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First generation vanadium-based PTEN inhibitors: Comparative study in vitro and in vivo and identification of a novel mechanism of action.
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Department of Pharmacology, Faculty of Medicine, School of Health Sciences, University of Ioannina, 45110 Ioannina, Greece; Institute of Biosciences, University Research Center Ioannina, University of Ioannina, Ioannina, Greece. Electronic address:
PTEN, a tumor suppressor phosphatase, regulates cellular functions by antagonizing the growth promoting PI3K/Akt/mTOR pathway through the dephosphorylation of the second messenger PIP. Many preclinical cellular and animal studies have used PTEN inhibitors to highlight specific disease contexts where acute activation of PI3K/Akt/mTOR pathway might offer therapeutic advantages. In the present study we have re-evaluated first-generation PTEN inhibitors, including established bisperoxo-vanadium complexes (bpVs).
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Department of Chemistry, Faculty of Science (Boys), Al-Azhar University 11884 Nasr City Cairo Egypt
Herein, novel thiazolo[4,5-]quinoxalin-2-ones 2-6 and thiazolo[4,5-]quinoxalin-2(3)-imines 7-9 were synthesized and characterized using elemental analysis, IR spectroscopy, and H/C NMR to confirm their structures. The efficacy of the newly designed thiazolo-quinoxalines 2, 3, 4, 5, 7, 8, and 9 against the cotton leafworm (2nd and 4th instar larvae) was evaluated, and results revealed insecticidal activity with variable and good mortality percentages. A SAR study was also discussed.
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Cadmium (Cd) is a widely available metal that has been found to have a role in causing nonalcoholic fatty liver disease (NAFLD). However, the detailed toxicological targets and mechanisms by which Cd causes NAFLD are unknown. Therefore, the present work aims to reveal the main targets of action, cellular processes, and molecular pathways by which cadmium causes NAFLD.
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Sickle cell disease (SCD) is a hereditary hemolytic anemia associated with the alteration of the membrane composition of the sickle erythrocytes, the loss of glycolysis, dysregulation of the pyruvate phosphatase pathway, and changes in nucleotide metabolism of the sickle red blood cell (RBC). This review provides a comprehensive overview of the impact of the presence of Hb S, which leads to the disruption of the normal RBC metabolism. The intricate interplay between the redox and energetic balance in erythrocytic cells, where the glycolysis, pentose phosphate pathway, and methemoglobin reductase pathways are all altered in sickle RBC, is a key focus.
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Aggressive variant prostate cancer (AVPC) is characterized by a molecular signature involving combined defects in , , and/or (AVPC-TSGs), identifiable through immunohistochemistry or genomic analysis. The reported prevalence of AVPC-TSG alterations varies widely, reflecting differences in assay sensitivity, treatment pressure, and disease stage evolution. Although robust clinical evidence is still emerging, the study of AVPC-TSG alterations in prostate cancer (PCa) is promising.
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