ArticlePloS one2016
GSK621 Targets Glioma Cells via Activating AMP-Activated Protein Kinase Signalings.
Article in PloS one, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed, 24 citations in OpenAlex.
- AMP-activated protein kinase mediates adaptation of glioblastoma cells to conditions of the tumor microenvironment.Journal of experimental & clinical cancer research : CR · 2025Article
- Small Molecule Modulators of AMP-Activated Protein Kinase (AMPK) Activity and Their Potential in Cancer Therapy.Journal of medicinal chemistry · 2025Review
- New insights into the role of tetraspanin 6, 7, and 8 in physiology and pathology.Cancer medicine · 2024Review
- EID3 Promotes Glioma Cell Proliferation and Survival by Inactivating AMPKα1.Journal of Korean Neurosurgical Society · 2022Article
- Metformin Protects Against Diabetes-Induced Cognitive Dysfunction by Inhibiting Mitochondrial Fission Protein DRP1.Frontiers in pharmacology · 2022Article
- Article
- TSPAN8 as a Novel Emerging Therapeutic Target in Cancer for Monoclonal Antibody Therapy.Biomolecules · 2020Review
- Lnc-THOR silencing inhibits human glioma cell survival by activating MAGEA6-AMPK signaling.Cell death & disease · 2019Article
- Finely-tuned regulation of AMP-activated protein kinase is crucial for human adult erythropoiesis.Haematologica · 2019Article
- Article
- Targeted activation of AMPK by GSK621 ameliorates H2O2-induced damages in osteoblasts.Oncotarget · 2017Article
- Gab3 overexpression in human glioma mediates Akt activation and tumor cell proliferation.PloS one · 2017Article
Corrections and comments
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Authors and funding
8 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Here, we studied the anti-glioma cell activity by a novel AMP-activated protein kinase (AMPK) activator GSK621. We showed that GSK621 was cytotoxic to human glioma cells (U87MG and U251MG lines), possibly via provoking caspase-dependent apoptotic cell death. Its cytotoxicity was alleviated by caspase inhibitors. GSK621 activated AMPK to inhibit mammalian target of rapamycin (mTOR) and downregulate Tetraspanin 8 (Tspan8) in glioma cells. AMPK inhibition, through shRNA knockdown of AMPKα or introduction of a dominant negative (T172A) AMPKα, almost reversed GSK621-induced AMPK activation, mTOR inhibition and Tspan8 degradation. Consequently, GSK621's cytotoxicity in glioma cells was also significantly attenuated by AMPKα knockdown or mutation. Further studies showed that GSK621, at a relatively low concentration, significantly potentiated temozolomide (TMZ)'s sensitivity and lethality against glioma cells. We summarized that GSK621 inhibits human glioma cells possibly via activating AMPK signaling. This novel AMPK activator could be a novel and promising anti-glioma cell agent.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.