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- Volume 19, Issue 14, 2013
Current Pharmaceutical Design - Volume 19, Issue 14, 2013
Volume 19, Issue 14, 2013
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D-Amino Acid Oxidase Inhibitors as a Novel Class of Drugs for Schizophrenia Therapy
Authors: Silvia Sacchi, Elena Rosini, Loredano Pollegioni and Gianluca MollaOver the years, accumulating evidence has indicated that D-serine represents the endogenous ligand for the glycinemodulatory binding site on the NR1 subunit of N-methyl-D-aspartate receptors in various brain areas. Cellular concentrations of D-serine are regulated by synthesis due to the enzyme serine racemase (isomerization reaction) and by degradation due to the same enzyme (elimination reaction) as well as by the F Read More
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1,4-Naphthoquinones and Other NADPH-Dependent Glutathione Reductase- Catalyzed Redox Cyclers as Antimalarial Agents
Authors: Didier Belorgey, Don Antoine Lanfranchi and Elisabeth Davioud-CharvetThe homodimeric flavoenzyme glutathione reductase catalyzes NADPH-dependent glutathione disulfide reduction. This reaction is important for keeping the redox homeostasis in human cells and in the human pathogen Plasmodium falciparum. Different types of NADPH-dependent disulfide reductase inhibitors were designed in various chemical series to evaluate the impact of each inhibition mode on the propagation of the Read More
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Inhibitor Design for Monoamine Oxidases
More LessFlavin-containing monoamine oxidases (MAO A and MAO B) located on the outer membrane of mitochondria oxidise amines and generate hydrogen peroxide. Inhibitors alleviate depression by increasing neurotransmitter levels in the brain. Elevation of neurotransmitters, although an established outcome, is a delicate balance because complete lack of MAO A is associated with aggression and combination of monoami Read More
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Is Renalase a Novel Player in Catecholaminergic Signaling? The Mystery of the Catalytic Activity of an Intriguing New Flavoenzyme
Authors: Sara Baroni, Mario Milani, Vittorio Pandini, Giulio Pavesi, David Horner and Alessandro AlivertiRenalase is a flavoprotein recently discovered in humans, preferentially expressed in the proximal tubules of the kidney and secreted in blood and urine. It is highly conserved in vertebrates, with homologs identified in eukaryotic and prokaryotic organisms. Several genetic, epidemiological, clinical and experimental studies show that renalase plays a role in the modulation of the functions of the cardiovascular system, being Read More
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Riboflavin Analogs as Antiinfectives: Occurrence, Mode of Action, Metabolism and Resistance
Antimetabolites are molecules, which are structurally similar to molecules needed to carry out primary metabolic reactions. The inhibitory activity of an antimetabolite depends on its successful competition with the natural substrate, ligand, modulator or cofactor of a given biomolecule. Antimetabolites are indispensable as molecular tools in order to understand biological processes. Beyond that, antimetabolites have a la Read More
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Targeting UDP-Galactopyranose Mutases from Eukaryotic Human Pathogens
Authors: Karina Kizjakina, John J. Tanner and Pablo SobradoUDP-Galactopyranose mutase (UGM) is a unique flavin-dependent enzyme that catalyzes the conversion of UDPgalactopyranose (UDP-Galp) to UDP-galactofuranose (UDP-Galf). The product of this reaction is the precursor to Galf, a major component of the cell wall and of cell surface glycoproteins and glycolipids in many eukaryotic and prokaryotic human pathogens. The function of UGM is important in the virulence of Read More
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Methylenetetrahydrofolate Reductase: Biochemical Characterization and Medical Significance
More LessMethylenetetrahydrofolate reductase (MTHFR) catalyzes the reduction of 5,10-methylenetetrahydofolate (CH2-H4folate) to 5- methyltetrahydrofolate (CH3-H4folate). The enzyme employs a noncovalently-bound flavin adenine dinucleotide (FAD), which accepts reducing equivalents from NAD(P)H and transfers them to CH2-H4folate. The reaction provides the sole source of CH3-H4folate, which is utilized Read More
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Redox Proteins as Targets for Drugs Development Against Pathogens
More LessAntimicrobial drug resistance in pathogens is an increasing human health problem. The rapid loss of effectiveness in antibiotics treatments and the accumulation of multi-resistant microbial strains are increasing worldwide threats. Moreover, several infectious diseases have been neglected for years and new antimicrobial treatments are lacking. In other cases, complexity of infectious organisms has exceeded the efforts to find Read More
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Chemical Nature and Reaction Mechanisms of the Molybdenum Cofactor of Xanthine Oxidoreductase
Authors: Ken Okamoto, Teruo Kusano and Takeshi NishinoXanthine oxidoreductase (XOR), a complex flavoprotein, catalyzes the metabolic reactions leading from hypoxanthine to xanthine and from xanthine to urate, and both reactions take place at the molybdenum cofactor. The enzyme is a target of drugs for therapy of gout or hyperuricemia. We review the chemical nature and reaction mechanisms of the molybdenum cofactor of XOR, focusing on molybdenum Read More
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Target Sites for the Design of Anti-trypanosomatid Drugs Based on the Structure of Dihydroorotate Dehydrogenase
Authors: Matheus Pinto Pinheiro, Flavio da Silva Emery and M. Cristina NonatoTrypanosomatids consist of a large group of flagellated parasitic protozoa, including parasites from the genera Leishmania and Trypanosoma, responsible for causing infections in millions of humans worldwide and for which currently no appropriate therapy is available. The significance of pyrimidines in cellular metabolism makes their de novo and salvage pathways ideal druggable targets for pharmacological intervention Read More
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The Oxido-reductase Activity of the Apoptosis Inducing Factor: A Promising Pharmacological Tool?
Authors: Patricia Ferreira, Raquel Villanueva, Lauriane Cabon, Santos A. Susin and Milagros MedinaThe apoptosis inducing factor (AIF) was first discovered as a caspase-independent apoptosis effector that promoted cell death upon release from the mitochondria (triggered by pro-apoptotic stimuli) and relocalization into the nucleus, where it promotes chromatin condensation and DNA fragmentation. AIF is a mammalian mitochondrial FAD-dependent flavoenzyme, ubiquitous in vertebrate cells, and with orthologs in all e Read More
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The Prokaryotic FAD Synthetase Family: A Potential Drug Target
Authors: Ana Serrano, Patricia Ferreira, Marta Martinez-Julvez and Milagros MedinaDisruption of cellular production of the flavin cofactors, flavin adenine mononucleotide (FMN) and flavin adenine dinucleotide (FAD) will prevent the assembly of a large number of flavoproteins and flavoenzymes involved in key metabolic processes in all types of organisms. The enzymes responsible for FMN and FAD production in prokaryotes and eukaryotes exhibit various structural characteristics to catalyze the same ch Read More
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Biosynthesis of Flavin Cofactors in Man: Implications in Health and Disease
The primary role of the water-soluble vitamin B2, i.e. riboflavin, in cell biology is connected with its conversion into FMN and FAD, the cofactors of a large number of dehydrogenases, reductases and oxidases involved in energetic metabolism, redox homeostasis and protein folding as well as in diverse regulatory events. Deficiency of riboflavin in men and experimental animal models has been linked to several diseases, including Read More
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Volumes & issues
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Volume 31 (2025)
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Volume 30 (2024)
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Volume 29 (2023)
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Volume 28 (2022)
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Volume 27 (2021)
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Volume 26 (2020)
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Volume 25 (2019)
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Volume 24 (2018)
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Volume 23 (2017)
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Volume 22 (2016)
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Volume 21 (2015)
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Volume 20 (2014)
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Volume 19 (2013)
- Issue 42
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Volume 18 (2012)
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Volume 17 (2011)
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Volume 16 (2010)
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Volume 15 (2009)
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Volume 14 (2008)
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Volume 13 (2007)
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Volume 12 (2006)
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Volume 11 (2005)
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Volume 10 (2004)
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Volume 9 (2003)
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Volume 8 (2002)
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Volume 7 (2001)
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Volume 6 (2000)
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