New insights for an old drug: difluoromethylornithine boosts the trypanocidal action of benznidazole on Trypanosoma cruzi in vitro and in vivo [PDF]
Frontiers in Cellular and Infection MicrobiologyChagas disease, caused by the protozoan parasite Trypanosoma cruzi, is currently a global health problem. Its multiple forms of transmission, which favor the spread of the infection, and the limited treatment options—still restricted to only two drugs ...
Santiago José Martínez +8 more
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Conformational analysis of difluoromethylornithine: factors influencing its gas-phase and bioactive conformations [PDF]
Beilstein Journal of Organic ChemistryDifluoromethylornithine (DFMO, eflornithine) is a fluorinated analogue of ornithine that serves both as an inhibitor of ornithine decarboxylase and as a therapeutic agent against African trypanosomiasis.
Matheus P. Freitas
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Difluoromethylornithine modulates mutant K-RAS signaling pathways in pancreatic cancer cells [PDF]
Amino AcidsOncogenic mutations in the K-RAS small GTPase occur in more than 90% of human PDACs and cause dysregulation of multiple metabolic pathways, including polyamine metabolism.
Hwudaurw Chen +4 more
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The Competitive Inhibition of Tissue Transglutaminase by α-Difluoromethylornithine [PDF]
FEBS Letters, 1984 The transglutaminase‐mediated insertion of putrescine into casein was inhibited competitively by α‐difluoromethylornithine (α‐DFMO), an enzyme‐activated irreversible inhibitor of ornithine decarboxylase. Preincubation of the amine acceptor (casein) or the enzyme itself with the inhibitor did not affect enzyme activity.
Jean-Guy Delcros +2 more
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The polyamine transporter ATP13A3 mediates difluoromethylornithine‐induced polyamine uptake in neuroblastoma [PDF]
Molecular OncologyHigh‐risk neuroblastomas, often associated with MYCN protooncogene amplification, are addicted to polyamines, small polycations vital for cellular functioning.
Mujahid Azfar +19 more
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Medical Sciences, 2018 The fluorinated ornithine analog α-difluoromethylornithine (DFMO, eflornithine, ornidyl) is an irreversible suicide inhibitor of ornithine decarboxylase (ODC), the first and rate-limiting enzyme of polyamine biosynthesis.
Sigrid C Roberts, Nicole Logiudice
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Preclinical Evaluation of the Efficacy of α-Difluoromethylornithine and Sulindac Against SARS-CoV-2 Infection [PDF]
VirusesDespite numerous research efforts and several effective vaccines and therapies developed against coronavirus disease 2019 (COVID-19), drug repurposing remains an attractive alternative approach for treatment of SARS-CoV-2 variants and other viral ...
Natalia A. Ignatenko +6 more
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In vitro and in vivo studies on exogenous polyamines and α-difluoromethylornithine to enhance bone formation and suppress osteoclast differentiation [PDF]
Amino AcidsExogenous polyamines, including putrescine (PUT), spermidine (SPD), and spermine (SPM), and the irreversible inhibitor of the rate-limiting enzyme ornithine decarboxylase (ODC) of polyamine biosynthesis, α-difluoromethylornithine (DFMO), are implicated ...
Chien-Ching Lee +6 more
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Frontiers in Chemistry, 2021 Targeting the polyamine biosynthetic pathway by inhibiting ornithine decarboxylase (ODC) is a powerful approach in the fight against diverse viruses, including SARS-CoV-2.
Joanna Bojarska +8 more
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Difluoromethylornithine (DFMO) Enhances the Cytotoxicity of PARP Inhibition in Ovarian Cancer Cells
Medical Sciences, 2022 Ovarian cancer accounts for 3% of the total cancers in women, yet it is the fifth leading cause of cancer deaths among women. The BRCA1/2 germline and somatic mutations confer a deficiency of the homologous recombination (HR) repair pathway.
Olivia El Naggar +3 more
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