Journal: bioRxiv

Article Title: A novel pan class-I glucose transporter inhibitor DRB18 exhibits synergistic effects in vitro and in vivo with paclitaxel against human non-small cell lung cancer

doi: 10.1101/2024.12.15.628558

Figure Lengend Snippet: 2 μM of DRB18 combined with or without other drugs to treat A549 cells for 48 hours. The inhibition of cell proliferation was compared to single compound treatment to identify anti-proliferation synergism. 4A. DRB18 combined with 10 µM V9302 showed more inhibition against A549 cells. 4B . DRB18 combined with 100 nM or 300 nM of CB839 showed more cytotoxicity against A549. 4C . DRB18 combined with 5 µM or 10 µM of sunitinib (Sutent) showed more inhibition against A549 cells. 4D . DRB18 combined with 10 µM V9302 showed more inhibition against Panc1 cells. 4E . DRB18 combined with 100 nM or 300 nM of CB839 showed more inhibition against Panc1 cells. 4F . DRB18 combined with 5 µM or 10 µM of sunitinib showed more inhibition against Panc1 cells. 4G . 5 µM of DRB18 combined with 0.75 µM of brigatinib showed more cytotoxicity against A549 cells. 4H . 5 µM of DRB18 combined with 15 µM of trametinib showed more inhibition against A549 cells.

Article Snippet: V9302 (HY-112683) and CB839 (HY-12248) were purchased from MedChemExpress.

Techniques: Inhibition

Journal: Cell Metabolism

Article Title: PML-Regulated Mitochondrial Metabolism Enhances Chemosensitivity in Human Ovarian Cancers

doi: 10.1016/j.cmet.2018.09.002

Figure Lengend Snippet:

Article Snippet: Carboplatin (ACCORD, 10 mg / ml) and Paclitaxel (KABI, 6 mg / ml), or Ironomycin (in-house drug), or CB-839 (at 10 μM, Selleckchem #S7655)), or Metformin (at 0.01 M, Sigma Aldrich #317240) were added the next day at the appropriate concentration.

Techniques: Virus, Derivative Assay, Recombinant, Protease Inhibitor, Western Blot, Staining, Membrane, Electron Microscopy, SYBR Green Assay, Bicinchoninic Acid Protein Assay, DNA Profiling, Reverse Transcription, Software, Imaging, Cell Culture

Journal: Cancer letters

Article Title: Glutaminase inhibition with telaglenastat (CB-839) improves treatment response in combination with ionizing radiation in head and neck squamous cell carcinoma models

doi: 10.1016/j.canlet.2020.12.038

Figure Lengend Snippet: (A) Glutamine dependence: Proliferation of CAL-27, and HN5 cell lines is glutamine dependent. Cell lines were grown with or without 0.5 mM glutamine. Error bars represent SD. (B) Efficacy of telaglenastat in inhibiting spheroid growth: Telaglenastat significantly reduced the size of CAL-27 and HN5 spheroids after 48 h. (C) Representative images of CAL-27, HN5 and FaDu spheroids at 8 days. HNC cells were grown in 3D culture and treated with vehicle or 1 μM CB-839 for 8 days. Scale bars represent 100 μM. Error bars represent SE (***p ≤ 0.001, ****p ≤ 0.0001).

Article Snippet: Inhibition of glutaminase by telaglenastat (Calithera Biosciences, Inc.) has been associated with reduced growth of lymphomas, breast, renal and pancreatic cancers in pre-clinical studies [ 12 ].

Techniques:

Journal: Cancer letters

Article Title: Glutaminase inhibition with telaglenastat (CB-839) improves treatment response in combination with ionizing radiation in head and neck squamous cell carcinoma models

doi: 10.1016/j.canlet.2020.12.038

Figure Lengend Snippet: Telaglenastat decreases OCR/ECAR ratio in HN5 and CAL-27 cells. OCR/ECAR ratios were calculated from Seahorse MitoStress test analysis in CAL-27, HN5 and FaDu cells. Vehicle or 1000 nM telaglenastat were injected during the MitoStress test into media containing 5 mM glucose and 0.5 mM glutamine. Error bars represent SE (****p ≤ 0.0001).

Article Snippet: Inhibition of glutaminase by telaglenastat (Calithera Biosciences, Inc.) has been associated with reduced growth of lymphomas, breast, renal and pancreatic cancers in pre-clinical studies [ 12 ].

Techniques: Injection

Journal: Cancer letters

Article Title: Glutaminase inhibition with telaglenastat (CB-839) improves treatment response in combination with ionizing radiation in head and neck squamous cell carcinoma models

doi: 10.1016/j.canlet.2020.12.038

Figure Lengend Snippet: Combination of telaglenastat and IR significantly reduces survival of HNSCC cell lines as compared to independent treatment with either telaglenastat or IR. (A) CAL-27 (Kruskal-Wallis: p =5.1e-07), (B) HN5 (Kruskal-Wallis: p =1.8e-06) or (C) FaDu (Kruskal-Wallis: p =1.4e-04) cells were treated with either 0 or 4 Gy IR and grown in the presence of vehicle or 10 nM telaglenastat. Error bars represent SD (*p ≤0.05,**p ≤0.01, ***p ≤0.001, ****p ≤0.0001).

Article Snippet: Inhibition of glutaminase by telaglenastat (Calithera Biosciences, Inc.) has been associated with reduced growth of lymphomas, breast, renal and pancreatic cancers in pre-clinical studies [ 12 ].

Techniques:

Journal: Cancer letters

Article Title: Glutaminase inhibition with telaglenastat (CB-839) improves treatment response in combination with ionizing radiation in head and neck squamous cell carcinoma models

doi: 10.1016/j.canlet.2020.12.038

Figure Lengend Snippet: (A) Immunofluorescent images of CAL-27 treated with vehicle, telaglenastat and radiation monotherapy, combination of telaglenastat and radiation, and combination treatment with NAC; 8-oxoguanine (green), γ-H2AX (red), DAPI (blue): nuclei. (B) Comparison of 8-oxoguanine and (C) γ-H2AX levels. Scale bars equal 50 μM. Error bars represent 95% confidence intervals (*p ≤0.05, **p ≤0.01, ***p ≤0.001, ****p ≤0.0001). Quantification results are from a representative biological replicate.

Article Snippet: Inhibition of glutaminase by telaglenastat (Calithera Biosciences, Inc.) has been associated with reduced growth of lymphomas, breast, renal and pancreatic cancers in pre-clinical studies [ 12 ].

Techniques: Comparison

Journal: Cancer letters

Article Title: Glutaminase inhibition with telaglenastat (CB-839) improves treatment response in combination with ionizing radiation in head and neck squamous cell carcinoma models

doi: 10.1016/j.canlet.2020.12.038

Figure Lengend Snippet: IR induces glutaminase activity in HNSCC and thereby increases production of glutamate for entry into the Krebs cycle. Glutaminase inhibitor, telaglenastat, reduces formation of glutamate, and thus impairs the Krebs cycle’s ability to create biomolecules necessary for rapid cellular proliferation.

Article Snippet: Inhibition of glutaminase by telaglenastat (Calithera Biosciences, Inc.) has been associated with reduced growth of lymphomas, breast, renal and pancreatic cancers in pre-clinical studies [ 12 ].

Techniques: Activity Assay