Publications



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Publications:

  1. Sanders MP, Roumen L, van der Horst E, Lane JR, Vischer HF, van Offenbeek J, de Vries H, Verhoeven S, Chow KY, Verkaar F, Beukers MW, McGuire R, Leurs R, IJzerman AP, de Vlieg J, de Esch IJ, Zaman GJ, Klomp JP, Bender A, de Graaf C. A Prospective Cross-Screening Study on G-Protein-Coupled Receptors: Lessons Learned in Virtual Compound Library Design. J Med Chem. 2012 May 23. Link to Article

  2. Beukers MW. Project management of life-sciences research projects: project characteristics, challenges and training needs. Drug Disc Today 2011 16: 93-98. Link to Article

  3. Peeters MC, van Westen GJ, Guo D, Wisse LE, Müller CE, Beukers MW, IJzerman AP. GPCR structure and activation: an essential role for the first extracellular loop in activating the adenosine A2B receptor. Faseb J 2011 25: 632-643. Link to Article

  4. Lane JR, Klaasse E, Lin J, van Bruchem J, Beukers MW, IJzerman AP. Characterization of [3H]LUF5834: a novel non-ribose high-affinity agonist radioligand for the adenosine A1 receptor. Biochem Pharmacol 2010 80: 1180-1189. Link to Article

  5. van der Horst E, Peironcely JE, IJzerman AP, Beukers MW, Lane JR, van

Vlijmen HW, Emmerich MT, Okuno Y, Bender A. A novel chemogenomics analysis of G protein-coupled receptors (GPCRs) and their ligands: a potential strategy for receptor de-orphanization. BMC Bioinformatics. 2010 Jun 10;11(1):316. Link to Article

  1. Lane JR, Beukers MW, Mulder-Krieger T, IJzerman AP. The endocannabinoid 2-arachidonylglycerol is a negative allosteric modulator of the human A3 adenosine receptor. Biochem Pharmacol. 2010 Jan 1;79(1):48-56. Link to Article

  2. Mantri M, de Graaf O, van Veldhoven J, Göblyös A, von Frijtag Drabbe Künzel JK, Mulder-Krieger T, Link R, de Vries H, Beukers MW, Brussee J, IJzerman AP. 2-Amino-6-furan-2-yl-4-substituted nicotinonitriles as A2A adenosine receptor antagonists. J Med Chem. 2008 Aug 14;51(15):4449-55. Link to Article

  3. Klaasse EC, IJzerman AP, de Grip WJ, Beukers MW. Internalization and desensitization of adenosine receptors. Purinergic Signal. 2008 Mar;4(1):21-37. Link to Article

  4. van Veldhoven JP, Chang LC, von Frijtag Drabbe Künzel JK, Mulder-Krieger T, Struensee-Link R, Beukers MW, Brussee J, IJzerman AP. A new generation of adenosine receptor antagonists: from di- to trisubstituted aminopyrimidines. Bioorg Med Chem. 16:2741-2752 (2008). Link to Article

  5. Li Q, Ye K, Blad CC, den Dulk H, Brouwer J, IJzerman AP, Beukers MW. ZM241385, DPCPX, MRS1706 are inverse agonists with different relative intrinsic efficacies on constitutively active mutants of the human adenosine A2B receptor. J Pharmacol Exp Ther. 320:637-645 (2007). Link to Article

  6. Beukers MW, Meurs I, IJzerman AP. Structure-affinity relationships of adenosine A2B receptor ligands. Med Res Rev. 26(5): 667-698 (2006). Link to Article

  7. Ye K, Lameijer EW, Beukers MW, IJzerman AP. A two-entropies analysis to identify functional positions in the transmembrane region of class A G protein-coupled receptors. Proteins. 63(4): 1018-1030 (2006). Link to Article

  8. Klaasse EC, van den Hout G, Roerink SF, de Grip WJ, IJzerman AP, Beukers MW. Allosteric modulators affect the internalization of human adenosine A1 receptors. Eur J Pharmacol. 522(1-3): 1-8 (2005). Link to Article

  9. Beukers MW, IJzerman AP. Techniques: how to boost GPCR mutagenesis studies using yeast. Trends Pharmacol Sci. 26(10): 533-539 (2005). Link to Article

  10. Chang LC, von Frijtag Drabbe Künzel JK, Mulder-Krieger T, Spanjersberg RF, Roerink SF, van den Hout G, Beukers MW, Brussee J, IJzerman AP. A series of ligands displaying a remarkable agonistic-antagonistic profile at the adenosine A1 receptor. J Med Chem 48: 2045-2053 (2005). Link to Article

  11. Chang LC, Spanjersberg RF, von Frijtag Drabbe Künzel JK, Mulder-Krieger T, van den Hout G, Beukers MW, Brussee J, IJzerman AP. 2,4,6-trisubstituted pyrimidines as a new class of selective adenosine A1 receptor antagonists. J Med Chem 47: 6529-6540 (2004). Link to Article

  12. Beukers MW, van Oppenraaij J, van der Hoorn PP, Blad CC, den Dulk H, Brouwer J, IJzerman AP. Random mutagenesis of the human adenosine A2B receptor followed by growth selection in yeast. Identification of constitutively active and gain of function mutations. Mol Pharmacol 65: 702-710 (2004). Link to Article

  13. Beukers MW, Chang LC, von Frijtag Drabbe Künzel JK, Mulder-Krieger T, Spanjersberg RF, Brussee J, IJzerman AP. New, non-adenosine, high-potency agonists for the human adenosine A2B receptor with an improved selectivity profile compared to the reference agonist N-ethylcarboxamidoadenosine. J Med Chem 47: 3707-3709 (2004). Link to Article

  14. E.V. Samsonova Back T, Beukers MW, IJzerman AP, Kok JN. Combining and comparing cluster methods in a receptor database. in: Advances in Intelligent Data Analysis V, LNCS (2003) 2810: 341-351 Springer-Verlag. Link to Article

  15. Beukers MW, Wanner MJ, Von Frijtag Drabbe Künzel JK, Klaasse EC, IJzerman AP, Koomen GJ. N6-Cyclopentyl-2-(3-phenylaminocarbonyltriazene-1-yl)adenosine (TCPA), a very selective agonist with high affinity for the human adenosine A1 receptor. J Med Chem 46: 1492-1503 (2003). Link to Article

  16. Lorenzen A, Beukers MW, van der Graaf PH, Lang H, van Muijlwijk-Koezen J, de Groote M, Menge W, Schwabe U, IJzerman AP. Modulation of agonist responses at the A1 adenosine receptor by an irreversible antagonist, receptor-G protein uncoupling and by the G protein activation state. Biochem Pharmacol. 64: 1251-1265 (2002). Link to Article

  17. Edvardsen Ø, Reiersen A-L, Beukers MW, Kristiansen K. tGRAP, the G-protein coupled receptors mutant database. Nucleic Acids Research 30: 361-363 (2002). Link to Article

  18. van Tilburg EW, van der Klein PAM, de Groote M, Beukers MW, IJzerman, AP. Substituted 4-phenyl-2-(phenylcarboxamido)-1,3-thiazole derivatives as antagonists for the adenosine A1 receptor. Bioorg Med Chem Lett 11: 2017-2019 (2001). Link to Article

  19. van Muijlwijk-Koezen JE, Timmerman H, van der Sluis RP, van de Stolpe AC, Menge WM, Beukers MW, van der Graaf PH, de Groote M, IJzerman AP. Synthesis and use of FSCPX, an irreversible adenosine A1 antagonist, as a 'receptor knock-down' tool. Bioorg Med Chem Lett 11: 815-818 (2001). Link to Article

  20. Beukers MW, van der Klein PAM, IJzerman AP. Nieuwe zoekstrategieen. In: Volksgezondheid Toekomst Verkenning 2002, Achtergrond studie. Geneesmiddelen nu en in de toekomst (Timmerman H en van den Berg Jeths A, eds) Bohn, Stafleu, Van Loghum (Houten) 2001, pp. 439 - 454. Link to Article

  21. Beukers MW, Den Dulk H, Van Tilburg EW, Brouwer J, IJzerman AP. Why are A2B receptors low affinity adenosine receptors? Mutation of Asn273 to Tyr increases affinity of human A2B receptor for 2-(1-hexynyl)adenosine. Mol Pharmacol 58: 1349-1356 (2000). Link to Article

  22. De Zwart M, Vollinga RC, Beukers MW, Sleegers DF, JKVD, De Groote M, IJzerman AP. Potent antagonists for the human adenosine A2B receptor. Derivatives of the triazolotriazine adenosine receptor antagonist ZM241385 with high affinity. Drug Development Research 48: 95-103 (1999). Link to Article

  23. Beukers MW, Kristiansen, K, IJzerman, AP, Edvardsen, Ø. TinyGRAP database: a bioinformatics tool to mine receptor mutant data. Trends in Pharmacol Sci 20: 475-477 (1999). Link to Article

  24. Dalpiaz A, Townsend-Nicholson A, Beukers MW, Schofield PR, IJzerman AP. Thermodynamics of full agonist, partial agonist and antagonist binding to wild-type and mutant adenosine A1 receptors. Biochem Pharmacol 56: 1437-1445 (1998). Link to Article

  25. Horn F, Weare J, Beukers MW, Hörsch S, Bairoch A, Chen W, Edvardsen Ø, Campagne F, Vriend G. GPCRDB: an information system for G protein-coupled receptors. Nucleic Acids Research 26: 275-279 (1998). Link to Article

  26. Beukers MW, Klaassen CHW, De Grip WJ, Verzijl D, Timmerman H, Leurs R. Heterologous expression of epitope-tagged rat histamine H2 receptors in insect Sf9 cells. British Journal of Pharmacology 122: 867-874 (1997). Link to Article

  27. Smit MJ, Timmerman H, Blauw J, Beukers MW, Roovers E, Jacobs EH, Hoffmann M, Leurs R. The C terminal tail of the histamine H2 receptor contains positive and negative signals important for signal transduction and receptor down-regulation. J Neurochem. 67(5): 1791-1800 (1996). Link to Article

  28. Beukers MW, Kerkhof CJM, Van Rhee MA, Ardanuy U, Gurgel C, Widjaja H, Nickel P, IJzerman AP, Soudijn W. Suramin analogs, divalent cations and ATPγS as inhibitors of ecto-ATPase. Naunyn-Schmiedeberg's Archiv Pharmacol 351: 523-528 (1995). Link to Article

  29. Crack BE, Pollard CE, Beukers MW, Roberts SM, Hunt F, Ingall AH, McKechnie KCW, IJzerman AP, Leff P. Pharmacological and biochemical analysis of FPL67156, a novel, selective inhibitor of ecto-ATPase. Br J Pharmacol 114: 475-481 (1995). Link to Article

  30. Crack BE, Beukers MW, McKechnie KCW, IJzerman AP, Leff P. Pharmacological analysis of ecto-ATPase inhibition: evidence for combined enzyme inhibition and receptor antagonism in P2X-purinoceptor ligands. Br J Pharmacol 113: 1432-1438 (1994). Link to Article

  31. Van Rhee MA, Van der Heijden MPA, Beukers MW, IJzerman AP, Soudijn W, Nickel P. Novel competitive antagonists for P2 purinoceptors. Eur J Pharmacol Mol Pharmacol sect 268: 1-7 (1994). Link to Article

  32. Beukers MW, Kerkhof CJM, IJzerman AP, Soudijn W. Nucleoside transport inhibition and platelet aggregation in human blood: R75231 and its enantiomers, draflazine and R88016. Eur J Pharmacol Molec Pharmacol Sect 266: 57-62 (1994). Link to Article

  33. Beukers MW, Pirovano IM, Van Weert A, Kerkhof CJM, IJzerman AP, Soudijn W. Characterization of ecto-ATPase on human blood cells. A physiological role in platelet aggregation? Biochem Pharmacol 46: 1959-1966 (1993). Link to Article

  34. Garritsen A, Beukers MW, IJzerman AP, Cragoe Jr EJ, Soudijn W. The mode of interacti­on of amiloride and some of its analogues with the adenosine A1 receptor. Neurochem Int 20: 207-213 (1992). Link to Article

  35. Garritsen A, Beukers MW, IJzerman AP, Soudijn W. Recognition of adenosine receptors by amiloride and its analogs. Nucleosides & Nucleotides 10(5): 1107-1111 (1991). Link to Article

  36. Oh Y, Beukers MW, Pham HM, Smanik PA, Smith MC, Rosenfeld RG. 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. Biochemical J 278: 249-254 (1991). Link to Article

  37. Neely EK, Beukers MW, Oh Y, Cohen P, Rosenfeld RG. Insulin-like growth factor receptors. Acta Paediatrica Scandinavia S372: 116-123 (1991). Link to Article

  38. Beukers MW, Oh Y, Zhang H, Ling N, Rosenfeld RG. [Leu27] Insulin-like growth factor II is highly selective for the type-II IGF receptor in binding, cross-linking and thymidine incorporation experiments. Endocrinology 128(2): 1201-1203 (1991). Link to Article

  39. Beukers MW, Boddeke HWGM. Pharmacology of long-term potentiation. A model for learning reviewed. Pharmaceutisch Weekblad Scientific Edition 13: 7-13 (1991). Link to Article

  40. Garritsen A, IJzerman AP, Beukers MW, Cragoe EJ Jr, Soudijn W. Interaction of amiloride and its analogues with adenosine A1 receptors in calf brain. Biochem Pharmacol 40: 827-834 (1990). Link to Article

  41. Garritsen A, IJzerman AP, Beukers MW, Soudijn W. Chemical modification of adenosine A1 receptors. Implication for the interaction with R-PIA, DPCPX and amiloride. Biochem Pharmacol 40: 835-842 (1990). Link to Article

Other:

Bottlenecks identification in Drug Discovery … And solutions please!



Beukers MW

http://www.eufeps.org/document/pdfs/eufepsnews1_2009.pdf



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