Výsledky vyhledávání - "Margot W. Beukers"

Predicting Drug Concentration-Time Profiles in Multiple CNS Compartments Using a Comprehensive Physiologically-Based Pharmacokinetic Model

Autor: Dirk-Jan van den Berg, Elizabeth C. M. de Lange, Pyry A. J. Välitalo, Margot W. Beukers, Johan G. C. van Hasselt, Walter Krauwinkel, An Vermeulen, Robin Hartman, Yumi Yamamoto, Meindert Danhof, Yin Cheong Wong, Dymphy Huntjens, Johannes H. Proost

Publikováno v: CPT: Pharmacometrics & Systems Pharmacology

Drug development targeting the central nervous system (CNS) is challenging due to poor predictability of drug concentrations in various CNS compartments. We developed a generic physiologically based pharmacokinetic (PBPK) model for prediction of drug

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::3d4d715949a80a858f5da61710dffa0a
https://doi.org/10.1002/psp4.12250

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Prediction of human CNS pharmacokinetics using a physiologically-based pharmacokinetic modeling approach

Autor: Yin Cheong Wong, Meindert Danhof, Hannu Kokki, Pyry A. J. Välitalo, Merja Kokki, An Vermeulen, Johannes H. Proost, Johan G. C. van Hasselt, Walter Krauwinkel, Yumi Yamamoto, Elizabeth C. M. de Lange, Margot W. Beukers, Dymphy Huntjens

Publikováno v: European Journal of Pharmaceutical Sciences, 112, 168-179
European Journal of Pharmaceutical Sciences, 112, 168-179. ELSEVIER SCIENCE BV
European Journal of Pharmaceutical Sciences

Knowledge of drug concentration-time profiles at the central nervous system (CNS) target-site is critically important for rational development of CNS targeted drugs. Our aim was to translate a recently published comprehensive CNS physiologically-base

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3bdd37f65ad2e5afa0823cc45a233681
https://pubmed.ncbi.nlm.nih.gov/29133240

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GPCR structure and activation: an essential role for the first extracellular loop in activating the adenosine A2Breceptor

Autor: Gerard J. P. van Westen, Margot W. Beukers, Miriam C. Peeters, Christa E. Müller, Lisanne E Wisse, Dong Guo, Adriaan P. IJzerman

Publikováno v: The FASEB Journal. 25:632-643

The highly variable extracellular loops in G protein-coupled receptors (GPCRs) have been implicated in receptor activation, the mechanism of which is poorly understood. In a random mutagenesis screen on the human adenosine A(2B) receptor (A(2B)R) usi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1df9ea3b1aa1319037e873ca0d091f9b
https://doi.org/10.1096/fj.10-164319

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Characterization of [3H]LUF5834: A novel non-ribose high-affinity agonist radioligand for the adenosine A1 receptor

Autor: Judy Lin, John van Bruchem, Adriaan P. IJzerman, J. Robert Lane, Margot W. Beukers, Elisabeth Klaasse

Publikováno v: Biochemical Pharmacology. 80:1180-1189

The adenosine A(1) receptor is a promising therapeutic target for neurological disorders such as cognition deficits and is involved in cardiovascular preconditioning. Classically adenosine receptor agonists were all derivatives of adenosine, and thou

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::980a7d58f83ce7fbfa1fd95ee0d44215
https://doi.org/10.1016/j.bcp.2010.06.041

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ZM241385, DPCPX, MRS1706 Are Inverse Agonists with Different Relative Intrinsic Efficacies on Constitutively Active Mutants of the Human Adenosine A2B Receptor

Autor: Kai Ye, Ad P. IJzerman, Margot W. Beukers, Jaap Brouwer, Clara C. Blad, Hans den Dulk, Qilan Li

Publikováno v: Journal of Pharmacology and Experimental Therapeutics. 320:637-645

The human adenosine A(2B) receptor belongs to class A G protein-coupled receptors (GPCRs). In our previous work, constitutively active mutant (CAM) human adenosine A(2B) receptors were identified from a random mutation bank. In the current study, thr

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::10cb60ff8e1a9ad4d3bd008a31f08c5b
https://doi.org/10.1124/jpet.106.111203

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Structure-affinity relationships of adenosine A2B receptor ligands

Autor: Margot W. Beukers, Illiana Meurs, Adriaan P. IJzerman

Publikováno v: Medicinal Research Reviews. 26:667-698

Many selective and high affinity agonists and antagonists have been developed for the adenosine A1, A2A, and A3 receptors. Very recently such compounds have been identified for the adenosine A2B receptors. This review presents an overview of the stru

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9e8b8138a9fad11d6b423a9f342c1a7a
https://doi.org/10.1002/med.20069

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2,4,6-Trisubstituted Pyrimidines as a New Class of Selective Adenosine A1 Receptor Antagonists

Autor: Lisa C. W. Chang, Adriaan P. IJzerman, Johannes Brussee, Jacobien K. Von Frijtag Drabbe Künzel, Margot W. Beukers, Gijs Van Den Hout, Thea Mulder-Krieger, Ronald F. Spanjersberg

Publikováno v: Journal of Medicinal Chemistry. 47:6529-6540

Adenosine receptor antagonists usually possess a bi- or tricyclic heteroaromatic structure at their core with varying substitution patterns to achieve selectivity and/or greater affinity. Taking into account molecular modeling results from a series o

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::716a8fd23e7b8811e875be3d57f5d0f7
https://doi.org/10.1021/jm049448r

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A Series of Ligands Displaying a Remarkable Agonistic−Antagonistic Profile at the Adenosine A1 Receptor

Autor: Gijs Van Den Hout, Johannes Brussee, Ronald F. Spanjersberg, Lisa C. W. Chang, Sophie F. Roerink, Adriaan P. IJzerman, Thea Mulder-Krieger, Jacobien K. Von Frijtag Drabbe Künzel, Margot W. Beukers

Publikováno v: Journal of Medicinal Chemistry. 48:2045-2053

Adenosine receptor agonists are usually variations of the natural ligand, adenosine. The ribose moiety in the ligand has previously been shown to be of great importance for the agonistic effects of the compound. In this paper, we present a series of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::334536ee20a46c7f61c90c46dcea84fc
https://doi.org/10.1021/jm049597+

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Random Mutagenesis of the Human Adenosine A2B Receptor Followed by Growth Selection in Yeast. Identification of Constitutively Active and Gain of Function Mutations

Autor: Margot W. Beukers, Jaap Brouwer, Clara C. Blad, Hans den Dulk, Joris van Oppenraaij, Patrick P. W. van der Hoorn, Adriaan P. IJzerman

Publikováno v: Molecular Pharmacology. 65:702-710

To gain insight in spontaneous as well as agonist-induced activation of the human adenosine A2B receptor, we applied a random mutagenesis approach in yeast to create a large number of receptor mutants and selected mutants of interest with a robust sc

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7af0f0d56a0409507a9addcaa9447644
https://doi.org/10.1124/mol.65.3.702

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Potent antagonists for the human adenosine A2B receptor. Derivatives of the triazolotriazine adenosine receptor antagonist ZM241385 with high affinity

Autor: Danielle F. Sleegers, Jacobien K. von Frijtag Drabbe Knzel, Miriam de Groote, Maarten de Zwart, Roel C. Vollinga, Margot W. Beukers, Ad P. IJzerman

Publikováno v: Drug Development Research. 48:95-103

A series of novel and known 5-substituted 7-amino-2-(2-furyl)[1,2,4]triazolo[1,5-a][1,3,5]triazine derivatives were synthesized and tested for adenosine receptor antagonism in radioligand binding assays at all four adenosine receptor subtypes and for

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::a24d019aeeb6d8a86db8f94b6ece671f
https://doi.org/10.1002/(sici)1098-2299(199911)48:3<95::aid-ddr1>3.0.co

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