Related Experiment Video
Updated: Jun 2, 2026

09:23
Coculture Assays to Study Macrophage and Microglia Stimulation of Glioblastoma Invasion
Published on: October 20, 2016
Baclofen Inhibits Glioma Proliferation via the MEK/ERK/CREB Pathway
Boqi Zhou1,2,3, Liping Shen2,3, Xiaojie Lu1,2,3
1Wuxi School of Medicine, Jiangnan University, Wuxi, China.
Oncology Research
|June 1, 2026
Summary
Baclofen, a GABAB receptor agonist, inhibits glioma cell growth, migration, and invasion. It targets the MEK/ERK/CREB pathway and epithelial-mesenchymal transition, showing therapeutic potential for glioma treatment.
Area of Science:
- Neuroscience
- Oncology
- Molecular Biology
Background:
- Gamma-aminobutyric acid type B (GABAB) receptors are implicated in cancer progression.
- Baclofen exhibits antitumor properties across various cancer types.
- The precise role and mechanisms of baclofen in glioma remain under investigation.
Purpose of the Study:
- To investigate the anti-glioma effects of baclofen.
- To elucidate the molecular pathways targeted by baclofen in glioma cells.
Main Methods:
- In vitro studies using glioma cell lines to assess baclofen's impact on proliferation, migration, and invasion.
- Transcriptome sequencing and Western blotting to identify molecular mechanisms.
- In vivo validation using a subcutaneous glioma xenograft model.
Main Results:
- Baclofen dose-dependently inhibited glioma cell proliferation, migration, and invasion.
- Baclofen suppressed phosphorylation in the MEK/ERK/CREB/FOS signaling pathway via GABAB receptors.
- Baclofen modulated the epithelial-mesenchymal transition (EMT)-like program.
- Effects were reversed by the GABAB antagonist CGP35348.
- In vivo studies confirmed baclofen's anti-glioma efficacy.
Conclusions:
- Baclofen demonstrates anti-glioma activity by inhibiting the GABAB receptor-mediated MEK/ERK/CREB signaling axis.
- Baclofen also modulates the EMT-like pathway, contributing to its anti-tumor effects.
- These findings suggest baclofen as a potential therapeutic agent for glioma.
Related Concept Videos
Antiepileptic Drugs: GABAergic Pathway Potentiators
γ-aminobutyric acid or GABA, plays a pivotal role as an inhibitory neurotransmitter in the brain. GABA pathway potentiators, also known as GABAergic drugs, are a class of pharmaceutical agents designed to enhance the functioning of the GABAergic system. These medications primarily treat epilepsy, a neurological disorder characterized by recurrent seizures.
The key GABA pathway potentiators used in epilepsy management are as follows.
Benzodiazepines are a well-known class of drugs used for their...
The key GABA pathway potentiators used in epilepsy management are as follows.
Benzodiazepines are a well-known class of drugs used for their...
Mitogens and the Cell Cycle
Mitogens and their receptors play a crucial role in controlling the progression of the cell cycle. However, the loss of mitogenic control over cell division leads to tumor formation. Therefore, mitogens and mitogen receptors play an important role in cancer research. For instance, the epidermal growth factor (EGF) - a type of mitogen and its transmembrane receptor (EGFR), decides the fate of the cell's proliferation. When EGF binds to EGFR, a member of the ErbB family of tyrosine kinase...
mTOR Signaling and Cancer Progression
The mammalian target of rapamycin or mTOR protein was discovered in 1994 due to its direct interaction with rapamycin. The protein gets its name from a yeast homolog called TOR. The mTOR protein complex in mammalian cells plays a major role in balancing anabolic processes such as the synthesis of proteins, lipids, and nucleotides and catabolic processes, such as autophagy in response to environmental cues, such as availability of nutrients and growth factors.
The mTOR pathway or the...
The mTOR pathway or the...
MAPK Signaling Cascades
Mitogen-activated protein kinase, or MAPK pathway, activates three sequential kinases to regulate cellular responses such as proliferation, differentiation, survival, and apoptosis. The canonical MAPK pathway starts with a mitogen or growth factor binding to an RTK. The activated RTKs stimulate Ras, which recruits Raf or MAP3 Kinase (MAPKKK), the first kinase of the MAPK signaling cascade. Raf further phosphorylates and activates MEK or MAP2 Kinases (MAPKK), which in turn phosphorylates MAP...
Inhibition of Cdk Activity
The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...
Interactions Between Signaling Pathways
Signaling cascades usually lack linearity. Multiple pathways interact and regulate one another, allowing cells to integrate and respond to diverse environmental stimuli.
Convergence and divergence, and cross-talk between signaling pathways
Two distinct signaling pathways can converge on a single functional unit, which may either be a single protein or a complex of proteins. The response is either functionally distinct or synergistic between the two pathways but different from the response...
Convergence and divergence, and cross-talk between signaling pathways
Two distinct signaling pathways can converge on a single functional unit, which may either be a single protein or a complex of proteins. The response is either functionally distinct or synergistic between the two pathways but different from the response...