Vivo Characterization.Pharmaceutics · 2019Article
- Metformin attenuates hypoxia-induced resistance to cisplatin in the HepG2 cell line.Oncology letters · 2019Article
- Noninvasive evaluation ofScientific reports · 2018Article
- Montelukast inhibits hypoxia inducible factor-1α translation in prostate cancer cells.Cancer biology & therapy · 2018Article
Corrections and comments
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Authors and funding
9 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Hypoxia‑inducible factor 1 (HIF‑1) activates the transcription of genes that act upon the adaptation of cancer cells to hypoxia. LW6, an HIF‑1 inhibitor, was hypothesized to improve resistance to cancer therapy in hypoxic tumors by inhibiting the accumulation of HIF‑1α. A clear anti‑tumor effect under low oxygen conditions would indicate that LW6 may be an improved treatment strategy for cancer in hypoxia. In the present study, the HIF‑1 inhibition potential of LW6 on the growth and apoptosis of A549 lung cancer cells in association with oxygen availability was evaluated. LW6 was observed to inhibit the expression of HIF‑1α induced by hypoxia in A549 cells at 20 mM, independently of the von Hippel‑Lindau protein. In addition, at this concentration, LW6 induced hypoxia‑selective apoptosis together with a reduction in the mitochondrial membrane potential. The intracellular reactive oxygen species levels increased in LW6‑treated hypoxic A549 cells and LW6 induced a hypoxia‑selective increase of mitochondrial O2•‑. In conclusion, LW6 inhibited the growth of hypoxic A549 cells by affecting the mitochondria. The inhibition of the mitochondrial respiratory chain is suggested as a potentially effective strategy to target apoptosis in cancer cells.
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