Research Topics
Species | Patrick M L VanderheydenSummaryAffiliation: Vrije Universiteit Brussel Country: Belgium Publications
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Publications
Effect of BIBP3226 on inositol phosphate accumulation and cytosolic calcium level in control and NPY Y1 receptor expressing CHO-K1 cellsP M Vanderheyden
Department of Protein Chemistry, Free University of Brussels VUB, Sint Genesius Rode, Belgium
Regul Pept 75:191-9. 1998..This effect of BIBP3226 is likely to be mediated by activation of an until now unknown receptor or cellular target that is endogeneously expressed in CHO-K1 cells...
Synergistic inhibition of the enzymatic activity of aminopeptidase N by divalent metal ion chelatorsPatrick M L Vanderheyden
Department of Molecular and Biochemical Pharmacology, Vrije Universiteit Brussel, Pleinlaan 2, B 1050 Brussels, Belgium
Fundam Clin Pharmacol 20:613-9. 2006..Compatible with this model, Ca2+ may bind to this allosteric site resulting in the potentiation of Zn2+-mediated re-activation of the enzyme activity in the presence of EDTA and 1,10-phenanthroline...
From angiotensin IV binding site to AT4 receptorPatrick M L Vanderheyden
Department of Molecular and Biochemical Pharmacology, Vrije Universiteit Brussel, Brussels, Belgium
Mol Cell Endocrinol 302:159-66. 2009..This link is discussed for the AT(4) receptor by providing an overview of the cellular effects by AT(4) ligands...
Binding characteristics of [(3)H]-irbesartan to human recombinant angiotensin type 1 receptorsP M Vanderheyden
Department of Molecular and Biochemical Pharmacology, Free University of Brussels, Rode, B 1640, Belgium
J Renin Angiotensin Aldosterone Syst 1:159-65. 2000..In contrast, other phenomena such as the plasma half life and tissue-related factors are necessary to explain its sustained in vivo antihypertensive effect...
Inhibition of angiotensin II-induced inositol phosphate production by triacid nonpeptide antagonists in CHO cells expressing human AT1 receptorsP M Vanderheyden
Department of Molecular and Biochemical Pharmacology, Institute of Molecular Biology and Biotechnology, Free University of Brussels, Sint Genesius Rode, Belgium
Pharm Res 17:1482-8. 2000..The aim of the present work is to describe the inhibitory properties of LY301875 and LY303336, two polysubstituted 4-aminoimidazole AT1 receptor antagonists, on CHO cells expressing human recombinant AT1 receptors...
Distinction between surmountable and insurmountable selective AT1 receptor antagonists by use of CHO-K1 cells expressing human angiotensin II AT1 receptorsP M Vanderheyden
Department of Protein Chemistry, Free University of Brussels VUB, Sint Genesius Rode, Belgium
Br J Pharmacol 126:1057-65. 1999....
Angiotensin II type 1 receptor antagonists. Why do some of them produce insurmountable inhibition?P M Vanderheyden
Department of Molecular and Biochemical Pharmacology, Free University of Brussels, Sint Genesius Rode, Belgium
Biochem Pharmacol 60:1557-63. 2000..In addition to the relatively slow dissociation of candesartan, reassociation to the receptor, which is measurable in CHO-AT(1) cells, likely contributes to its long-lasting blood pressure lowering effect in vivo...
Reversible and syntopic interaction between angiotensin receptor antagonists on Chinese hamster ovary cells expressing human angiotensin II type 1 receptorsP M Vanderheyden
Department of Molecular Pharmacology, Free University of Brussels, Sint Genesius Rode, Belgium
Biochem Pharmacol 59:927-35. 2000..In addition, similar kinetic data were obtained from the slowing of the [(3)H]candesartan association rate to antagonist preincubated cells...
Metal ion modulation of cystinyl aminopeptidaseHilde Laeremans
Department of Molecular and Biochemical Pharmacology, Vrije Universiteit Brussel, Pleinlaan 2, B-1050 Brussels, Belgium
Biochem J 390:351-7. 2005..These findings support the concept that high-affinity [125I]angiotensin IV binding, previously referred to as 'AT4 receptor binding', only occurs for the cystinyl aminopeptidase apoenzyme...
Ligand binding and functional properties of human angiotensin AT1 receptors in transiently and stably expressed CHO-K1 cellsMinh Tam Le
Department of Molecular and Biochemical Pharmacology, Institute for Molecular Biology and Biotechnology, Vrije Universiteit Brussel VUB, Belgium
Eur J Pharmacol 513:35-45. 2005..Confocal microscopy revealed rapid internalization induced by angiotensin II and sarile but not by candesartan. The above disparities may result from differences in receptor maturation and/or cellular surrounding...
Peptide and nonpeptide antagonist interaction with constitutively active human AT1 receptorsMinh Tam Le
Department of Molecular and Biochemical Pharmacology, Institute for Molecular Biology and Biotechnology, Vrije Universiteit Brussel VUB, Pleinlaan 2, Belgium
Biochem Pharmacol 65:1329-38. 2003....
Antagonist interaction with endogenous AT(1) receptors in human cell linesIlse Verheijen
Department of Molecular and Biochemical Pharmacology, Free University of Brussels VUB, 65 Paardenstraat, B 1640 Sint Genesius Rode, Belgium
Biochem Pharmacol 64:1207-14. 2002..The similar binding and inhibitory properties of these antagonists among the investigated cell types validates the use of CHO-hAT(1) cells for investigating pharmacological properties of human AT(1) receptors...
Synergistic modulation of cystinyl aminopeptidase by divalent cation chelatorsHeidi Demaegdt
Research Group on Experimental Pharmacology, Department of Molecular and Biochemical Pharmacology, Vrije Universiteit Brussel, Pleinlaan 2, 1050 Brussels, Belgium
Biochem Pharmacol 68:893-900. 2004..Modulation of the effects of 1,10-PHE by other chelators such as EDTA or EGTA, suggests that, in addition to the binding site for zinc in the catalytic site, cystinyl aminopeptidase also bears a regulatory divalent cation binding site...
Effect of saponin and filipin on antagonist binding to AT 1 receptors in intact cellsIlse Verheijen
Department of Molecular and Biochemical Pharmacology, Free University of Brussels VUB, Pleinlaan 2, 1050 Brussels, Belgium
Biochem Pharmacol 67:1601-6. 2004..This suggests that the intracellular composition and/or organisation of living cells play an active role with regard to antagonist-AT1 receptor interactions...
Distinct binding properties of the AT(1) receptor antagonist [(3)H]candesartan to intact cells and membrane preparationsFrederik L P Fierens
Department of Molecular and Biochemical Pharmacology, Free University of Brussels VUB, 65 Paardenstraat, B 1640 Sint Genesius Rode, Belgium
Biochem Pharmacol 63:1273-9. 2002..Whereas the binding was almost completely enthalpy-driven on intact cells, there was a mixed contribution of both enthalpy and entropy on membranes...
Antagonist-radioligand binding to D2L-receptors in intact cellsAnn Packeu
Free University of Brussels VUB, Department of Molecular and Biochemical Pharmacology, Institute for Molecular Biology and Biotechnology, Pleinlaan 2, B 1050 Brussels, Belgium
Biochem Pharmacol 75:2192-203. 2008..To integrate these new findings, a model is proposed in which raclopride approaches the receptor from the aqueous phase, while spiperone approaches the receptor by lateral diffusion within the membrane...
Molecular characterization of the high-affinity [3H]neuropeptide Y-binding component from the venom of Conus anemoneMinh Tam Le
Department of Molecular and Biochemical Pharmacology, Institute for Molecular Biology and Biotechnology, Free University of Brussels VUB, Pleinlaan 2, 1050 Brussel, Belgium
Fundam Clin Pharmacol 17:457-62. 2003..Its approximate molecular weight is 17.5 kDa and its [3H]NPY binding activity is extremely stable below 37 degrees C, even in the absence of protease inhibitors...
Angiotensin IV is a potent agonist for constitutive active human AT1 receptors. Distinct roles of the N-and C-terminal residues of angiotensin II during AT1 receptor activationMinh Tam Le
Department of Molecular and Biochemical Pharmacology, Institute of Molecular Biology and Biotechnology, Vrije Universiteit Brussel, B 1640 Sint Genesius Rode, Belgium
J Biol Chem 277:23107-10. 2002..The receptor adopts a more relaxed conformation, allowing the binding of the C-terminal five residues of Ang II that switches this "preactivated" receptor into the fully active conformation...
Formation of angiotensin-(1-7) from angiotensin II by the venom of Conus geographusMinh Tam Le
Department of Molecular and Biochemical Pharmacology, Institute for Molecular Biology and Biotechnology, Free University of Brussels VUB, Paardenstraat 65, B 1640 Sint Genesius Rode, Belgium
Regul Pept 105:101-8. 2002..The molecular weight of the involved peptidases exceeds 50 kDa, as determined by gel chromatography and ultrafitration...
