Search Results - "Beukers, M. W."

GPCRDB: An information system for G protein-coupled receptors by Horn, F., Weare, J., Beukers, M. W., Hörsch, S., Bairoch, A., Chen, W., Edvardsen, Ø., Campagne, F., Vriend, G.

“…The GPCRDB is a G protein-coupled receptor (GPCR) database system aimed at the collection and dissemination of GPCR related data. It holds sequences, mutant…”
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Pharmacological and biochemical analysis of FPL 67156, a novel, selective inhibitor of ecto‐ATPase by Crack, B.E., Pollard, C.E., Beukers, M.W., Roberts, S.M., Hunt, S.F., Ingall, A.H., McKechnie, K.C.W., IJzerman, A.P., Leff, P.

“…1 FPL 67156 (6‐N,N‐diethyl‐β,γ‐dibromomethylene‐d‐ATP), is a newly synthesized analogue of ATP. 2 In a rabbit isolated tracheal epithelium preparation,…”
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Pharmacological analysis of ecto‐ATPase inhibition: evidence for combined enzyme inhibition and receptor antagonism in P2X‐purinoceptor ligands by Crack, B.E., Beukers, M.W., McKechnie, K.C.W., IJzerman, A.P., Leff, P.

“…1 Previous studies have shown that suramin and FPL 66301 are competitive antagonists at the P2X‐purinoceptor in the rabbit ear artery. Those studies employed…”
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Heterologous expression of rat epitope‐tagged histamine H2 receptors in insect Sf9 cells by Beukers, M. W., Klaassen, C. H. W., De Grip, W. J., Verzijl, D., Timmerman, H., Leurs, R.

“…1 Rat histamine H2 receptors were epitope‐tagged with six histidine residues at the C‐terminus to allow immunological detection of the receptor. Recombinant…”
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The C terminal tail of the histamine H2 receptor contains positive and negative signals important for signal transduction and receptor down-regulation by Smit, M J, Timmerman, H, Blauw, J, Beukers, M W, Roovers, E, Jacobs, E H, Hoffmann, M, Leurs, R

“…To examine the role of the C terminal tail in H2 receptor regulation, three cDNAs, encoding truncated histamine H2 receptor mutants (H2T295, H2T307, and…”
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2,4,6-Trisubstituted Pyrimidines as a New Class of Selective Adenosine Receptor Antagonists by Chang, LCW, Spanjersberg, R F, von Frijtag Drabbe Kuenzel, JK, Mulder-Krieger, T, van den Hout, G, Beukers, M W, Brussee, J, Ijzerman, A P

“…Adenosine receptor antagonists usually possess a bi- or tricyclic heteroaromatic structure at their core with varying substitution patterns to achieve…”
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Heterologous expression of rat epitope‐tagged histamine H 2 receptors in insect Sf9 cells by Beukers, M. W., Klaassen, C. H. W., De Grip, W. J., Verzijl, D., Timmerman, H., Leurs, R.

“…Rat histamine H 2 receptors were epitope‐tagged with six histidine residues at the C‐terminus to allow immunological detection of the receptor. Recombinant…”
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Nucleoside transport inhibition and platelet aggregation in human blood: R75231 and its enantiomers, draflazine and R88016 by Beukers, M W, Kerkhof, C J, IJzerman, A P, Soudijn, W

“…In this study, we determined whether R75231, (+/-)-2-(aminocarbonyl)-N-(4-amino-2,6-dichlorophenyl)-4-[5,5-bis( 4-fluoro- phenyl)pentyl]-1-piperazineacetamide,…”
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Characterization of ecto-ATPase on human blood cells. A physiological role in platelet aggregation? by Beukers, M W, Pirovano, I M, van Weert, A, Kerkhof, C J, IJzerman, A P, Soudijn, W

“…Ecto-ATPase (EC 3.6.1.15) is a plasma membrane-bound enzyme which degrades extracellular triphosphate nucleotides. Although its physiological function is still…”
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Substituted 4-phenyl-2-(phenylcarboxamido)-1,3-thiazole derivatives as antagonists for the adenosine A1 receptor by VAN TILBURG, E. W, VAN DER KLEIN, P. A. M, DE GROOTE, M, BEUKERS, M. W, IJZERMAN, A. P

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Interaction of amiloride and its analogues with adenosine A1 receptors in calf brain by Garritsen, A, Ijzerman, A P, Beukers, M W, Cragoe, Jr, E J, Soudijn, W

“…Amiloride, a potassium sparing diuretic, is known to interact with a number of ion transport systems, receptors and enzymes. Here, we report on the interaction…”
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TinyGRAP database: a bioinformatics tool to mine G-protein-coupled receptor mutant data by Beukers, Margot W., Kristiansen, Kurt, IJzerman, Adriaan P., Edvardsen, Øyvind

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Chemical modification of adenosine A1 receptors. Implications for the interaction with R-PIA, DPCPX and amiloride by Garritsen, A, Ijzerman, A P, Beukers, M W, Soudijn, W

“…Amiloride, a potassium sparing diuretic, inhibits the specific binding of [3H]8-cyclopentyl-1,3-dipropylxanthine (DPCPX) and…”
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Substituted 4-phenyl-2-(phenylcarboxamido)-1,3-thiazole derivatives as antagonists for the adenosine A(1) receptor by van Tilburg, E W, van der Klein, P A, de Groote, M, Beukers, M W, IJzerman, A P

“…The synthesis and receptor binding of novel adenosine receptor antagonists is described. We found that non-xanthine 4-phenyl-2-(phenylcarboxamido)-1,3-thiazole…”
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tGRAP, the G-protein coupled receptors mutant database by Edvardsen, Oyvind, Reiersen, Anne Lise, Beukers, Margot W, Kristiansen, Kurt

“…The searchable mutant database tGRAP (previously called tinyGRAP) at the University of Tromsø contains data on mutated G-protein coupled receptors (GPCRs). All…”
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Altered affinity of insulin-like growth factor II (IGF-II) for receptors and IGF-binding proteins, resulting from limited modifications of the IGF-II molecule by Oh, Y, Beukers, M W, Pham, H M, Smanik, P A, Smith, M C, Rosenfeld, R G

“…The binding affinities of seven analogues of recombinant human insulin-like growth factor II (hIGF-II) were characterized for the IGF type-I and type-II…”
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The mode of interaction of amiloride and some of its analogues with the adenosine A1 receptor by Garritsen, A, Beukers, M W, IJzerman, A P, Cragoe, Jr, E J, Soudijn, W

“…Amiloride, a potassium sparing diuretic, inhibits adenosine A1 receptor-radioligand binding in calf and rat brain membranes in the low micromolar range. The…”
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[Leu27] insulin-like growth factor II is highly selective for the type-II IGF receptor in binding, cross-linking and thymidine incorporation experiments by Beukers, M W, Oh, Y, Zhang, H, Ling, N, Rosenfeld, R G

“…Insulin-like growth factor-II (IGF-II) is able to interact with three different receptors: the type-I and type-II IGF receptors, and the insulin receptor,…”
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Suramin analogs, divalent cations and ATP gamma S as inhibitors of ecto-ATPase by Beukers, M W, Kerkhof, C J, van Rhee, M A, Ardanuy, U, Gurgel, C, Widjaja, H, Nickel, P, IJzerman, A P, Soudijn, W

“…Ecto-nucleotidases are plasma membrane-bound enzymes that sequentially dephosphorylate extracellular nucleotides such as ATP. This breakdown of ATP and other…”
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Why are A(2B) receptors low-affinity adenosine receptors? Mutation of Asn273 to Tyr increases affinity of human A(2B) receptor for 2-(1-Hexynyl)adenosine by Beukers, M W, den Dulk, H, van Tilburg, E W, Brouwer, J, Ijzerman, A P

“…Adenosine A(2B) receptors are known as low-affinity receptors due to their modest-to-negligible affinity for adenosine and prototypic agonists. Despite…”
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