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. 2020 Oct 14;12(10):2973. doi: 10.3390/cancers12102973

Table 1.

Overview of experimental data listing the effects of TSPO modification on different glioma cell lines.

Treatment, Ligand Cell Line Effect on GBM Year Reference
TSPO KO Mouse GL261 cells
Human GBM1B cells
↑ glioma growth and angiogenesis in vivo,
↑ fragmented mitochondria, glucose uptake, lactic acid conversion, ↑ ROS, ↑ glycolysis,
↓ oxidative phosphorylation and ATP production
2020 [104]
PK11195 (25 µM) Human U118MG cells Changes in expression of immediate early genes and transcription factors, functional changes related to cell cycle, cell death, proliferation, migration, cell viability, inflammatory, immune response, and tumorigenesis 2017 [127]
PK11195 (25 µM), TSPO KD Human U118MG cells Changes in gene expression related to cell cycle, apoptosis, oxidative stress, immune response, DNA repair, adhesion 2014 [124]
Ammonium chloride + PK11196, Ro5 4864, FGN-1-27 (1 nM–100 µM) Human U118MG cells ↓ cell death at nanomolar concentration,
↑ mitochondrial dysfunction and cell death at micromolar concentration
2014 [142]
Quinazoline derivate compound 19 (10 nM–100 µM) Human U343 cells ↓ proliferation, dose-dependent,
↑ dissipation of ΔΨm
2014 [138]
irDE-MPIGA (1.25 × 10−3 nmol/L + 106 cells), PIGA (2.5 µM)
irDE-MPIGA + TSPO KD
Human U87MG cells ↓ cell viability without cell cycle arrest,
↑ ΔΨm dissipation,
No effect on ATPase activity
No reduction of cell viability
2014 [205]
PK11195 (25 µM), TSPO KD Human U118MG cells ↑ tumor growth, ↑ angiogenesis, ↑ migration,
↓ adhesion of ECM
2012 [103]
Sodium nitroprusside + PK11195 (25 µM), TSPO KD Human U118MG cells ↓ cell death and collapse of ΔΨm, restoration of metabolic activity 2012 [151]
TSPO KD
Glutamate + TSPO KD
Human U118MG cells,
Rat C6 cells
Changes in glutamate metabolism
↓ DNA fragmentation
2012 [135]
PPIX (1–30 µM) + light + TSPO KD
GSH + PPIX
Human U118MG cells ↑ cell death, ↑ PPIX accumulation in cell and mitochondria
↑ PPIX accumulation in mitochondria
2012 [26]
Oxazolacetamide compound 6d (30 times of Ki value) Human U87MG cells ↑ cell proliferation/viability,
↑ dissipation of ΔΨm,
2011 [105]
CoCl2 + PK11195 (25 µM), TSPO KD Human U118MG cells ↓ cell death, ↓ ΔΨm collapse, ↓ ROS generation, ↓ cardiolipin oxidation 2009 [21]
ErPC3 + PK 11195, Ro5 4864 (25 µM–100 µM) Human U87MG cells
Human A172 cells
Human U118MG cells
↓ ErPC3 induced apoptosis, ↓ cytochrome c release, processing of caspase 9 and 3 2008 [22]
TSPO overexpression
PK11195 (1–100 µM) + TSPO overexpression
Rat C6 cells ↑ proliferation, ↑ migration and transmigrative capabilities,
↑ anti-proliferative effect
2007 [100]
Ro5 4864 (10 nM) Rat C6 cells, human T89G cells ↓ cell death 2004 [19]
PK11195, Ro5 4864 (10 nM) Rat C6 cells, human T98G cells ↑ mitochondrial replication, shift of mitochondria from peripheral cytoplasm to the perinuclear region 1991 [206]

Abbreviations: ΔΨm, mitochondrial membrane potential; ECM, extracellular matrix; ErPC3, erucyl-phospho-homocholine; CoCl2, cobalt chloride; GSH, glutathione; KD, knockdown; KO, knockout; PPIX, protoporphyrin IX; ROS, reactive oxygen species.