Research Topics
Species | Georges VauquelinSummaryAffiliation: Vrije Universiteit Brussel Country: Belgium Publications
| Collaborators
|
Detail Information
Publications
Exploring avidity: understanding the potential gains in functional affinity and target residence time of bivalent and heterobivalent ligandsGeorges Vauquelin
Department Molecular and Biochemical Pharmacology, Vrije Universiteit Brussel, Brussels, Belgium
Br J Pharmacol 168:1771-85. 2013..In in vitro experiments, the manifestation of steep saturation curves and of accelerated dissociation in the presence of competitive ligands could mistakenly be interpreted as evidence for non-competitive, allosteric interactions...
Rebinding: or why drugs may act longer in vivo than expected from their in vitro target residence timeGeorges Vauquelin
Free University Brussels VUB, Department of Molecular and Biochemical Pharmacology, Building E 5 10, Pleinlaan 2, B 1050 Brussels, Belgium 32 2 6291955 32 2 6291358
Expert Opin Drug Discov 5:927-41. 2010..Intact cell radioligand dissociation and related ex vivo experiments offer useful indications about a drug's aptitude to experience target rebinding...- Radioligand dissociation measurements: potential interference of rebinding and allosteric mechanisms and physiological relevance of the biological model systemsGeorges Vauquelin
Free University Brussels VUB, Molecular and Biochemical Pharmacology Department, Brussels, Belgium
Expert Opin Drug Discov 7:583-95. 2012.... - Clozapine, atypical antipsychotics, and the benefits of fast-off D2 dopamine receptor antagonismGeorges Vauquelin
Department of Molecular and Biochemical Pharmacology, Vrije Universiteit Brussel, Pleinlaan 2, 1050, Brussels, Belgium
Naunyn Schmiedebergs Arch Pharmacol 385:337-72. 2012..Attention is also drawn to the divergent residence times of hydrophobic antagonists like haloperidol when comparing radioligand binding data on cell membranes with those on intact cells and clinical data... - A two-state receptor model for the interaction between angiotensin II type 1 receptors and non-peptide antagonistsG Vauquelin
Department of Molecular and Biochemical Pharmacology, Free University of Brussels VUB, Sint Genesius Rode, Belgium
Biochem Pharmacol 61:277-84. 2001..In conclusion, these findings provide further support for the concept that insurmountable and surmountable AT1 antagonists are mutually competitive and that insurmountable antagonist-receptor complexes may adopt different states... - New insights in insurmountable antagonismG Vauquelin
Department of Molecular and Biochemical Pharmacology, Free University of Brussels VUB, Sint Genesius Rode, Belgium
Fundam Clin Pharmacol 16:263-72. 2002..New experimental approaches, such as intact cell studies and the use of computer-assisted simulations based on dynamic receptor models, herald the advent of better insight in the future... 
Long-lasting target binding and rebinding as mechanisms to prolong in vivo drug actionGeorges Vauquelin
Department of Molecular and Biochemical Pharmacology, Vrije Universiteit Brussel, Brussels, Belgium
Br J Pharmacol 161:488-508. 2010..By mimicking the complexity of tissues, intact cells offer the opportunity to investigate both mechanisms under the same, physiologically relevant conditions...- Models and methods for studying insurmountable antagonismGeorges Vauquelin
Dept of Molecular and Biochemical Pharmacology, Institute for Molecular Biology and Biotechnology, Free University of Brussels VUB, Paardenstraat 65, B 1640 Sint Genesius Rode, Belgium
Trends Pharmacol Sci 23:514-8. 2002..Intact cell studies allow greater flexibility and tighter control of the experimental conditions and therefore have the potential to offer a better insight into the molecular basis of insurmountable antagonism... - Ligands, their receptors and ... plasma membranesG Vauquelin
Department of Molecular and Biochemical Pharmacology, Institute for Molecular Biology and Biotechnology, Vrije Universiteit Brussel VUB, Pleinlaan 2, B 1050 Brussel, Belgium
Mol Cell Endocrinol 311:1-10. 2009..Pharmacologists focused attention at ligand concentrations in membrane, their adsorption and release rates and the effects thereof on ligand potency and residence time at the receptor... - Slow antagonist dissociation and long-lasting in vivo receptor protectionGeorges Vauquelin
Department of Molecular and Biochemical Pharmacology, Vrije Universiteit Brussel, Pleinlaan 2, B 1050 Brussels, Belgium
Trends Pharmacol Sci 27:356-9. 2006..However, when the half-life of the free antagonist prevails, longer effective protection by slowly dissociating antagonists occurs only if the receptor is exposed to rapid fluctuations in free agonist concentration... - Long-lasting angiotensin type 1 receptor binding and protection by candesartan: comparison with other biphenyl-tetrazole sartansGeorges Vauquelin
Department of Molecular and Biochemical Pharmacology, Free University of Brussels VUB, Brussels, Belgium
J Hypertens Suppl 24:S23-30. 2006..The proportion of insurmountable antagonism, the potency and the dissociation rate of the BTsartans decreases in the order: candesartan > EXP3174 (losartan's active metabolite) > valsartan > irbesartan >> losartan... - The effects of candesartan on human AT1 receptor-expressing Chinese hamster ovary cellsG Vauquelin
Department of Molecular and Biochemical Pharmacology, Institute of Molecular Biology, Free University of Brussels VUB, Sint Genesius Rode, Belgium
J Am Soc Nephrol 10:S15-7. 1999..The insurmountable effect of candesartan can therefore be ascribed to its long-lasting inhibition of the AT1 receptor... - Kinetic versus allosteric mechanisms to explain insurmountable antagonism and delayed ligand dissociationGeorges Vauquelin
Department of Molecular and Biochemical Pharmacology, Free University of Brussels VUB, Building E 5 10, Pleinlaan 2, Brussel B 1050, Belgium
Neurochem Int 51:254-60. 2007..On the other hand, these observations can also be explained by negative allosteric interactions among topographically distinct ligand binding sites at the same receptor or di/multimeric receptor complex... - Angiotensin AT4 receptor ligand interaction with cystinyl aminopeptidase and aminopeptidase N: [125I]Angiotensin IV only binds to the cystinyl aminopeptidase apo-enzymeHeidi Demaegdt
Research Group on Experimental Pharmacology, Department of Molecular and Biochemical Pharmacology, Vrije Universiteit Brussel, Pleinlaan 2, 1050 Brussels, Belgium
Eur J Pharmacol 546:19-27. 2006..We provide evidence that CAP predominates in these cell lines and that, comparatively, CHO-K1 cells display the highest level of this enzyme... - 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... - 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... - A two-state model of antagonist-AT1 receptor interaction: further support by binding studies at low temperatureIlse Verheijen
Department of Molecular and Biochemical Pharmacology, Free University of Brussels VUB, Building E, 2 Pleinlaan, Belgium
Biochem Pharmacol 65:1339-41. 2003..This gave the opportunity to verify the two-state model for the first time with experimental data... - 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.... - 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... - Binding of "AT4 receptor" ligands to insulin regulated aminopeptidase (IRAP) in intact Chinese hamster ovary cellsHeidi Demaegdt
Department of Molecular and Biochemical Pharmacology, Research Group of Experimental Pharmacology, Vrije Universiteit Brussel, Pleinlaan 2, 1050 Brussels, Belgium
Mol Cell Endocrinol 339:34-44. 2011..The in vivo efficacy of stable and unstable "AT(4)-receptor" ligands could therefore differ... - Selective labeling of IRAP by the tritiated AT(4) receptor ligand [3H]Angiotensin IV and its stable analog [3H]AL-11Heidi Demaegdt
Research Group of Experimental Pharmacology, Department of Molecular and Biochemical Pharmacology, Vrije Universiteit Brussel, Pleinlaan 2, 1050 Brussels, Belgium
Mol Cell Endocrinol 311:77-86. 2009..This confirms that the active and apo-forms of IRAP have a distinct pharmacological profile... - Angiotensin IV displays only low affinity for native insulin-regulated aminopeptidase (IRAP)Heidi Demaegdt
Research Group of Experimental Pharmacology, Department of Molecular and Biochemical Pharmacology, Vrije Universiteit Brussel, Pleinlaan 2, 1050 Brussels, Belgium
Fundam Clin Pharmacol 26:194-7. 2012..By using 7B along with the new stable Ang IV-analog [(3) H]AL-11, we here show that the native enzyme is only a low-affinity target for Ang IV... - Conformational constraints in angiotensin IV to probe the role of Tyr², Pro⁵ and Phe⁶Aneta Lukaszuk
Department of Organic Chemistry, Vrije Universiteit Brussel, Pleinlaan 2, 1050 Brussels, Belgium
J Pept Sci 17:545-53. 2011..These results confirm the importance of conformational constrained amino acids to generate selectivity in bioactive peptides... - Endogenous cystinyl aminopeptidase in Chinese hamster ovary cells: characterization by [125I]Ang IV binding and catalytic activityHeidi Demaegdt
Research Group on Experimental Pharmacology, Department of Molecular and Biochemical Pharmacology, Vrije Universiteit Brussel, Pleinlaan 2, Brussels 1050, Belgium
Biochem Pharmacol 68:885-92. 2004..This difference in potency varied from one peptide to another. These pharmacological properties match those previously reported for the recombinantly-expressed human cystinyl aminopeptidase in embryonal kidney cells... - 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... - 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... - 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... - Metabolism of angiotensin II is required for its in vivo effect on dopamine release in the striatum of the ratBart Stragier
Department of Pharmaceutical Chemistry and Drug Analysis, Research Group Experimental Pharmacology, Vrije Universiteit Brussel, Brussels, Belgium
J Neurochem 90:1251-7. 2004..We propose a role for IRAP as mediator for the effects of Ang IV and related peptides on extracellular dopamine levels in the striatum of the rat... - Beta-homo-amino acid scan of angiotensin IVAneta Lukaszuk
Department of Organic Chemistry, Department of Molecular and Biochemical Pharmacology, Vrije Universiteit Brussel, Pleinlaan 2, 1050 Brussels, Belgium
J Med Chem 51:2291-6. 2008.... - Involvement of the AT1 receptor subtype in the effects of angiotensin IV and LVV-haemorphin 7 on hippocampal neurotransmitter levels and spatial working memoryDimitri De Bundel
Research Group Experimental Pharmacology, Department of Pharmaceutical Chemistry, Drug Analysis and Drug Information, Vrije Universiteit Brussel, Brussels, Belgium
J Neurochem 112:1223-34. 2010..c.v. injection, suggesting an extrahippocampal site of action. We propose that AT1 receptors are implicated in the neurochemical and cognitive effects of Ang IV, whereas LVV-H7 may mediate its effects via IRAP... - 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... - The replacement of His(4) in angiotensin IV by conformationally constrained residues provides highly potent and selective analoguesAneta Lukaszuk
Department of Organic Chemistry, Vrije Universiteit Brussel, Pleinlaan 2, 1050 Brussels, Belgium
J Med Chem 52:5612-8. 2009.... - Non-competitive interaction between raclopride and spiperone on human D-receptors in intact Chinese hamster ovary cellsAnn Packeu
Department of Molecular and Biochemical Pharmacology, Institute for Molecular Biology and Biotechnology, Free University of Brussels VUB, Pleinlaan 2, B 1050 Brussels, Belgium
Fundam Clin Pharmacol 24:283-91. 2010..These new findings could point at the occurrence of allosteric interactions between different classes of D(2)-receptor antagonists... - Involvement of insulin-regulated aminopeptidase in the effects of the renin-angiotensin fragment angiotensin IV: a reviewBart Stragier
Department of Pharmaceutical Chemistry, Drug Analysis and Drug Information, Research Group Experimental Pharmacology, Vrije Universiteit Brussel, Brussels, Belgium
Heart Fail Rev 13:321-37. 2008..On the other hand, a wide range of studies have made it clear that IRAP might become an important target for drug development against different pathologies such as Alzheimer's disease, epilepsy and ischemia... - Molecular characterisation of the interactions between olmesartan and telmisartan and the human angiotensin II AT1 receptorM T Le
Departments of Molecular and Biochemical Pharmacology, Free University of Brussels VUB, Pleinlaan 2, B 1050 Brussels, Belgium
Br J Pharmacol 151:952-62. 2007..This study compared the molecular interactions of olmesartan and telmisartan with the human AT(1) receptor, using well characterised in vitro methods and model systems... - Pressor and renal hemodynamic effects of the novel angiotensin A peptide are angiotensin II type 1A receptor dependentRui Yang
Department of Pharmacology, Vrije Universiteit Brussel, Laarbeeklaan 103, B 1090 Brussels, Belgium
Hypertension 57:956-64. 2011..Overall, the responses to Ang A and Ang II were similar. Ang A has no physiological role to modulate the pressor and renal hemodynamic effects of Ang II... - Amino triazolo diazepines (Ata) as constrained histidine mimicsKoen Buysse
Laboratory of Organic Chemistry, Vrije Universiteit Brussel, Pleinlaan 2, B 1050 Brussels, Belgium
Org Lett 13:6468-71. 2011.... - 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-D2S-dopamine receptor interactions in intact recombinant Chinese hamster ovary cells [corrected]Ann Packeu
Department of Molecular and Biochemical Pharmacology, Institute for Molecular Biology and Biotechnology, Free University of Brussels VUB, Pleinlaan 2, B 1050 Brussels, Belgium
Fundam Clin Pharmacol 24:293-303. 2010..These different modes of approach could imply the existence of topologically distinct ligand binding sites at D(2)-receptors... - Effects of BIBP3226 and BIBP3435 on cytosolic calcium in neuropeptide Y Y1 receptor-transfected Chinese hamster ovary cells and wild type CHO-K1 cellsP M Vanderheyden
Department of Molecular and Biochemical Pharmacology, Free University of Brussels (VUB, Paardenstraat 65, B-1640 Sint-Genesius Rode, Belgium
J Recept Signal Transduct Res 21:11-23. 2001.... - Cellular targets for angiotensin II fragments: pharmacological and molecular evidenceGeorges Vauquelin
Department of Molecular and Biochemical Pharmacology, Vrije Universiteit Brussel (VUB, Sint-Genesius, Rode, B-1640, Belgium
J Renin Angiotensin Aldosterone Syst 3:195-204. 2002.... - [(3)H]IVDE77, a novel radioligand with high affinity and selectivity for the insulin-regulated aminopeptidaseAlexandros Nikolaou
Molecular and Biochemical Pharmacology, Vrije Universiteit Brussel, Building E, Pleinlaan 2, B 1050 Brussels, Belgium Myeloid Cell Immunology Laboratory, VIB, Brussels, Belgium Cellular and Molecular Immunology Unit, Vrije Universiteit Brussel, Building E, Pleinlaan 2, B 1050 Brussels, Belgium
Eur J Pharmacol 702:93-102. 2013..In summary, IVDE77 is a useful tool for the detection of IRAP under physiological conditions, and may contribute to elucidating the mechanism of Ang IV to ascertain which functions are IRAP-dependent... - 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... - Interaction between the partially insurmountable antagonist valsartan and human recombinant angiotensin II type 1 receptorsI Verheijen
Department of Molecular and Biochemical Pharmacology, Free University of Brussels, Belgium
Fundam Clin Pharmacol 14:577-85. 2000..These kinetic data suggest that the insurmountable inhibition by valsartan is related to its relatively slow dissociation from the human AT1 receptors... - 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... - Tight binding of the angiotensin AT(1) receptor antagonistF L Fierensa
Department of Molecular and Biochemical Pharmacology, Institute for Molecular Biology, Free University of Brussels, Paardenstraat 65, B 1640, Sint Genesius Rode, Belgium
Biochem Pharmacol 61:1227-35. 2001..Insurmountable antagonism of candesartan is therefore independent from receptor internalization via clathrin-coated pits... - AT1 receptor antagonistsI Verheijen
Department of Molecular and Biochemical Pharmacology, Free University of Brussels VUB, 2 Pleinlaan, 1050 Brussels, Belgium
Curr Med Chem Cardiovasc Hematol Agents 2:69-77. 2004..This may contribute to their long lasting clinical effect. This paper also focuses on the influence of a number of methodological approaches used to study AT1 receptor antagonists on their observed in vitro receptor binding properties... - 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... - Lys(199) mutation of the human angiotensin type 1 receptor differentially affects the binding of surmountable and insurmountable non-peptide antagonistsF L Fierens
Department of Molecular and Biochemical Pharmacology, Free University of Brussels, Rode, B 1640, Belgium
J Renin Angiotensin Aldosterone Syst 1:283-8. 2000..His256 -->Ala substitution had only minor effects. This suggests that Lys199 is important for the tight binding of non-peptide antagonists... - 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... - Translocation of the insulin-regulated aminopeptidase to the cell surface: detection by radioligand bindingH Demaegdt
Department of Molecular and Biochemical Pharmacology, Vrije Universiteit Brussel, Brussels, Belgium
Br J Pharmacol 154:872-81. 2008..A more widespread application of the method was demonstrated by the use of 3T3-L1 adipocytes... - Identification and characterization of imidazoline-binding sites from calf striatumE Czerwiec
Department of Protein Chemistry, Institute for Molecular Biology and Biotechnology, Free University of Brussels VUB, St Genesius Rode, Belgium
Eur J Pharmacol 315:99-109. 1996..The venom of the marine snail Conus geographus is the most potent of the 13 tested Conus venom preparations. None of the tested venoms is able to discriminate between both sites... - 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... - 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.... - Insurmountable angiotensin AT1 receptor antagonists: the role of tight antagonist bindingF L Fierens
Department of Molecular and Biochemical Pharmacology, Free University of Brussels VUB, Belgium
Eur J Pharmacol 372:199-206. 1999..Our data indicate that antagonist-receptor complexes are divided into a fast reversible/surmountable population and a tight binding/insurmountable population at the very onset of the incubation with angiotensin II... - G protein-coupled receptors: a count of 1001 conformationsG Vauquelin
Department of Molecular and Biochemical Pharmacology, Institute for Molecular Biology and Biotechnology, Vrije Universiteit Brussel VUB, Pleinlaan 2, B 1050 Brussel, Belgium
Fundam Clin Pharmacol 19:45-56. 2005..g. other cellular proteins, lipids) allosteric modulators also affect ligand-GPCR interaction and receptor activation. These new developments in GPCR research could lead to the development of more selective therapeutic drugs... - 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... - Subtypes of adrenergic and dopaminergic receptors in bovine cerebral blood vesselsJ De Keyser
Department of Neurology, Akademisch Ziekenhuis, Vrije Universiteit Brussel, Belgium
Neurosci Lett 85:272-6. 1988..This suggests a functionally more important vasoconstrictor adrenergic control of the cerebral circulation in pial vessels of the convexity than in the arteries at the base of the brain... - Sartan-AT1 receptor interactions: in vitro evidence for insurmountable antagonism and inverse agonismI Van Liefde
Department of Molecular and Biochemical Pharmacology, Institute for Molecular Biology and Biotechnology, Vrije Universiteit Brussel VUB, Brussel, Belgium
Mol Cell Endocrinol 302:237-43. 2009..This rather affects long-term, G protein-independent hypertrophic responses leading to cardiovascular remodelling... - Involvement of insulin-regulated aminopeptidase and/or aminopeptidase N in the angiotensin IV-induced effect on dopamine release in the striatum of the ratBart Stragier
Research Group Experimental Pharmacology, Department of Pharmaceutical Chemistry, Drug Analysis and Drug Information, Vrije Universiteit Brussel Laarbeeklaan 103 B 1090 Brussels, Belgium
Brain Res 1131:97-105. 2007..We therefore hypothesize that the effect of angiotensin IV on dopamine release in the striatum is mediated via activation of IRAP and/or AP-N, possibly acting as receptors for angiotensin IV... - Cyclic insulin-regulated aminopeptidase (IRAP)/AT4 receptor ligandsAndreas Axén
Department of Medicinal Chemistry, Uppsala University, Box 574, SE 75123 Uppsala, Sweden
J Pept Sci 12:705-13. 2006..The cyclic constrained analogs allowed us to propose a tentative bioactive conformation of angiotensin IV and it seems that the peptide adopts an inverse gamma-turn at the C-terminal... - Agonist induction and conformational selection during activation of a G-protein-coupled receptorLaszlo Hunyady
Department of Physiology, Semmelweis University, Faculty of Medicine, Budapest, Hungary
Trends Pharmacol Sci 24:81-6. 2003..Because agonist binding also actively facilitates the conformational rearrangements leading to activation of other GPCRs we propose that agonist induction should be considered as a general mechanism of GPCR activation... - Ligands to the (IRAP)/AT4 receptor encompassing a 4-hydroxydiphenylmethane scaffold replacing Tyr2Hanna Andersson
Department of Medicinal Chemistry, Uppsala University, Box 574, SE 751 23 Uppsala, Sweden
Bioorg Med Chem 16:6924-35. 2008.... - Inhibitory activity on binding of specific ligands to the human angiotensin II AT(1) and endothelin 1 ET(A) receptors: bioactive benzo[c]phenanthridine alkaloids from the root of Bocconia frutescensCatherina Caballero-George
Department of Pharmaceutical Sciences, University of Antwerp, Antwerp, Belgium
Planta Med 68:770-5. 2002..Furthermore, the ability of these compounds to block AT(1) and/or ET(A) receptors may provide some justification for the traditional use of Bocconia frutescens L. to control hypertension... - In vitro inhibition of [3H]-angiotensin II binding on the human AT1 receptor by proanthocyanidins from Guazuma ulmifolia barkCatherina Caballero-George
Department of Pharmaceutical Sciences, University of Antwerp, Antwerp, Belgium
Planta Med 68:1066-71. 2002..Angiotensin II AT 1 receptor binding might be considered as a potentially interesting biological activity of proanthocyanidins contributing to the very broad spectrum of biological activities of the condensed tannins... - In vitro effect of sanguinarine alkaloid on binding of [3H]candesartan to the human angiotensin AT1 receptorCatherina Caballero-George
Department of Pharmaceutical Sciences, University of Antwerp, Belgium
Eur J Pharmacol 458:257-62. 2003..The present findings indicate that sanguinarine interacts with the receptor in a slow, nearly irreversible and noncompetitive manner... - Small potent ligands to the insulin-regulated aminopeptidase (IRAP)/AT(4) receptorAndreas Axén
Department of Medicinal Chemistry, Uppsala University, Box 574, SE 751 23 Uppsala, Sweden
J Pept Sci 13:434-44. 2007..Furthermore, ligand 4 is degraded considerably more slowly in membrane preparations than angiotensin IV. Hence, it might constitute a suitable research tool for biological studies of the (IRAP)/AT(4) receptor... - Cys2,7EtalphaCGRP is a potent agonist for CGRP1 receptors in SK-N-MC cellsChristina Nodin
Preclinical Research and Development, , , Sweden
Biochem Pharmacol 69:1235-40. 2005..Differences between the agonistic profile of this ligand in this and other experimental systems might be species--or even cell type--dependent... - Expression, binding, and signaling properties of CRF2(a) receptors endogenously expressed in human retinoblastoma Y79 cells: passage-dependent regulation of functional receptorsEric Gutknecht
CNS Research, Johnson and Johnson Research and Development, Beerse, Belgium
J Neurochem 104:926-36. 2008..These data demonstrate that Y79 cells express functional CRF1 and CRF2a receptors and that the CRF2(a) receptor protein is up-regulated during prolonged culture...