Summary: The antidiabetic drug phenformin displays potent anticancer activity in different tumors, but its mechanism of action remains elusive. Using Shh medulloblastoma as model, we show here that at clinically relevant concentrations, phenformin ...
Laura Di Magno +20 more
doaj +3 more sources
Brain-Targeted Delivery of Phenformin Using Phospholipid and Non-Phospholipid Vesicles for SHH Medulloblastoma [PDF]
Medulloblastoma (MB) is the most frequent brain malignancy in children, frequently driven by deregulated Sonic Hedgehog (SHH) signaling. We previously identified the antidiabetic drug phenformin (Phen) as a potent Gli1 inhibitor that suppresses SHH ...
Laura Di Magno +11 more
doaj +2 more sources
Metabolic reprogramming in diffuse intrinsic pontine gliomas (DIPG): dual inhibition of mitochondrial oxidative phosphorylation and lactate metabolism to enhance anti-tumor and radiosensitizing effects in DIPG cells [PDF]
Background Diffuse midline gliomas (DMGs), including diffuse intrinsic pontine gliomas (DIPGs), are universally fatal pediatric brain tumors with no effective treatments.
Han Shen +9 more
doaj +2 more sources
Repurposing Metabolic Inhibitors in the Treatment of Colon Adenocarcinoma Patient-Derived Models [PDF]
The effect of agonists on AMP-activated protein kinase (AMPK), mainly metformin and phenformin, has been appreciated in the treatment of multiple types of tumors.
Bora Lee +5 more
doaj +2 more sources
Phenformin alone or combined with gefitinib inhibits bladder cancer via AMPK and EGFR pathways
Background In previous studies, we have shown that the combination of metformin and gefitinib inhibits the growth of bladder cancer cells. Here we examined whether the metformin analogue phenformin, either used alone or in combination with gefitinib ...
Yanjun Huang +8 more
doaj +3 more sources
Novel combination therapy with phenformin enhances the effects of lenvatinib in hepatocellular carcinoma via AMPK-mediated PDGFRβ degradation [PDF]
Background Hepatocellular carcinoma (HCC) is an invasive malignant tumour for which few effective treatment options are currently available. Lenvatinib is a small-molecule inhibitor of multiple receptor tyrosine kinases used for the treatment of patients
Duo Li +9 more
doaj +2 more sources
A Comparative Study of the Lipophilicity of Metformin and Phenformin
The results presented in this paper confirm the beneficial role of an easy-to-use and low-cost thin-layer chromatography (TLC) technique for describing the retention behavior and the experimental lipophilicity parameter of two biguanide derivatives ...
Małgorzata Dołowy +2 more
doaj +3 more sources
Phenformin activates ER stress to promote autophagic cell death via NIBAN1 and DDIT4 in oral squamous cell carcinoma independent of AMPK [PDF]
The efficient clinical treatment of oral squamous cell carcinoma (OSCC) is still a challenge that demands the development of effective new drugs. Phenformin has been shown to produce more potent anti-tumor activities than metformin on different tumors ...
Dexuan Zhuang +10 more
doaj +2 more sources
Mechanisms of NMDA Receptor Inhibition by Biguanide Compounds [PDF]
N-methyl-D-aspartate (NMDA) receptors are inhibited by many medicinal drugs. The recent successful repurposing of NMDA receptor antagonists ketamine and dextromethorphan for the treatment of major depressive disorder further enhanced the interest in this
Arseniy S. Zhigulin +2 more
doaj +2 more sources
Metabolic modeling elucidates phenformin and atpenin A5 as broad-spectrum antiviral drugs against RNA viruses [PDF]
The SARS-CoV-2 pandemic has reemphasized the urgent need for broad-spectrum antiviral therapies. We developed a computational workflow using scRNA-Seq data to assess cellular metabolism during viral infection. With this workflow we predicted the capacity
Alina Renz +19 more
doaj +2 more sources

