Searched for: subject:"enzyme%5C+inhibition"
(1 - 20 of 41)

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Carmany, D. (author), Walz, A.J. (author), Hsu, F.L. (author), Benton, B. (author), Burnett, D. (author), Gibbons, J. (author), Noort, D. (author), Glaros, T. (author), Sekowski, J.W. (author)
Organophosphorus (OP) nerve agents continue to be a threat at home and abroad during the war against terrorism. Human exposure to nerve agents such as VX results in a cascade of toxic effects relative to the exposure level including ocular miosis, excessive secretions, convulsions, seizures, and death. The primary mechanism behind these overt...
article 2017
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Raaphorst, R.M. (author), Savolainen, H. (author), Cantore, M. (author), van de Steeg, E. (author), van Waarde, A. (author), Colabufo, N.A. (author), Elsinga, P.H. (author), Lammertsma, A.A. (author), Windhorst, A.D. (author), Luurtsema, G. (author)
Positron emission tomography (PET) imaging of P-glycoprotein (P-gp) in the blood-brain barrier can be important in neurological diseases where P-gp is affected, such as Alzheimer’s disease. Radiotracers used in the imaging studies are present at very small, nanomolar, concentration, whereas in vitro assays where these tracers are characterized,...
article 2017
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Busnadiego, O. (author), Gorbenko del Blanco, D. (author), González-Santamaría, J. (author), Habashi, J.P. (author), Calderon, J.F. (author), Sandoval, P. (author), Bedja, D. (author), Guinea-Viniegra, J. (author), Lopez-Cabrera, M. (author), Rosell-Garcia, T. (author), Snabel, J.M. (author), Hanemaaijer, R. (author), Forteza, A. (author), Dietz, H.C. (author), Egea, G. (author), Rodriguez-Pascual, F. (author)
Patients with Marfan syndrome (MFS) are at high risk of life-threatening aortic dissections. The condition is caused by mutations in the gene encoding fibrillin-1, an essential component in the formation of elastic fibers. While experimental findings in animal models of the disease have shown the involvement of transforming growth factor-β (TGF...
article 2015
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van Diepen, J.A. (author), Vroegrijk, I.O.C.M. (author), Berbée, J.F.P. (author), Shoelson, S.E. (author), Romijn, J.A. (author), Havekes, L.M. (author), Rensen, P.C.N. (author), Voshol, P.J. (author)
Systemic inflammation is strongly involved in the pathophysiology of the metabolic syndrome, a cluster of metabolic risk factors that includes hypertriglyceridemia. Aspirin treatment lowers inflammation via inhibition of NF-?B activity but also reduces hypertriglyceridemia in humans. The aim of this study was to investigate the mechanism by...
article 2011
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Rubbens, M.P. (author), Mol, A. (author), van Marion, M.H. (author), Hanemaaijer, R. (author), Bank, R.A. (author), Baaijens, F.P.T. (author), Bouten, C.V.C. (author), TNO Kwaliteit van Leven (author)
Similar to native cardiovascular tissues, the mechanical properties of engineered cardiovascular constructs depend on the composition and quality of the extracellular matrix, which is a net result of matrix remodeling processes within the tissue. To improve tissue remodeling, and hence tissue mechanical properties, various mechanical...
article 2009
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Knippenberg, M. (author), Helder, M.N. (author), Doulabi, B.Z. (author), Bank, R.A. (author), Wuisman, P.I.J.M. (author), Klein-Nulend, J. (author), TNO Kwaliteit van Leven (author)
Adipose tissue-derived mesenchymal stem cells (AT-MSCs) in combination with bone morphogenetic protein-2 (BMP-2) or transforming growth factor-β1 (TGF-β1) are under evaluation for bone tissue engineering. Posttranslational modification of type I collagen is essential for functional bone tissue with adequate physical and mechanical properties. We...
article 2009
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Lindeman, J.H.N. (author), Abdul-Hussien, H. (author), van Bockel, J.H. (author), Wolterbeek, R. (author), Kleemann, R. (author), TNO Kwaliteit van Leven (author)
Background-Doxycycline has been shown to effectively inhibit aneurysm formation in animal models of abdominal aortic aneurysm. Although this effect is ascribed to matrix metalloproteinase-9 inhibition, such an effect is unclear in human studies. We reevaluated the effect of doxycycline on aortic wall protease content in a inical trial and found...
article 2009
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Drissen, R.E.T. (author), Maas, R.H.W. (author), van der Maarel, M.J.E.C. (author), Kabel, M.A. (author), Schols, H.A. (author), Tramper, J. (author), Beeftink, H.H. (author), TNO Kwaliteit van Leven (author)
The kinetics of cellulose hydrolysis by commercially available Cellubrix were described mathematically, with Avicel and wheat straw as substrates. It was demonstrated that hydrolysis could be described by three reactions: direct glucose formation and indirect glucose formation via cellobiose. Hydrolysis did not involve any soluble oligomers...
article 2007
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Jeurissen, S.M.F. (author), Claassen, F.W. (author), Havlik, J. (author), Bouwmans, E.E. (author), Cnubben, N.H.P. (author), Sudhölter, E.J.R. (author), Rietjens, I.M.C.M. (author), van Beek, T.A. (author), TNO Kwaliteit van Leven (author)
An on-line HPLC screening method for detection of inhibitors of human cytochrome P450 1A2 in extracts was developed. HPLC separation of extracts is connected to a continuous methoxyresorufin-O-demethylation (MROD) assay in which recombinant human P450 1A2 converts methoxyresorufin to its fluorescent metabolite resorufin. The system was tested...
article 2007
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van Zanden, J.J. (author), van der Woude, H. (author), Vaessen, J. (author), Usta, M. (author), Wortelboer, H.M. (author), Cnubben, N.H.P. (author), Rietjens, I.M.C.M. (author), TNO Kwaliteit van Leven (author)
The present study characterises the effect of phase II metabolism, especially methylation and glucuronidation, of the model flavonoid quercetin on its capacity to inhibit human MRP1 and MRP2 activity in Sf9 inside-out vesicles. The results obtained reveal that 3′-O-methylation does not affect the MRP inhibitory potential of quercetin. However, 4...
article 2007
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Houben, E. (author), Uchida, Y. (author), Nieuwenhuizen, W.F. (author), de Paepe, K. (author), Vanhaecke, T. (author), Holleran, W.M. (author), Rogiers, V. (author), TNO Kwaliteit van Leven (author)
It has recently become evident that at least five ceramidase (CDase) isoforms are present in human epidermis, and that specifically acidic CDase (aCDase) and alkaline CDase (alkCDase) activities increase during keratinocyte differentiation, and thus might play a pivotal role(s) in permeability barrier function. Prior to investigating their...
article 2007
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Noort, D. (author), Fidder, A. (author), van der Schans, M.J. (author), Hulst, A.G. (author), TNO Defensie en Veiligheid (author)
We present a generic mass spectrometric method to verify exposure to organophosphates, based on the chemical conversion of the phosphylated peptides obtained after pepsin digestion of human butyrylcholinesterase (HuBuChE) to a common precursor peptide. After exposure of plasma to various organophosphates (nerve agents, pesticides), HuBuChE was...
article 2006
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Westerterp, M. (author), de Haan, W. (author), Berbée, J.F.P. (author), Havekes, L.M. (author), Rensen, P.C.N. (author), TNO Kwaliteit van Leven (author)
Previous studies have shown that overexpression of human apolipoprotein C-I (apoC-I) results in moderate hypercholesterolemia and severe hypertriglyceridemia in mice in the presence and absence of apoE. We assessed whether physiological endogenous apoC-I levels are sufficient to modulate plasma lipid levels independently of effects of apoE on...
article 2006
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Parnham, M.J. (author), Bogaards, J.J.P. (author), Schrander, F. (author), Schut, M.W. (author), Orešković, K. (author), Mildner, B. (author), TNO Kwaliteit van Leven (author)
PLD-118 is a novel, oral antifungal drug, under development for the treatment of Candida infections. Possible metabolism of PLD-118 by rat, dog and human S9 liver homogenates and inhibition of human cytochrome P450 (CYP) enzymes were investigated. PLD-118 (10 and 100 μm) incubated for 0-60 min with S9 fractions and NADPH was determined by HPLC,...
article 2005
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Goudriaan, J.R. (author), den oer, M.A.M. (author), Rensen, P.C.N. (author), Febbraio, M. (author), Kuipers, F. (author), Romijn, J.A. (author), Havekes, L.M. (author), Voshol, P.J. (author), TNO Kwaliteit van Leven (author)
CD36 is involved in high-affinity peripheral FFA uptake. CD36-deficient (cd36-/-) mice exhibit increased plasma FFA and triglyceride (TG) levels. The aim of the present study was to elucidate the cause of the increased plasma TG levels in cd36-/- mice. cd36-/- mice showed no differences in hepatic VLDL-TG production or intestinal [3H]TG uptake...
article 2005
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Kaper, T. (author), Talik, B. (author), Ettema, T.J. (author), Bos, H. (author), van der Maarel, M.J.E.C. (author), Dijkhuizen, L. (author), TNO Kwaliteit van Leven (author)
Amylomaltases are 4-α-glucanotransferases (EC 2.4.1.25) of glycoside hydrolase family 77 that transfer α-1,4-linked glucans to another acceptor, which can be the 4-OH group of an α-1,4-linked glucan or glucose. The amylomaltase-encoding gene (PAE1209) from the hyperthermophilic archaeon Pyrobaculum aerophilum IM2 was cloned and expressed in...
article 2005
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Tchetverikov, I. (author), Lohmander, L.S. (author), Verzijl, N. (author), Huizinga, T.W.J. (author), TeKoppele, J.M. (author), Hanemaaijer, R. (author), de Groot, J. (author), TNO Preventie en Gezondheid (author)
Objective: To determine protein and activity levels of matrix metalloproteinases 1 and 3 (MMP-1 and MMP-3) in synovial fluid of patients with knee joint injury, primary osteoarthritis, and acute pyrophosphate arthritis (pseudogout). Methods: Measurements were done on knee synovial fluid obtained in a cross sectional study of cases of injury (n...
article 2005
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Lamfers, M.L.M. (author), Gianni, D. (author), Tung, C.H. (author), Idema, S. (author), Schagen, F.H.E. (author), Carette, J.E. (author), Quax, P.H.A. (author), van Beusechem, V.W. (author), van der Top, W.P. (author), Dirven, C.M.F. (author), Chiocca, E.A. (author), Gerritsen, W.R. (author), TNO Kwaliteit van Leven (author)
Oncolytic adenoviruses exhibiting tumor-selective replication are promising anticancer agents. Insertion and expression of a transgene encoding tissue inhibitor of metalloproteinase-3 (TIMP-3), which has been reported to inhibit angiogenesis and tumor cell infiltration and induce apoptosis, may improve the antitumor activity of these agents. To...
article 2005
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TNO Kwaliteit van Leven (author), Grefhorst, A. (author), Hoekstra, J. (author), Derks, T.G.J. (author), Ouwens, D.M. (author), Baller, J.F.W. (author), Havinga, R. (author), Havekes, L.M. (author), Romijn, J.A. (author), Kuipers, F. (author)
Accumulation of triglycerides (TG) in the liver is generally associated with hepatic insulin resistance. We questioned whether acute hepatic steatosis induced by pharmacological blockade of β-oxidation affects hepatic insulin sensitivity, i.e., insulin-mediated suppression of VLDL production and insulin-induced activation of phosphatidylinositol...
article 2005
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van Zanden, J.J. (author), Geraets, L. (author), Wortelboer, H.M. (author), van Bladeren, P.J. (author), Rietjens, I.M.C.M. (author), Cnubben, N.H.P. (author), TNO Voeding (author)
The objective of this study was to investigate the structural requirements necessary for inhibition of glutathione S-transferase P1-1 (GSTP1-1) and GS-X pump (MRP1 and MRP2) activity by structurally related flavonoids, in GSTP1-1 transfected MCF7 cells (pMTG5). The results reveal that GSTP1-1 activity in MCF7 pMTG5 cells can be inhibited by some...
article 2004
Searched for: subject:"enzyme%5C+inhibition"
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