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Browsing by Subject "enzyme inhibition"

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    • Article  

      The 1.76 Å resolution crystal structure of glycogen phosphorylase b complexed with glucose, and CP320626, a potential antidiabetic drug 

      Oikonomakos, Nikos G.; Zographos, Spyros E.; Skamnaki, Vicky T.; Archontis, Georgios Z. (2002)
      CP320626, a potential antidiabetic drug, inhibits glycogen phosphorylase in synergism with glucose. To elucidate the structural basis of synergistic inhibition, we determined the structure of muscle glycogen phosphorylase ...

    • Article  

      Analysis of binding parameters of HIV-1 integrase inhibitors: Correlates of drug inhibition and resistance 

      Loizidou, Eriketi Z.; Zeinalipour-Yazdi, Constantinos D.; Christofides, Tasos C.; Kostrikis, Leontios G. (2009)
      This study undertook an exploratory data analysis of the binding parameters of HIV-1 integrase inhibitors. The study group involved inhibitors in preclinical development from the diketo acid, pyrroloquinoline and naphthyridine ...

    • Article  

      Analysis of binding parameters of HIV-1 integrase inhibitors: Correlates of drug inhibition and resistance 

      Loizidou, Eriketi Z.; Zeinalipour-Yazdi, Constantinos D.; Christofides, Tasos C.; Kostrikis, Leontios G. (2009)
      This study undertook an exploratory data analysis of the binding parameters of HIV-1 integrase inhibitors. The study group involved inhibitors in preclinical development from the diketo acid, pyrroloquinoline and naphthyridine ...

    • Article  

      Analysis of binding parameters of HIV-1 integrase inhibitors: Correlates of drug inhibition and resistance 

      Loizidou, Eriketi Z.; Zeinalipour-Yazdi, Constantinos D.; Christofides, Tasos C.; Kostrikis, Leondios G. (2009)
      This study undertook an exploratory data analysis of the binding parameters of HIV-1 integrase inhibitors. The study group involved inhibitors in preclinical development from the diketo acid, pyrroloquinoline and naphthyridine ...

    • Article  

      Application of topoisomerase assays in the evaluation of natural products as antitumor agents 

      Constantinou, Andreas I.; Salti, G. (1999)
      Initially, DNA topoisomerase (topo) inhibitors found clinical applications as antibiotics and cancer chemotherapeutic agents. Recently, we demonstrated that plant flavonoids that inhibit mammalian topo I or topo II might ...

    • Article  

      D-alpha-tocopheryl polyethylene glycol succinate (TPGS) induces cell cycle arrest and apoptosis selectively in Survivin-overexpressing breast cancer cells 

      Neophytou, Christiana M.; Constantinou, Constantina; Papageorgis, P.; Constantinou, Andreas I. (2014)
      d-alpha-tocopheryl polyethylene glycol succinate (TPGS) is a vitamin E derivative that has been intensively applied as a vehicle for drug delivery systems to enhance drug solubility and increase the oral bioavailability ...

    • Article  

      The Dietary Anticancer Agent Ellagic Acid is a Potent Inhibitor of DNA Topoisomerases in Vitro 

      Constantinou, Andreas I.; Mehta, R.; Runyan, C.; Moon, R.; Stoner, G. D.; Rao, K. (1995)
      Ellagic acid and 12 related agents have been tested for their ability to inhibit the activities of human DNA topoisomerase (topo) I and IL Using specific in vitro assays, we found ellagic acid and flavellagic acid to be ...

    • Article  

      Discovery of anti-cancer activity for benzo[1,2,4]triazin-7-ones: Very strong correlation to pleurotin and thioredoxin reductase inhibition 

      Sweeney, M.; Coyle, R.; Kavanagh, P.; Berezin, Andrey A.; Lo Re, D.; Zissimou, Georgia A.; Koutentis, Panayiotis Andreas; Carty, Michael P.; Aldabbagh, Fawaz (2016)
      The thioredoxin (Trx)–thioredoxin reductase (TrxR) system plays a key role in maintaining the cellular redox balance with Trx being over-expressed in a number of cancers. Inhibition of TrxR is an important strategy for ...

    • Article  

      Genistein as an Inducer of Tumor Cell Differentiation: Possible Mechanisms of Action 

      Constantinou, Andreas I.; Huberman, E. (1995)
      Decreased activity of either topoisomerases or tyrosine kinases has been implicated in the differentiation of a number of cell types. It is therefore conceivable that genistein, because of its reported ability to inhibit ...

    • Article  

      Glucose-based spiro-isoxazolines: A new family of potent glycogen phosphorylase inhibitors 

      Benltifa, Mahmoud; Hayes, Joseph M.; Vidal, Sébastien; Gueyrard, David; Goekjian, Peter G.; Praly, Jean Pierre; Kizilis, Gregory; Tiraidis, Costas; Alexacou, Kyra Melinda; Chrysina, Evangelia D.; Zographos, Spyros E.; Leonidas, Demetres D.; Archontis, Georgios Z.; Oikonomakos, Nikos G. (2009)
      A series of glucopyranosylidene-spiro-isoxazolines was prepared through regio- and stereoselective [3+2]-cycloaddition between the methylene acetylated exo-glucal and aromatic nitrile oxides. The deprotected cycloadducts ...

    • Article  

      Glycogen phosphorylase inhibitors: A free energy perturbation analysis of glucopyranose spirohydantoin analogues 

      Archontis, Georgios Z.; Watson, K. A.; Xie, Q.; Andreou, Georgia; Chrysina, Evangelia D.; Zographos, Spyros E.; Oikonomakos, Nikos G.; Karplus, M. (2005)
      GP catalyzes the phosphorylation of glycogen to Glc-1-P. Because of its fundamental role in the metabolism of glycogen, GP has been the target for a systematic structure-assisted design of inhibitory compounds, which could ...

    • Article  

      Identification of a potent activator of Akt phosphorylation from a novel series of phenolic, picolinic, pyridino, and hydroxamic zinc(II) complexes 

      Georgiades, Savvas N.; Mak, L. H.; Angurell, I.; Rosivatz, E.; Firouz Mohd Mustapa, M.; Polychroni, Christoulla; Woscholski, R.; Vilar, R. (2011)
      The discovery of small-molecule modulators of signaling pathways is currently a particularly active area of research. We aimed at developing unprecedented metal-based activators of Akt signaling which can potentially find ...

    • Article  

      Imaging morphogenesis, in Xenopus with Quantum Dot nanocrystals 

      Stylianou, Panayiota; Skourides, Paris A. (2009)
      Mesoderm migration is a well studied morphogenetic movement that takes place during Xenopus gastrulation. The study of mesoderm migration and other morphogenetic movements has been primarily based on in vitro assays due ...

    • Article  

      Inhibition of mitogen-activated protein kinase (MAPK) and cyclin-dependent kinase 2 (Cdk2) by platinum(II) phenanthroline complexes 

      Child, E. S.; Georgiades, Savvas N.; Rose, K. N.; Stafford, V. S.; Patel, C. B. K.; Steinke, J. H. G.; Mann, D. J.; Vilar, R. (2011)
      Inhibition of protein kinases in the fight against disease remains a constant challenge for medicinal chemists, who have screened multitudes of predominantly planar organic scaffolds, natural and synthetic, to identify ...

    • Article  

      Inhibition of topoisomerase IIα activity in CHO K1 cells by 2- [(aminopropyl)amino]ethanethiol (WR-1065) 

      Grdina, D. J.; Constantinou, Andreas I.; Shigematsu, N.; Murley, J. S. (1994)
      The aminothiol 2-[(aminopropyl)amino]ethanethiol (WR-1065) is the active thiol of the clinically studied radioprotective agent S-2-(3- aminopropylamino)ethylphosphorothioic acid (WR-2721). WR-1065 is an effective radiation ...

    • Article  

      Kinetic and crystallographic studies of glucopyranose spirohydantoin and glucopyranosylamine analogs inhibitors of glycogen phosphorylase 

      Watson, K. A.; Chrysina, Evangelia D.; Tsitsanou, K. E.; Zographos, Spyros E.; Archontis, Georgios Z.; Fleet, G. W. J.; Oikonomakos, Nikos G. (2005)
      Glycogen phosphorylase (GP) is currently exploited as a target for inhibition of hepatic glycogenolysis under high glucose conditions. Spirohydantoin of glucopyranose and N-acetyl-β-D-glucopyranosylamine have been identified ...

    • Article  

      Modeling the effects of toxins in metabolic networks 

      Tamaddoni-Nezhad, A.; Chaleil, R.; Kakas, Antonis C.; Sternberg, M.; Nicholson, J.; Muggleton, S. (2007)

    • Article  

      Mutant polycystin-2 induces proliferation in primary rat tubular epithelial cells in a STAT-1/p21-independent fashion accompanied instead by alterations in expression of p57KIP2 and Cdk2 

      Felekkis, Kyriacos N.; Koupepidou, P.; Kastanos, E.; Witzgall, R.; Bai, C. -X; Li, L.; Tsiokas, L.; Gretz, N.; Constantinou-Deltas, Constantinos D. (2008)
      Background. Autosomal Dominant Polycystic Kidney Disease (ADPKD) is characterized by the formation of multiple fluid-filled cysts that destroy the kidney architecture resulting in end-stage renal failure. Mutations in genes ...

    • Article  

      A novel QSAR model for evaluating and predicting the inhibition activity of dipeptidyl aspartyl fluoromethylketones 

      Afantitis, Antreas; Melagraki, G.; Sarimveis, H.; Koutentis, Panayiotis Andreas; Markopoulos, J.; Igglessi-Markopoulou, O. (2006)
      A linear quantitative structure activity relationship model is obtained using Multiple Linear Regression (MLR) analysis as applied to a series of 49 dipeptidyl aspartyl fluoromethylketone derivatives with inhibitory activity ...

    • Article  

      A novel use for the comet assay: Detection of topoisomerase II inhibitors 

      Salti, G. I.; Das Gupta, T. K.; Constantinou, Andreas I. (2000)
      Background: The simple and quick comet assay can quantitatively detect DNA cleavage in cells. This study aimed to determine whether the comet assay could be used to detect topoisomerase (topo) II inhibitors. Materials and ...

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