A covalent creatine kinase inhibitor ablates glioblastoma migration and sensitizes tumors to oxidative stress.
Study Goal
The researchers aimed to explore the role of a creatine kinase inhibitor (CKi) on glioblastoma (GBM) biology, particularly its effects on migration, invasion, and ferroptosis protection.
Results Summary
CKi significantly reduced GBM cell migration and invasion, hindered radiation-induced migration, and altered glutathione metabolism and ferroptosis protection genes. Combining CKi with glutathione inhibition or ferroptosis activation reduced cell survival.
Population
Glioblastoma cell lines and patient-derived xenografts (in vitro study).
Effective Dosage
Not specified
Duration
Not specified
Interactions
None mentioned
| Intervention | Direction | Endpoint | Population | Dosage | Impact | Claim # |
|---|---|---|---|---|---|---|
creatine kinase inhibitor (CKi) | no change | GBM cell proliferation and viability | GBM cells in vitro | - | minimally impacted | #1 |
creatine kinase inhibitor (CKi) | decrease | migration | GBM cells in vitro | - | significantly affected | #2 |
creatine kinase inhibitor (CKi) | decrease | migration and invasion of GBM cells | established GBM cell lines and patient-derived xenografts | - | ablated | #3 |
creatine kinase inhibitor (CKi) | decrease | radiation-induced migration | GBM cells | - | hindered | #4 |
creatine kinase inhibitor (CKi) | decrease | invasion-related genes | - | - | revealed a decrease in | #5 |
creatine kinase inhibitor (CKi) | increase | glutathione metabolism and ferroptosis protection genes | - | - | increase in | #6 |
cell-permeable glutathione | neutral | effects of CKi | - | - | reversed | #7 |
creatine kinase inhibitor (CKi) | increase | glutathione biosynthesis | - | - | indicated heightened | #8 |
combinatorial CKi blockade and glutathione inhibition or ferroptosis activation | decrease | cell survival | - | - | abrogated | #9 |
creatine kinase inhibitor (CKi) | decrease | promigratory and anti-ferroptotic roles | GBM | - | perturbs | #10 |
Glioblastoma is a Grade 4 primary brain tumor defined by therapy resistance, diffuse infiltration, and near-uniform lethality. The underlying mechanisms are unknown, and no treatment has been curative. Using a recently developed creatine kinase inhibitor (CKi), we explored the role of this inhibitor on GBM biology in vitro. While CKi minimally impacted GBM cell proliferation and viability, it significantly affected migration. In established GBM cell lines and patient-derived xenografts, CKi ablated both the migration and invasion of GBM cells. CKi also hindered radiation-induced migration. RNA-seq revealed a decrease in invasion-related genes, with an unexpected increase in glutathione metabolism and ferroptosis protection genes post-CKi treatment. The effects of CKi could be reversed by the addition of cell-permeable glutathione. Carbon-13 metabolite tracing indicated heightened glutathione biosynthesis post-CKi treatment. Combinatorial CKi blockade and glutathione inhibition or ferroptosis activation abrogated cell survival. Our data demonstrated that CKi perturbs promigratory and anti-ferroptotic roles in GBM, identifying the creatine kinase axis as a druggable target for GBM treatment.