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Margot Beukers

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Marijn P A Sanders; Eelke van der Horst; Jody van Offenbeek; Stefan Verhoeven; Folkert Verkaar; Henry Vischer; Guido J R Zaman; Andreas Bender; Margot W Beukers; Ken Y Chow; Iwan J P De Esch; Jacob de Vlieg; Henk de Vries; Adriaan P IJzerman; Jan P G Klomp; J Robert Lane; Rob Leurs; Ross McGuire; Luc Roumen; Chris de Graaf
A prospective cross-screening study on G-protein-coupled receptors: lessons learned in virtual compound library design.
Margot W Beukers
Project management of life-science research projects: project characteristics, challenges and training needs.
Miriam C Peeters; Gerard van Westen; Dong Guo; Lisanne E Wisse; Christa E Müller; Margot W Beukers; Adriaan P IJzerman
GPCR structure and activation: an essential role for the first extracellular loop in activating the adenosine A2B receptor.

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2012: Marijn P A Sanders; Eelke van der Horst; Jody van Offenbeek; Stefan Verhoeven; Folkert Verkaar; Henry Vischer; Guido J R Zaman; Andreas Bender; Margot W Beukers; Ken Y Chow; Iwan J P De Esch; Jacob de Vlieg; Henk de Vries; Adriaan P IJzerman; Jan P G Klomp; J Robert Lane; Rob Leurs; Ross McGuire; Luc Roumen; Chris de Graaf
A prospective cross-screening study on G-protein-coupled receptors: lessons learned in virtual compound library design.
Journal of medicinal chemistry 2012;55(11):5311-25.
2011: Margot W Beukers
Project management of life-science research projects: project characteristics, challenges and training needs.
Drug discovery today 2011;16(3-4):93-8.
2011: Miriam C Peeters; Gerard van Westen; Dong Guo; Lisanne E Wisse; Christa E Müller; Margot W Beukers; Adriaan P IJzerman
GPCR structure and activation: an essential role for the first extracellular loop in activating the adenosine A2B receptor.
FASEB journal : official publication of the Federation of American Societies for Experimental Biology 2011;25(2):632-43.
2010: J Robert Lane; Elisabeth Klaasse; Judy Lin; John van Bruchem; Margot W Beukers; Adriaan P IJzerman
Characterization of [3H]LUF5834: A novel non-ribose high-affinity agonist radioligand for the adenosine A1 receptor.
Biochemical pharmacology 2010;80(8):1180-9.
2010: Eelke van der Horst; Julio Peironcely; Adriaan P IJzerman; Margot W Beukers; Jonathan R Lane; Herman van Vlijmen; Michael T M Emmerich; Yasushi Okuno; Andreas Bender
A novel chemogenomics analysis of G protein-coupled receptors (GPCRs) and their ligands: a potential strategy for receptor de-orphanization.
BMC bioinformatics 2010;11():316.
2010: J Robert Lane; Margot W Beukers; Thea Mulder-Krieger; Adriaan P IJzerman
The endocannabinoid 2-arachidonylglycerol is a negative allosteric modulator of the human A3 adenosine receptor.
Biochemical pharmacology 2010;79(1):48-56.
2008: Monica Mantri; Olivier de Graaf; Jacobus van Veldhoven; Anikó Göblyös; Jacobien K Von Frijtag Drabbe Künzel; Thea Mulder-Krieger; Regina Link; Henk de Vries; Margot W Beukers; Johannes Brussee; Adriaan P IJzerman
2-Amino-6-furan-2-yl-4-substituted nicotinonitriles as A2A adenosine receptor antagonists.
Journal of medicinal chemistry 2008;51(15):4449-55.
2008: Jacobus P D van Veldhoven; Lisa C W Chang; Jacobien K Von Frijtag Drabbe Künzel; Thea Mulder-Krieger; Regina Struensee-Link; Margot W Beukers; Johannes Brussee; Adriaan P IJzerman
A new generation of adenosine receptor antagonists: from di- to trisubstituted aminopyrimidines.
Bioorganic & medicinal chemistry 2008;16(6):2741-52.
2008: Elisabeth C Klaasse; Adriaan P IJzerman; Willem J De Grip; Margot W Beukers
Internalization and desensitization of adenosine receptors.
Purinergic signalling 2008;4(1):21-37.
2007: Qilan Li; Kai Ye; Clara C Blad; Hans den Dulk; Jaap Brouwer; Adriaan P IJzerman; Margot W Beukers
ZM241385, DPCPX, MRS1706 are inverse agonists with different relative intrinsic efficacies on constitutively active mutants of the human adenosine A2B receptor.
The Journal of pharmacology and experimental therapeutics 2007;320(2):637-45.
2006: Margot W Beukers; Illiana Meurs; Adriaan P IJzerman
Structure-affinity relationships of adenosine A2B receptor ligands.
Medicinal research reviews 2006;26(5):667-98.
2006: Kai Ye; Eric-Wubbo M Lameijer; Margot W Beukers; Adriaan P IJzerman
A two-entropies analysis to identify functional positions in the transmembrane region of class A G protein-coupled receptors.
Proteins 2006;63(4):1018-30.
2005: Elisabeth C Klaasse; Gijs van den Hout; Sophie F Roerink; Willem J De Grip; Adriaan P IJzerman; Margot W Beukers
Allosteric modulators affect the internalization of human adenosine A1 receptors.
European journal of pharmacology 2005;522(1-3):1-8.
2005: Margot W Beukers; Adriaan P IJzerman
Techniques: how to boost GPCR mutagenesis studies using yeast.
Trends in pharmacological sciences 2005;26(10):533-9.
2005: Lisa C W Chang; Jacobien K Von Frijtag Drabbe Künzel; Thea Mulder-Krieger; Ronald F Spanjersberg; Sophie F Roerink; Gijs van den Hout; Margot W Beukers; Johannes Brussee; Adriaan P IJzerman
A series of ligands displaying a remarkable agonistic-antagonistic profile at the adenosine A1 receptor.
Journal of medicinal chemistry 2005;48(6):2045-53.
2004: Lisa C W Chang; Ronald F Spanjersberg; Jacobien K Von Frijtag Drabbe Künzel; Thea Mulder-Krieger; Gijs van den Hout; Margot W Beukers; Johannes Brussee; Adriaan P IJzerman
2,4,6-trisubstituted pyrimidines as a new class of selective adenosine A1 receptor antagonists.
Journal of medicinal chemistry 2004;47(26):6529-40.
2004: Margot W Beukers; Lisa C W Chang; Jacobien K Von Frijtag Drabbe Künzel; Thea Mulder-Krieger; Ronald F Spanjersberg; Johannes Brussee; Adriaan P IJzerman
New, non-adenosine, high-potency agonists for the human adenosine A2B receptor with an improved selectivity profile compared to the reference agonist N-ethylcarboxamidoadenosine.
Journal of medicinal chemistry 2004;47(15):3707-9.
2004: Margot W Beukers; Joris van Oppenraaij; Patrick P W van der Hoorn; Clara C Blad; Hans den Dulk; Jaap Brouwer; Adriaan P IJzerman
Random mutagenesis of the human adenosine A2B receptor followed by growth selection in yeast. Identification of constitutively active and gain of function mutations.
Molecular pharmacology 2004;65(3):702-10.
2003: Margot W Beukers; Martin J Wanner; Jacobien K Von Frijtag Drabbe Künzel; Elisabeth C Klaasse; Adriaan P IJzerman; Gerrit-Jan Koomen
N6-cyclopentyl-2-(3-phenylaminocarbonyltriazene-1-yl)adenosine (TCPA), a very selective agonist with high affinity for the human adenosine A1 receptor.
Journal of medicinal chemistry 2003;46(8):1492-503.
2002: Anna Lorenzen; Margot W Beukers; Piet Hein van der Graaf; Heidrun Lang; Jacqueline van Muijlwijk-Koezen; Miriam de Groote; Wiro M P B Menge; Ulrich Schwabe; Adriaan P IJzerman
Modulation of agonist responses at the A(1) adenosine receptor by an irreversible antagonist, receptor-G protein uncoupling and by the G protein activation state.
Biochemical pharmacology 2002;64(8):1251-65.
2002: Oyvind Edvardsen; Anne Lise Reiersen; Margot W Beukers; Kurt Kristiansen
tGRAP, the G-protein coupled receptors mutant database.
Nucleic acids research 2002;30(1):361-3.
2001: Erica W van Tilburg; Pieter A M van der Klein; Miriam de Groote; Margot W Beukers; Adriaan P IJzerman
Substituted 4-phenyl-2-(phenylcarboxamido)-1,3-thiazole derivatives as antagonists for the adenosine A(1) receptor.
Bioorganic & medicinal chemistry letters 2001;11(15):2017-9.
2001: Jacqueline van Muijlwijk-Koezen; Henk Timmerman; R P van der Sluis; Andrea C van de Stolpe; Wiro M P B Menge; Margot W Beukers; Piet Hein van der Graaf; Miriam de Groote; Adriaan P IJzerman
Synthesis and use of FSCPX, an irreversible adenosine A1 antagonist, as a 'receptor knock-down' tool.
Bioorganic & medicinal chemistry letters 2001;11(6):815-8.
2000: Margot W Beukers; Hans den Dulk; Erica W van Tilburg; Jaap Brouwer; Adriaan P IJzerman
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.
Molecular pharmacology 2000;58(6):1349-56.
1999: Margot W Beukers; I Kristiansen; Adriaan P IJzerman; I Edvardsen
TinyGRAP database: a bioinformatics tool to mine G-protein-coupled receptor mutant data.
Trends in pharmacological sciences 1999;20(12):475-7.
1998: A Dalpiaz; A Townsend-Nicholson; Margot W Beukers; PR Schofield; Adriaan P IJzerman
Thermodynamics of full agonist, partial agonist, and antagonist binding to wild-type and mutant adenosine A1 receptors.
Biochemical pharmacology 1998;56(11):1437-45.
1998: Florence Horn; J Weare; Margot W Beukers; S Hörsch; Amos Bairoch; W Chen; Oyvind Edvardsen; Fabien Campagne; Gert Vriend
GPCRDB: an information system for G protein-coupled receptors.
Nucleic acids research 1998;26(1):275-9.
1997: Margot W Beukers; Corné Klaassen; Willem J De Grip; Dennis Verzijl; Henk Timmerman; Rob Leurs
Heterologous expression of rat epitope-tagged histamine H2 receptors in insect Sf9 cells.
British journal of pharmacology 1997;122(5):867-74.
1996: Martine J Smit; H Timmerman; J Blauw; Margot W Beukers; E Roovers; E H Jacobs; Marcel Hoffmann; R Leurs
The C terminal tail of the histamine H2 receptor contains positive and negative signals important for signal transduction and receptor down-regulation.
Journal of neurochemistry 1996;67(5):1791-800.
1995: Margot W Beukers; C J Kerkhof; M A van Rhee; U Ardanuy; C Gurgel; H Widjaja; Peter Nickel; Adriaan P IJzerman; Willem Soudijn
Suramin analogs, divalent cations and ATP gamma S as inhibitors of ecto-ATPase.
Naunyn-Schmiedeberg's archives of pharmacology 1995;351(5):523-8.
1994: A M van Rhee; M P van der Heijden; Margot W Beukers; Adriaan P IJzerman; Willem Soudijn; Peter Nickel
Novel competitive antagonists for P2 purinoceptors.
European journal of pharmacology 1994;268(1):1-7.
1994: Margot W Beukers; C J Kerkhof; Adriaan P IJzerman; Willem Soudijn
Nucleoside transport inhibition and platelet aggregation in human blood: R75231 and its enantiomers, draflazine and R88016.
European journal of pharmacology 1994;266(1):57-62.
1993: Margot W Beukers; I M Pirovano; A van Weert; C J Kerkhof; Adriaan P IJzerman; Willem Soudijn
Characterization of ecto-ATPase on human blood cells. A physiological role in platelet aggregation?
Biochemical pharmacology 1993;46(11):1959-66.
1992: A Garritsen; Margot W Beukers; Adriaan P IJzerman; E J Cragoe; Willem Soudijn
The mode of interaction of amiloride and some of its analogues with the adenosine A1 receptor.
Neurochemistry international 1992;20(2):207-13.
1990: A Garritsen; Adriaan P IJzerman; Margot W Beukers; Willem Soudijn
Chemical modification of adenosine A1 receptors. Implications for the interaction with R-PIA, DPCPX and amiloride.
Biochemical pharmacology 1990;40(4):835-42.
1990: A Garritsen; Adriaan P IJzerman; Margot W Beukers; E J Cragoe; Willem Soudijn
Interaction of amiloride and its analogues with adenosine A1 receptors in calf brain.
Biochemical pharmacology 1990;40(4):827-34.