Metabolism 2014 – Alterations of metabolic pathways as therapeutic targets
Published in Biochemical Pharmacology
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Modulatory roles of glycolytic enzymes in cell death
Published in Biochemical Pharmacology
Cancer cells depend on an altered energy metabolism characterized by increased rates of both glycolysis and glutaminolysis. Accordingly, corresponding key metabolic enzymes are overexpressed or hyperactivated. As a result, this newly acquired metabolic profile determines most other cancer hallmarks including resistance to cell death. Recent finding...
Valproic acid regulates erythro-megakaryocytic differentiation through the modulation of transcription factors and micro...
Published in Biochemical Pharmacology
Valproic acid (VPA) exhibits important pharmacological properties but has been reported to trigger side effects, notably on the hematological system. We previously reported that VPA affects hematopoietic homeostasis by inhibiting erythroid differentiation and promoting myeloid and megakaryocyte differentiation. Here, we analyzed the effect of VPA o...
Plant-derived epigenetic modulators for cancer treatment and prevention
Published in Biotechnology Advances
Carcinogenesis is a complex and multistep process that involves the accumulation of successive transformational events driven by genetic mutations and epigenetic alterations that affect major cellular processes and pathways such as proliferation, differentiation, invasion and survival. Massive deregulation of all components of the epigenetic machin...
From Nature to bedside: Pro-survival and cell death mechanisms as therapeutic targets in cancer treatment
Published in Biotechnology Advances
•act as activators of specific apoptotic commitments•modulate the stress balance and equilibrate between death and survival•target prosurvival and pro-death pathways•inhibit NF-kB-regulated survival genes
Energy restriction mimetic agents to target cancer cells: Comparison between 2-deoxyglucose and thiazolidinediones.
The use of energy restriction mimetic agents (ERMAs) to selectively target cancer cells addicted to glycolysis could be a promising therapeutic approach. Thiazolidinediones (TZDs) are synthetic agonists of the nuclear receptor peroxisome proliferator-activated receptor (PPAR)γ that were developed to treat type II diabetes. These compounds also disp...
Valproic acid regulates erythro-megakaryocytic differentiation through the modulation of transcription factors and micro...
Published in Biochemical pharmacology
Valproic acid (VPA) exhibits important pharmacological properties but has been reported to trigger side effects, notably on the hematological system. We previously reported that VPA affects hematopoietic homeostasis by inhibiting erythroid differentiation and promoting myeloid and megakaryocyte differentiation. Here, we analyzed the effect of VPA o...
Synthesis and bioactivity of novel amino-pyrazolopyridines
Published in European Journal of Medicinal Chemistry
Here we describe the synthesis and biological activity of novel amino-pyrazolopyridines with anti-NF-κB and pro-apoptotic potential. α-Methylene ketones were used as a starting point for synthesis of amino-pyrazolopyridine 3. The alkylidene malononitriles 1 were obtained by the Knoevenagel reaction of ketones with malononitriles. Vilsmeier-Haack re...
Methylenedioxy flavonoids: Assessment of cytotoxic and anti-cancer potential in human leukemia cells
Published in European Journal of Medicinal Chemistry
A new series of chalcones, flavanones and flavones with methylenedioxy group at the 3',4' position in chalcone, 7,8 position in flavanones and flavones with mono-, di- and trimethoxy groups in the benzaldehyde ring have been assessed for their effect on proliferation, cytotoxic potential and apoptosis in human leukemia cells. Among the tested compo...
Epigenetic modulators from “The Big Blue”: A treasure to fight against cancer
Published in Cancer Letters
Cancer remains a major public health problem in our society. The development of potent novel anti-cancer drugs selective for tumor cells is therefore still required. Deregulation of the epigenetic machinery including DNA methylation, histone modifications and non-coding RNAs is a hallmark of cancer, which provides potential new therapeutic targets....
