1,721,083 research outputs found
Measurement of the near-infrared fluorescence of the air for the detection of ultra-high-energy cosmic rays
No full textEvaluation of novel 1,3-diketone curcumin analogues and glycogen synthase kinase-3 betainhibitors as potential anti-inflammatory agents in glial cultures
No full text9-(4-Dimethylaminophenyl)benzo[b]quinolizinium: A Near-Infrared Fluorophore for the Multicolor Analysis of Proteins and Nucleic Acids in Living Cells
No full textSynthesis, DNA-binding and antiproliferative properties of diarylquinolizinium derivatives
Full text linkA series of ten 2,7- and 2,8-diarylquinolizinium derivatives was synthesized and their DNA-binding and cytotoxic properties were investigated. Except for one nitro-substituted derivative all tested diarylquinolizinium ions bind to DNA with sufficient affinity (2 × 104 M-1-2 × 105 M-1). It was shown with photometric, fluorimetric and polarimetric titrations as well as with flow-LD analysis that the ligands bind mainly by intercalation to duplex DNA, however, depending on the ligand-DNA ratio, groove binding and backbone association were also observed with some derivatives. The biological activity was further investigated with tests of cytotoxicity and antiproliferative properties towards non-tumor cells and selected cancer cells, along with cell cycle analysis and an annexin-V assay. Notably, substrates that carry donor-functionalities in the 4-position of the phenyl substituents revealed a strong, and in some cases selective, antiproliferative activity as quantified by the growth inhibition, GI50, at very low micromolar and even submicromolar level both in leukemia and solid tumors
Surviving the hunger games: Metabolic reprogramming in medulloblastoma
Full text link: Medulloblastoma is a highly malignant pediatric brain tumor characterized by its aggressive nature and limited treatment options. Metabolic changes have recently emerged as key factors in the development, progression, and response to therapy in various types of cancer. Cancer cells exhibit remarkable adaptability by modulating glucose, lipids, amino acids, and nucleotide metabolism to survive in nutrient- and oxygen-deprived environments. Although medulloblastoma has been extensively studied from a genomic perspective, leading to the identification of four subgroups and their respective subcategories, the investigation of its metabolic phenotype has remained relatively understudied. This review focus on the available literature, aiming to summarize the current knowledge about the main metabolic pathways that are deregulated in medulloblastoma tumors, while emphasizing the controversial aspects and the progress that is yet to be made. Furthermore, we underscored the insights gained so far regarding the impact of metabolism on the development of drug resistance in medulloblastoma and the therapeutic strategies employed to target specific metabolic pathways
Control of the DNA-Binding and Antiproliferative Properties of Hydroxybenzo[b]quinolizinium Derivatives with pH and Light
No full textDiscovery of MG-2603 with in vitro potent antiproliferative activity by interfering with kinases and tubulin polymerisation
No full textDiscovery of a novel class of anti-proliferative pyrrolo[3,2-f]quinolin-9-ones characterized by interfering with both PI3K-Akt-mTOR signalling and microtubule assembling
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