G. Vauquelin

发表

A study of the molecular mechanism of binding kinetics and long residence times of human CCR5 receptor small molecule allosteric ligands

D. Swinney, Jun Zhang, P. Beavis, 2014, British journal of pharmacology.

Clozapine, atypical antipsychotics, and the benefits of fast-off D2 dopamine receptor antagonism

P. Seeman, G. Vauquelin, Sophie Bostoen, 2012, Naunyn-Schmiedeberg's Archives of Pharmacology.

Exploring avidity: understanding the potential gains in functional affinity and target residence time of bivalent and heterobivalent ligands

S. Charlton, G. Vauquelin, Georges Vauquelin, 2013, British journal of pharmacology.

The influence of drug distribution and drug‐target binding on target occupancy: The rate‐limiting step approximation

P. H. van der Graaf, G. Vauquelin, W. E. A. de Witte, 2017, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.

Effect of BIBP3226 on inositol phosphate accumulation and cytosolic calcium level in control and NPY Y1 receptor expressing CHO-K1 cells

G. Vauquelin, G. Ebinger, P. Vanderheyden, 1998, Regulatory Peptides.

Molecular mechanism of allosteric modulation at GPCRs: insight from a binding kinetics study at the human A1 adenosine receptor

A. IJzerman, D. Guo, L. Heitman, 2014, British journal of pharmacology.

Review: Structural requirements for signalling and regulation of AT1-receptors

L. Hunyady, K. Catt, G. Vauquelin, 2001, Journal of the renin-angiotensin-aldosterone system : JRAAS.

[3H]-BIBP3226 and [3H]-NPY binding to intact SK-N-MC cells and CHO cells expressing the human Y1 receptor.

G. Vauquelin, P. Vanderheyden, I. Van Liefde, 1998, Journal of receptor and signal transduction research.

Distinct binding properties of the AT(1) receptor antagonist [(3)H]candesartan to intact cells and membrane preparations.

G. Vauquelin, P. Vanderheyden, J. De Backer, 2002, Biochemical pharmacology.

Expression, binding, and signaling properties of CRF2(a) receptors endogenously expressed in human retinoblastoma Y79 cells: passage‐dependent regulation of functional receptors

I. van der Linden, R. Hauger, G. Vauquelin, 2008, Journal of neurochemistry.

AT1 Receptor Interactions

G. Vauquelin, P. Vanderheyden, 2004 .

New insights in insurmountable antagonism

G. Vauquelin, P. Vanderheyden, I. Van Liefde, 2002, Fundamental & clinical pharmacology.

Models and methods for studying insurmountable antagonism.

G. Vauquelin, P. Vanderheyden, I. Van Liefde, 2002, Trends in pharmacological sciences.

Avidity and positive allosteric modulation/cooperativity act hand in hand to increase the residence time of bivalent receptor ligands

G. Vauquelin, G. Bricca, I. Van Liefde, 2014, Fundamental & clinical pharmacology.

Simplified models for heterobivalent ligand binding: when are they applicable and which are the factors that affect their target residence time

G. Vauquelin, 2013, Naunyn-Schmiedeberg's Archives of Pharmacology.

Determination of drug–receptor residence times by radioligand binding and functional assays: experimental strategies and physiological relevance

G. Vauquelin, 2012 .

Rebinding: or why drugs may act longer in vivo than expected from their in vitro target residence time

G. Vauquelin, 2010, Expert opinion on drug discovery.

Slow antagonist dissociation and long-lasting in vivo receptor protection.

G. Vauquelin, I. Van Liefde, 2006, Trends in pharmacological sciences.

Neurokinin 1 Receptor Antagonists: Correlation between in Vitro Receptor Interaction and in Vivo Efficacy

G. Vauquelin, E. Lindström, Rakel Martinsson, 2007, Journal of Pharmacology and Experimental Therapeutics.

Molecular mechanisms for the persistent bronchodilatory effect of the β2‐adrenoceptor agonist salmeterol

G. Vauquelin, A. Szczuka, A. Packeu, 2009, British journal of pharmacology.

J. De Keyser, G. Vauquelin, G. Ebinger, 1990, Annals of neurology.

D1-dopamine receptor abnormality in frontal cortex points to a functional alteration of cortical cell membranes in Alzheimer's disease.

J. De Keyser, G. Vauquelin, G. Ebinger, 1990, Archives of neurology.

Molecular Mechanisms of Corticotropin-Releasing Factor Receptor-Induced Calcium Signaling

I. van der Linden, G. Vauquelin, F. Dautzenberg, 2009, Molecular Pharmacology.

Subtypes of adrenergic and dopaminergic receptors in bovine cerebral blood vessels

G. Vauquelin, A. Convents, J. Keyser, 1988, Neuroscience Letters.

The β-adrenergic receptor of turkey erythrocyte membranes: Conformational modification by β-adrenergic agonists

A. Strosberg, G. Vauquelin, O. Durieu, 1979 .

Inactivation of beta-adrenergic receptors by N-ethylmaleimide in S49 lymphoma cells. Agonist induction of functional receptor heterogeneity.

M. Maguire, G. Vauquelin, 1980, Molecular pharmacology.

Inactivation of beta-adrenergic receptors by N-ethylmaleimide: permissive role of beta-adrenergic agents in relation to adenylate cyclase activation.

A. Strosberg, G. Vauquelin, S. Bottari, 1980, Molecular pharmacology.

Interaction between beta-adrenergic receptors and guanine nucleotide sites in turkey erythrocyte membranes.

A. Strosberg, G. Vauquelin, B. Jacobsson, 1980, Proceedings of the National Academy of Sciences of the United States of America.

Cyclic insulin‐regulated aminopeptidase (IRAP)/AT4 receptor ligands

G. Lindeberg, A. Karlén, G. Vauquelin, 2006, Journal of peptide science : an official publication of the European Peptide Society.

Beta-homo-amino acid scan of angiotensin IV.

P. Karoyan, A. Misicka, G. Vauquelin, 2008, Journal of medicinal chemistry.

Regional Distribution of α2A‐and α2B‐Adrenoceptor Subtypes in Postmortem Human Brain

G. Vauquelin, J. Keyser, Hilde De Vos, 1992 .

Mivazerol, a novel compound with high specificity for α 2 adrenergic receptors: Binding studies on different human and rat membrane preparations

J. Gobert, G. Vauquelin, E. Wülfert, 1994, Neurochemistry International.

α2A Adrenoceptors and non-adrenergic idazoxan binding sites in calf brain and retina are distinct from those in human brain

G. Vauquelin, J. Keyser, I. V. Liefde, 1993, Neurochemistry International.

Characterization of alpha 2-adrenergic receptors of calf retina membranes by [3H]-rauwolscine and [3H]-RX 781094 binding.

G. Vauquelin, A. Convents, J. De Backer, 1987, Biochemical pharmacology.

Shallow agonist competition binding curves for beta-adrenergic receptors: the role of tight agonist binding.

A. IJzerman, H. Timmerman, G. Vauquelin, 1987, Molecular pharmacology.

High affinity binding of 3H rauwolscine and 3H RX781094 to alpha 2 adrenergic receptors and non-stereoselective sites in human and rabbit brain cortex membranes.

J. De Keyser, G. Vauquelin, A. Convents, 1989, Biochemical pharmacology.

[3H]Rauwolscine labels α2-adrenoceptors and 5-HT1A receptors in human cerebral cortex

G. Vauquelin, A. Convents, J. Keyser, 1989 .

Identification of α 2 adrenergic receptors in human frontal cortex membranes by binding of [3H]RX 821002, the 2-methoxy analog of [3H]idazoxan

G. Vauquelin, G. Ebinger, J. Backer, 1990, Neurochemistry International.

Chronic isoproterenol administration causes altered beta adrenoceptor-Gs-coupling in guinea pig lung.

G. Vauquelin, V. Nerme, T. Abrahamsson, 1990, The Journal of pharmacology and experimental therapeutics.

EFFECTS OF BIBP3226 AND BIBP3435 ON CYTOSOLIC CALCIUM IN NEUROPEPTIDE Y Y1 RECEPTOR-TRANSFECTED CHINESE HAMSTER OVARY CELLS AND WILD TYPE CHO-K1 CELLS

G. Vauquelin, G. Ebinger, P. Vanderheyden, 2001, Journal of receptor and signal transduction research.

Interaction between the partially insurmountable antagonist valsartan and human recombinant angiotensin II type 1 receptors

G. Vauquelin, P. Vanderheyden, J. Debacker, 2000, Fundamental & clinical pharmacology.

Conformational constraints in angiotensin IV to probe the role of Tyr2, Pro5 and Phe6

G. Vauquelin, D. Tourwé, P. Vanderheyden, 2011, Journal of peptide science : an official publication of the European Peptide Society.

Agonist-mediated conformational changes of β-adrenoceptors could occur independent of functional coupling to Ns

G. Vauquelin, L. Kanarek, Y. Severne, 1986, Naunyn-Schmiedeberg's Archives of Pharmacology.

Cellular targets for angiotensin II fragments: pharmacological and molecular evidence

Y. Michotte, G. Vauquelin, I. Smolders, 2002, Journal of the renin-angiotensin-aldosterone system : JRAAS.

Distinction between surmountable and insurmountable selective AT1 receptor antagonists by use of CHO‐K1 cells expressing human angiotensin II AT1 receptors

G. Vauquelin, P. Vanderheyden, J. De Backer, 1999, British journal of pharmacology.

Agonist induction and conformational selection during activation of a G-protein-coupled receptor.

L. Hunyady, G. Vauquelin, P. Vanderheyden, 2003, Trends in pharmacological sciences.

KLHL12-mediated ubiquitination of the dopamine D4 receptor does not target the receptor for degradation.

G. Haegeman, G. Vauquelin, K. Van Craenenbroeck, 2010, Cellular signalling.

Angiotensin IV Is a Potent Agonist for Constitutive Active Human AT1 Receptors

L. Hunyady, G. Vauquelin, P. Vanderheyden, 2002, The Journal of Biological Chemistry.

Translocation of the insulin‐regulated aminopeptidase to the cell surface: detection by radioligand binding

Y. Michotte, G. Vauquelin, P. Vanderheyden, 2008, British journal of pharmacology.

Involvement of insulin-regulated aminopeptidase in the effects of the renin–angiotensin fragment angiotensin IV: a review

Y. Michotte, G. Vauquelin, I. Smolders, 2008, Heart Failure Reviews.

Cys2,7EtαCGRP is a potent agonist for CGRP1 receptors in SK-N-MC cells

G. Vauquelin, C. Nodin, B. Mentzer, 2005 .

Synergistic modulation of cystinyl aminopeptidase by divalent cation chelators.

Y. Michotte, V. Kersemans, G. Vauquelin, 2004, Biochemical pharmacology.

No functional atypical β-adrenergic receptors in human omental adipocytes

G. Vauquelin, I. V. Liefde, A. Ermen, 1994 .

Isoproterenol and selective agonists stimulate similar atypical beta-adrenoceptors in rat adipocytes.

G. Vauquelin, I. Van Liefde, A. van Witzenburg, 1993, Biochemical Pharmacology.

Inhibition of evoked neurotransmitter release from rat hippocampus by a polypeptide toxin isolated from the marine snail Conus distans

G. Vauquelin, V. Saxena, E. Coen, 1992, Neurochemistry International.

Cirsimarin and Cirsimaritin, Flavonoids of Microtea debilis (Phytolaccaceae) with Adenosine Antagonistic Properties in Rats: Leads for New Therapeutics in Acute Renal Failure

G. Vauquelin, A. Vlietinck, T. Bruyne, 1997, The Journal of pharmacy and pharmacology.

Serotonin binding proteins "SBP": target proteins and tool for in vitro neurotoxicity studies.

C. Velez-Pardo, G. Vauquelin, G. Ebinger, 1995, General pharmacology.

Serotonin Binding Proteins: An In Vitro Model System for Monoamine‐related Neurotoxicity a

G. Vauquelin, C. Pardo, M. J. Rio, 1994, Annals of the New York Academy of Sciences.

Case Study: Angiotensin Receptor Blockers (ARBs)

G. Vauquelin, 2015 .

‘Partial’ competition of heterobivalent ligand binding may be mistaken for allosteric interactions: a comparison of different target interaction models

S. Charlton, G. Vauquelin, David Hall, 2015, British journal of pharmacology.

A two-state receptor model for the interaction between angiotensin II type 1 receptors and non-peptide antagonists.

G. Vauquelin, P. Morsing, P. Vanderheyden, 2001, Biochemical pharmacology.

Binding properties of antagonists to Cannabinoid receptors in intact cells

S. Hjorth, J. Clapham, G. Vauquelin, 2011, Fundamental & clinical pharmacology.

D1 and D2 Dopamine Receptors in Human Substantia Nigra: Localization and the Effect of Aging

G. Vauquelin, J. Keyser, G. Ebinger, 1991, Journal of neurochemistry.

In Human Brain Two Subtypes of D1 Dopamine Receptors Can Be Distinguished on the Basis of Differences in Guanine Nucleotide Effect on Agonist Binding

G. Vauquelin, J. Keyser, G. Ebinger, 1989, Journal of neurochemistry.

Receptors for corticotropin-releasing hormone in human pituitary: binding characteristics and autoradiographic localization to immunocytochemically defined proopiomelanocortin cells.

G. Klöppel, L. Moons, J. Smitz, 1991, The Journal of clinical endocrinology and metabolism.

Lack of GTP-insensitive D2 dopamine receptors in Huntington's disease

R. Roos, G. Vauquelin, J. Keyser, 1989, Journal of the Neurological Sciences.

Distinct In Vitro Binding Profile of the Somatostatin Receptor Subtype 2 Antagonist [177Lu]Lu-OPS201 Compared to the Agonist [177Lu]Lu-DOTA-TATE

G. Vauquelin, P. Plas, R. Mansi, 2021, Pharmaceuticals.

Sartan–AT1 receptor interactions: In vitro evidence for insurmountable antagonism and inverse agonism

G. Vauquelin, I. V. Liefde, Georges Vauquelin, 2009, Molecular and Cellular Endocrinology.

Reversible and syntopic interaction between angiotensin receptor antagonists on Chinese hamster ovary cells expressing human angiotensin II type 1 receptors.

G. Vauquelin, P. Vanderheyden, J. De Backer, 2000, Biochemical pharmacology.

Estimation of the dissociation rate of unlabelled ligand–receptor complexes by a ‘two‐step’ competition binding approach

G. Vauquelin, A. Balendran, A. Packeu, 2010, British journal of pharmacology.

Unravelling the complex dissociation of [3H]‐rimonabant from plated CB1 cannabinoid receptor‐expressing cells

J. Clapham, G. Vauquelin, A. Balendran, 2009, Fundamental & clinical pharmacology.

Angiotensin II type 1 receptor antagonists. Why do some of them produce insurmountable inhibition?

G. Vauquelin, P. Vanderheyden, F. Fierens, 2000, Biochemical pharmacology.

Identification and chemical characterisation of beta-adrenergic receptors in intact turkey erythrocytes.

A. Strosberg, G. Vauquelin, J. De Backer, 1981, Biochemical pharmacology.

Regional distribution of alpha 2A- and alpha 2B-adrenoceptor subtypes in postmortem human brain.

J. De Keyser, G. Vauquelin, I. Van Liefde, 1992, Journal of neurochemistry.

Species and strain-related differences in the expression and functionality of beta-adrenoceptor subtypes in adipose tissue.

G. Vauquelin, A. Van Ermen, I. Van Liefde, 1994, Archives internationales de pharmacodynamie et de therapie.

Insurmountable AT(1) receptor antagonism: the need for different antagonist binding states of the receptor.

G. Vauquelin, P. Vanderheyden, F. Fierens, 2001, Trends in pharmacological sciences.

Insurmountable angiotensin AT1 receptor antagonists: the role of tight antagonist binding.

G. Vauquelin, P. Vanderheyden, J. De Backer, 1999, European journal of pharmacology.

Multiple beta adrenergic receptor subclasses mediate the l-isoproterenol-induced lipolytic response in rat adipocytes.

G. Vauquelin, I. Van Liefde, A. van Witzenburg, 1992, The Journal of pharmacology and experimental therapeutics.

Endogenous noradrenaline masks beta-adrenergic receptors in rat heart membranes via tight agonist binding.

G. Vauquelin, V. Nerme, T. Abrahamsson, 1985, Biochemical pharmacology.

G Protein-Coupled Receptors: Molecular Pharmacology from Academic Concept to Pharmaceutical Research

G. Vauquelin, B. Mentzer, 2008 .

Two polypeptide toxins with opposite effects on calcium uptake in bovine chromaffin cells: Isolation from the venom of the marine snail Conus distans

G. Vauquelin, E. Coen, W. P. Potter, 1996, Neurochemistry International.

Differential regulation of alpha-adrenergic receptor subclasses by gonadal steroids in human myometrium.

G. Vauquelin, J. Lescrainier, S. Bottari, 1983, The Journal of clinical endocrinology and metabolism.

Formation of angiotensin-(1–7) from angiotensin II by the venom of Conus geographus

J. Broeck, G. Baggerman, G. Vauquelin, 2002, Regulatory Peptides.

Binding of ”AT receptor” ligands to insulin regulated aminopeptidase (IRAP) in intact Chinese hamster ovary cells

G. Vauquelin, P. Gard, D. Tourwé, 2020 .

[3H]IVDE77, a novel radioligand with high affinity and selectivity for the insulin-regulated aminopeptidase.

J. V. Van Ginderachter, G. Vauquelin, D. Tourwé, 2013, European Journal of Pharmacology.

Binding of “AT4 receptor” ligands to insulin regulated aminopeptidase (IRAP) in intact Chinese hamster ovary cells

G. Vauquelin, P. Gard, D. Tourwé, 2011, Molecular and Cellular Endocrinology.

Pressor and Renal Hemodynamic Effects of the Novel Angiotensin A Peptide Are Angiotensin II Type 1A Receptor Dependent

A. Dupont, T. Walther, G. Vauquelin, 2011, Hypertension.

Renin-Angiotensin-Aldosterone System Pressor and Renal Hemodynamic Effects of the Novel Angiotensin A Peptide Are Angiotensin II Type 1 A Receptor Dependent

A. Dupont, T. Walther, G. Vauquelin, 2011 .

Selective labeling of IRAP by the tritiated AT4 receptor ligand [3H]Angiotensin IV and its stable analog [3H]AL-11

Y. Michotte, G. Vauquelin, S. Chakravarthy, 2009, Molecular and Cellular Endocrinology.

Ligands to the (IRAP)/AT4 receptor encompassing a 4-hydroxydiphenylmethane scaffold replacing Tyr2.

G. Lindeberg, A. Karlén, G. Vauquelin, 2008, Bioorganic & medicinal chemistry.

Molecular characterisation of the interactions between olmesartan and telmisartan and the human angiotensin II AT1 receptor

G. Vauquelin, M. Pugsley, I. Van Liefde, 2007, British journal of pharmacology.

Involvement of insulin-regulated aminopeptidase and/or aminopeptidase N in the angiotensin IV-induced effect on dopamine release in the striatum of the rat

Y. Michotte, G. Vauquelin, I. Smolders, 2007, Brain Research.

Peptide and nonpeptide antagonist interaction with constitutively active human AT1 receptors.

L. Hunyady, V. Kersemans, G. Vauquelin, 2003, Biochemical pharmacology.

In vitro effect of sanguinarine alkaloid on binding of [3H]candesartan to the human angiotensin AT1 receptor.

Mahabir P. Gupta, C. Caballero-George, G. Vauquelin, 2003, European journal of pharmacology.

Tight binding of the angiotensin AT1 receptor antagonist [3H]candesartan is independent of receptor internalization

G. Vauquelin, P. Vanderheyden, T. Thekkumkara, 2001 .

Role of basic amino acids of the human angiotensin type 1 receptor in the binding of the non-peptide antagonist candesartan

L. Hunyady, G. Vauquelin, P. Vanderheyden, 2001, Journal of the renin-angiotensin-aldosterone system : JRAAS.

Soluble serotonin and catecholamine binding proteins in the bovine adrenal medulla

G. Vauquelin, G. Ebinger, C. Pardo, 1993, Neurochemistry International.

Serotonin binding proteins in bovine retina: Binding of serotonin and catecholamines

G. Vauquelin, G. Ebinger, W. Potter, 1993, Neurochemistry International.

Effect of saponin and filipin on antagonist binding to AT 1 receptors in intact cells.

Dieter M. Tourlousse, G. Vauquelin, P. Vanderheyden, 2004, Biochemical pharmacology.

Sartan-AT receptor interactions: evidence for insurmountable antagonism and inverse agonism

G. Vauquelin, I. V. Liefde, I. Liefde, 2020 .

Ligand binding and functional properties of human angiotensin AT1 receptors in transiently and stably expressed CHO-K1 cells.

L. Hunyady, G. Vauquelin, P. Vanderheyden, 2005, European journal of pharmacology.

Metabolism of angiotensin II is required for its in vivo effect on dopamine release in the striatum of the rat

Y. Michotte, G. Vauquelin, G. Ebinger, 2004, Journal of neurochemistry.

Molecular characterization of the high‐affinity [3H]neuropeptide Y‐binding component from the venom of Conus anemone

G. Vauquelin, P. Vanderheyden, F. Fierens, 2003, Fundamental & clinical pharmacology.

Deglycosylated mammalian beta 2-adrenergic receptors are still able to undergo functional coupling to Ns.

G. Vauquelin, Y. Severne, R. Jurss, 1986, Biochemical pharmacology.

Biological screening of selected medicinal Panamanian plants by radioligand-binding techniques.

C. Caballero-George, G. Vauquelin, L. Pieters, 2001, Phytomedicine : international journal of phytotherapy and phytopharmacology.

Agonist-mediated conformational changes of muscarinic receptors in rat brain.

A. Strosberg, G. Vauquelin, P. Laduron, 1982, European journal of biochemistry.

How can the differences among AT1-receptor antagonists Be explained?

G. Vauquelin, P. Morsing, 2007, Cell Biochemistry and Biophysics.

Distinctions between non-peptide angiotensin II AT1-receptor antagonists

G. Vauquelin, P. Vanderheyden, F. Fierens, 2001, Journal of the renin-angiotensin-aldosterone system : JRAAS.

What intracranial tissues in humans contain sumatriptan-sensitive serotonin 5-HT1-type receptors?

N. Wilczak, G. Vauquelin, J. Keyser, 1993, Neuroscience Letters.

Different agonist binding properties of M1 and M2 muscarinic receptors in calf brain cortex membranes.

G. Vauquelin, G. Ebinger, P. Vanderheyden, 1987, Biochemical pharmacology.

Desensitization of alpha 2-adrenergic receptors in NG 108 15 cells by (-)-adrenaline and phorbol 12-myristate 13-acetate.

G. Vauquelin, A. Convents, J. De Backer, 1989, The Biochemical journal.

Identification of I1 and I2 Imidazoline Receptors in Striatum Membranes from Different Speciesa

G. Vauquelin, A. Flamez, P. Ladure, 1999, Annals of the New York Academy of Sciences.

Identification and characterization of imidazoline-binding sites from calf striatum.

G. Vauquelin, A. Flamez, E. Czerwiec, 1996, European journal of pharmacology.

Non-competitive binding of the nonpeptide antagonist BIBP3226 to rat forebrain neuropeptide Y1 receptors.

G. Vauquelin, P. Vanderheyden, I. Van Liefde, 1997, European journal of pharmacology.

Coupling of D1 dopamine receptors to the guanine nucleotide binding protein Gs is deficient in Huntington's disease

G. Vauquelin, J. Keyser, G. Ebinger, 1989, Brain Research.

Identification of D1-like dopamine receptors on human blood platelets.

J. De Keyser, G. Vauquelin, A. Convents, 1988, Life sciences.

Agonist/N-ethylmaleimide mediated inactivation of beta-adrenergic receptors. Molecular aspects.

G. Vauquelin, Y. Severne, C. Wemers, 1985, Biochemical pharmacology.

Imidazoline receptors, non-adrenergic idazoxan binding sites and α2-adrenoceptors in the human central nervous system

G. Vauquelin, J. Keyser, G. Bricca, 1994, Neuroscience.

Autoradiographic distribution of α 2 adrenoceptors, NAIBS, and 5-HT1A receptors in human brain using [3H]idazoxan and [3H]rauwolscine

G. Vauquelin, A. Convents, J. Keyser, 1991, Brain Research.

Molecular distinction between calf heart and brain muscarine receptors: different N-ethylmaleimide modulation of agonist binding.

G. Vauquelin, P. Vanderheyden, L. Kanarek, 1986, European Journal of Pharmacology.

Simplified models for heterobivalent ligand binding: when are they applicable and which are the factors that affect their target residence time

G. Vauquelin, 2013, Naunyn-Schmiedeberg's Archives of Pharmacology.

Characterization with [3H] dihydroergocryptine of the alpha-adrenergic receptor of the hepatic plasma membrane. Comparison with the beta-adrenergic receptor in normal and adrenalectomized rats.

G. Guellaen, J. Hanoune, G. Vauquelin, 1978, The Journal of biological chemistry.

Visualization of the turkey erythrocyte β‐adrenergic receptor

A. Strosberg, G. Vauquelin, O. Durieu-Trautmann, 1980 .

Manganese and copper promote the binding of dopamine to “serotonin binding proteins” in bovine frontal cortex

C. Velez-Pardo, G. Vauquelin, G. Ebinger, 1995, Neurochemistry International.

Interaction of serotonin- and dopamine-related neurotoxins with "serotonin binding proteins" in bovine frontal cortex.

M. Jiménez Del Río, G. Vauquelin, G. Ebinger, 1994, Biochemical pharmacology.

Binding of serotonin and dopamine to 'serotonin binding proteins' in bovine frontal cortex: evidence for iron-induced oxidative mechanisms.

M. Jiménez Del Río, G. Vauquelin, G. Ebinger, 1993, European journal of pharmacology.

The In Vitro Binding Properties of Non-Peptide AT1 Receptor Antagonists

G. Vauquelin, I. Verheijen, Vanderheyden Pml, 2002 .

Synergistic inhibition of the enzymatic activity of aminopeptidase N by divalent metal ion chelators

G. Vauquelin, P. Vanderheyden, L. Vogel, 2006, Fundamental & clinical pharmacology.

Epinephrine and norepinephrine stimulation of adenylate cyclase in bovine retina homogenate: evidence for interaction with the dopamine D1 receptor.

G. Vauquelin, G. Ebinger, P. Vanderheyden, 1986, Life sciences.

[3H]SCH 23390 labels a novel 5-hydroxytryptamine binding site in human blood platelet membranes.

J. De Keyser, G. Vauquelin, A. Convents, 1989, European journal of pharmacology.

Adenosine-1 active ligands: cirsimarin, a flavone glycoside from Microtea debilis.

M. Claeys, G. Vauquelin, L. Pieters, 1997, Journal of natural products.

The effect of aging on the D1 dopamine receptors in human frontal cortex

G. Vauquelin, J. Keyser, G. Ebinger, 1990, Brain Research.

Amino triazolo diazepines (Ata) as constrained histidine mimics.

G. Vauquelin, D. Tourwé, P. Vanderheyden, 2011, Organic letters.

Identification of Drug-Like Inhibitors of Insulin-Regulated Aminopeptidase Through Small-Molecule Screening.

K. Sigmundsson, T. Lundbäck, G. Vauquelin, 2016, Assay and drug development technologies.

Potent macrocyclic inhibitors of insulin-regulated aminopeptidase (IRAP) by olefin ring-closing metathesis.

A. Hallberg, G. Lindeberg, A. Karlén, 2011, Journal of medicinal chemistry.

Disulfide cyclized tripeptide analogues of angiotensin IV as potent and selective inhibitors of insulin-regulated aminopeptidase (IRAP).

A. Hallberg, G. Lindeberg, A. Karlén, 2010, Journal of medicinal chemistry.

Endogenous cystinyl aminopeptidase in Chinese hamster ovary cells: characterization by [125I]Ang IV binding and catalytic activity.

Veerle Kersemans, Minh Tam Le, Patrick Vanderheyden, 2004, Biochemical pharmacology.

Tazolol (1-isopropylamino-3-(2-thiazoloxy)-2-propanol) as a beta-adrenergic blocker.

A. Strosberg, G. Guellaen, J. Hanoune, 1976, Biochemical pharmacology.

Monoamine and iron-related toxicity: from "serotonin-binding proteins" to lipid peroxidation and apoptosis in PC12 cells.

C. Velez-Pardo, G. Vauquelin, G. Ebinger, 1998, General pharmacology.

Serotonin-binding proteins in the bovine cerebral cortex: interaction with serotonin and catecholamines.

M. Jiménez Del Río, G. Vauquelin, G. Ebinger, 1992, European journal of pharmacology.

Dopamine and iron induce apoptosis in PC12 cells.

H. Verschueren, C. Velez-Pardo, M. Jiménez Del Río, 1997, Pharmacology & toxicology.

Redox cycling activity of monoamine-serotonin binding protein conjugates.

C. Velez-Pardo, M. Jiménez Del Río, G. Vauquelin, 1996, Biochemical pharmacology.

Fe(2+)-mediated binding of serotonin and dopamine to skeletal muscle actin: resemblance to serotonin binding proteins.

M. Jiménez Del Río, G. Vauquelin, G. Ebinger, 1995, European journal of pharmacology.

Effects of target binding kinetics on in vivo drug efficacy: koff, kon and rebinding

G. Vauquelin, 2016, British journal of pharmacology.

Autoradiographic localization of D1 and D2 dopamine receptors in the human brain

Frank Roels, G. Vauquelin, J. Keyser, 1988, Neuroscience Letters.

Inhibitory Activity on Binding of Specific Ligands to the Human Angiotensin II AT1 and Endothelin 1 ETA Receptors: Bioactive Benzo[c]phenanthridine Alkaloids from the Root of Bocconia frutescens

C. Caballero-George, M. Claeys, S. Apers, 2002, Planta medica.

Screening of medicinal plants from Suriname for 5-HT(1A) ligands: Bioactive isoquinoline alkaloids from the fruit of Annona muricata.

G. Vauquelin, L. Pieters, A. Vlietinck, 1997, Phytomedicine : international journal of phytotherapy and phytopharmacology.

Isoquinoline Derivatives Isolated from the Fruit of Annona muricata as 5‐HTergic 5‐HT1A Receptor Agonists in Rats: Unexploited Antidepressive (Lead) Products

G. Vauquelin, A. Vlietinck, T. Bruyne, 1997, The Journal of pharmacy and pharmacology.

Evaluation of bioactive saponins and triterpenoidal aglycons for their binding properties on human endothelin ETA and angiotensin AT1 receptors

Mahabir P. Gupta, C. Caballero-George, T. Masaki, 2004, Phytotherapy research : PTR.

Ligands, their receptors and … plasma membranes

G. Vauquelin, A. Packeu, 2009, Molecular and Cellular Endocrinology.

Melanosome binding and oxidation-reduction properties of synthetic L-dopa-melanin as in vitro tests for drug toxicity.

A. IJzerman, G. Vauquelin, I. Debing, 1988, Molecular pharmacology.

Evidence for essential disulfide bonds in beta1-adrenergic receptors of turkey erythrocyte membranes. Inactivation by dithiothreitol.

A. Strosberg, G. Vauquelin, L. Kanarek, 1979, The Journal of biological chemistry.

Human M1-, M2- and M3-muscarinic cholinergic receptors: Binding characteristics of agonists and antagonists

Patrick Vanderheyden, J. Gies, G. Vauquelin, 1990, Journal of the Neurological Sciences.

Characterization of M1- and M2-muscarinic receptors in calf retina membranes

G. Vauquelin, G. Ebinger, P. Vanderheyden, 1988, Vision Research.

Muscarinic cholinergic receptor subtypes in normal human brain and Alzheimer's presenile dementia

G. Vauquelin, G. Vauquelin, R. Dierckx, 1987, Journal of the Neurological Sciences.

Fluxes for Unraveling Complex Binding Mechanisms.

D. Maes, D. Swinney, G. Vauquelin, 2020, Trends in pharmacological sciences.

On the different experimental manifestations of two‐state ‘induced‐fit’ binding of drugs to their cellular targets

D. Swinney, G. Vauquelin, I. Van Liefde, 2016, British journal of pharmacology.

Purification of beta-adrenergic receptors: the search for an adequate affinity adsorbent.

A. Strosberg, J. Hanoune, G. Vauquelin, 1978, Life sciences.

Human neuropeptide YY1 receptors exert unequal control of the extracellular acidification rate in different cell lines.

G. Vauquelin, P. Vanderheyden, I. Van Liefde, 1998, European journal of pharmacology.

Corticotropin-releasing factor receptors induce calcium mobilization through cross-talk with Gq-coupled receptors.

G. Vauquelin, F. Dautzenberg, E. Gutknecht, 2010, European journal of pharmacology.

Mechanisms of PDZ domain scaffold assembly illuminated by use of supported cell membrane sheets

K. L. Martinez, K. Teilum, U. Gether, 2018, eLife.

Myometrial β1-Adrenoreceptors Are Detectable Only in the Midfollicular Phase*

G. Vauquelin, J. Lescrainier, S. Bottari, 1986 .

Differential muscarinic receptor binding of acetylcholinesterase inhibitors in rat brain, human brain and Chinese hamster ovary cells expressing human receptors.

G. Vauquelin, M. Oortgiesen, P. Vanderheyden, 1997, The Journal of pharmacology and experimental therapeutics.

Selective masking of M1-receptors in calf retina membranes by the venom of the marine snail Conus tessulatus

G. Vauquelin, E. Czerwiec, W. Potter, 1993, Neurochemistry International.

Conus venom interaction with α2-adrenergic receptors in calf retina membranes

G. Vauquelin, A. Convents, E. Czerwiec, 1989, Neurochemistry International.

Agonist mediated conformational changes of solubilized calf forebrain muscarinic acetylcholine receptors.

G. Vauquelin, P. Vanderheyden, J. De Backer, 1984, Biochemical pharmacology.

The venom of Conus pennaceus inhibits the binding of [3H]neuropeptide Y by direct interaction with the radioligand

G. Vauquelin, P. Vanderheyden, B. Diallo, 1998, Neurochemistry International.

NEUROPEPTIDE Y RECEPTORS FROM CALF BRAIN: EFFECT OF CRUDE CONUS VENOM PREPARATIONS ON [3H]NPY BINDING

G. Vauquelin, P. Vanderheyden, E. Czerwiec, 1996, Neurochemistry International.

High-affinity binding of [3H]neuropeptide Y to a polypeptide from the venom of Conus anemone.

G. Vauquelin, P. Vanderheyden, E. Czerwiec, 1996, European journal of pharmacology.

[3H]rauwolscine behaves as an agonist for the 5-HT1A receptors in human frontal cortex membranes.

G. Vauquelin, E. Czerwiec, J. De Backer, 1991, European journal of pharmacology.

Tight agonist binding may prevent the correct interpretation of agonist competition binding curves for alpha 2-adrenergic receptors.

G. Vauquelin, A. Convents, D. Convents, 1987, Molecular pharmacology.

Identification of M2 muscarinic receptors in membranes from bovine cerebral basal arteries.

G. Vauquelin, G. Ebinger, P. Vanderheyden, 1986, Life sciences.

Purification of muscarinic acetylcholine receptors by affinity chromatography.

A. Strosberg, G. Vauquelin, P. Vanderheyden, 1983, The EMBO journal.

Arginine and cysteine residues in the ligand binding site of alpha 2-adrenergic receptors.

G. Vauquelin, S. Bottari, A. Vokaer, 1985, Life sciences.

Identification and characterization of alpha 2-adrenergic receptors in human myometrium by [3H]rauwolscine binding.

G. Vauquelin, J. Lescrainier, S. Bottari, 1983, American journal of obstetrics and gynecology.

Regulation of alpha- and beta-adrenergic receptor subclasses by gonadal steroids in human myometrium.

G. Vauquelin, J. Lescrainier, S. Bottari, 1985, Acta physiologica Hungarica.

Identification and characterization of alpha 1-adrenergic receptors in human myometrium by [3H]prazosin binding.

G. Vauquelin, J. Lescrainier, S. Bottari, 1983, Biochemical pharmacology.

Regional distribution of the dopamine D2 receptors in the mesotelencephalic dopamine neuron system of human brain

G. Vauquelin, J. Keyser, G. Ebinger, 1985, Journal of the Neurological Sciences.

Angiotensin IV displays only low affinity for native insulin‐regulated aminopeptidase (IRAP)

G. Vauquelin, D. Tourwé, G. Tóth, 2012, Fundamental & clinical pharmacology.

[3H]Clozapine is not a suitable radioligand for the labelling of D4 dopamine receptors in postmortem human brain

N. Wilczak, G. Vauquelin, A. Flamez, 1994, Neuroscience Letters.

Elusive equilibrium: the challenge of interpreting receptor pharmacology using calcium assays

S. Charlton, G. Vauquelin, Georges Vauquelin, 2010, British journal of pharmacology.

Affinity chromatography of the beta-adrenergic receptor from turkey erythrocytes.

A. Strosberg, J. Hanoune, G. Vauquelin, 1979, European journal of biochemistry.

125I-Tyr0-hCRH Labelling characteristics of corticotropin-releasing hormone receptors: differences between normal and adenomatous corticotrophs

G. Vauquelin, A. Beckers, R. Abs, 1997, Neurochemistry International.

Insulin‐like growth factor‐I receptors in human brain and pituitary gland: An autoradiographic study

N. Wilczak, J. De Keyser, G. Vauquelin, 1994, Synapse.

Medicinal plants in Suriname: screening of plant extracts for receptorbinding activity.

G. Vauquelin, A. Vlietinck, J. De Backer, 1997, Phytomedicine : international journal of phytotherapy and phytopharmacology.

Kinetic versus allosteric mechanisms to explain insurmountable antagonism and delayed ligand dissociation

G. Vauquelin, A. Szczuka, 2007, Neurochemistry International.

Long-lasting angiotensin type 1 receptor binding and protection by candesartan: comparison with other biphenyl-tetrazole sartans

G. Vauquelin, Georges Vauquelin, Isabelle Van Liefde, 2006, Journal of hypertension. Supplement : official journal of the International Society of Hypertension.

G protein‐coupled receptors: a count of 1001 conformations

G. Vauquelin, I. Van Liefde, I. Liefde, 2005, Fundamental & clinical pharmacology.

The production and characterization of antibodies against β-adrenergic antagonists

A. Strosberg, J. Hoebeke, G. Vauquelin, 1978 .

Small potent ligands to the insulin‐regulated aminopeptidase (IRAP)/AT4 receptor

G. Lindeberg, A. Karlén, G. Vauquelin, 2007, Journal of peptide science : an official publication of the European Peptide Society.

Involvement of the AT1 receptor subtype in the effects of angiotensin IV and LVV‐haemorphin 7 on hippocampal neurotransmitter levels and spatial working memory

Y. Michotte, G. Vauquelin, V. Caveliers, 2010, Journal of neurochemistry.

Radioligand dissociation measurements: potential interference of rebinding and allosteric mechanisms and physiological relevance of the biological model systems

G. Vauquelin, I. Van Liefde, 2012, Expert opinion on drug discovery.

Clozapine, atypical antipsychotics, and the benefits of fast-off D2 dopamine receptor antagonism

P. Seeman, G. Vauquelin, Sophie Bostoen, 2012, Naunyn-Schmiedeberg's Archives of Pharmacology.

Long‐lasting target binding and rebinding as mechanisms to prolong in vivo drug action

S. Charlton, G. Vauquelin, Georges Vauquelin, 2010, British journal of pharmacology.

Myometrial beta 1-adrenoreceptors are detectable only in the midfollicular phase.

J. Roberts, G. Vauquelin, J. Lescrainier, 1986, The Journal of clinical endocrinology and metabolism.

Competition in drug binding and … the race to equilibrium

D. Maes, G. Vauquelin, 2022, Fundamental & clinical pharmacology.

Induced fit versus conformational selection: From rate constants to fluxes… and back to rate constants

D. Maes, G. Vauquelin, 2021, Pharmacology research & perspectives.

Distinct in vivo target occupancy by bivalent‐ and induced‐fit‐like binding drugs

G. Vauquelin, 2017, British journal of pharmacology.

On the ‘micro’-pharmacodynamic and pharmacokinetic mechanisms that contribute to long-lasting drug action

G. Vauquelin, Georges Vauquelin, 2015, Expert opinion on drug discovery.

Antagonist‐D2S‐dopamine receptors interactions in intact Chinese recombinant ovary cells

G. Vauquelin, A. Packeu, J. De Backer, 2009, Fundamental & clinical pharmacology.

Link between a high k on for drug binding and a fast clinical action: to be or not to be?

G. Vauquelin, 2018, MedChemComm.

Cell membranes… and how long drugs may exert beneficial pharmacological activity in vivo

G. Vauquelin, Georges Vauquelin, 2016, British journal of clinical pharmacology.

Experimental Methods to Determine Binding Kinetics

D. Swinney, W. Huber, G. Vauquelin, 2015 .

Antagonist-radioligand binding to D2L-receptors in intact cells.

G. Vauquelin, P. Vanderheyden, A. Packeu, 2008, Biochemical pharmacology.

Efaroxan (RX 821037) is a potent and selective α 2-adrenoceptor antagonist in human frontal cortex membranes

G. Vauquelin, J. Backer, H. Vos, 1991, Neurochemistry International.

Pharmacological characterization of I1 and I2 imidazoline receptors in human striatum

G. Vauquelin, A. Flamez, E. Czerwiec, 1997, Neurochemistry International.

Identification of a D1 dopamine receptor, not linked to adenylate cyclase, on lactotroph cells

A. Dupont, L. Vanhaelst, B. Velkeniers, 1991, British journal of pharmacology.

Towards the chemical and functional characterization of the β-adrenergic receptor

A. Strosberg, G. Vauquelin, S. Bottari, 1980 .

THE NOVEL ALPHA2-ADRENOCEPTOR AGONIST [3H]MIVAZEROL BINDS TO NON-ADRENERGIC BINDING SITES IN HUMAN STRIATUM MEMBRANES THAT ARE DISTINCT FROM IMIDAZOLINE RECEPTORS

G. Vauquelin, A. Flamez, M. Gillard, 1997, Neurochemistry International.

Isolation of adenylate cyclase-free, beta-adrenergic receptor from turkey erythrocyte membranes by affinity chromatography.

A. Strosberg, J. Hanoune, G. Vauquelin, 1977, Proceedings of the National Academy of Sciences of the United States of America.

[3H]GBR 12935 Binding to Dopamine Uptake Sites in the Human Brain

G. Vauquelin, J. Keyser, G. Ebinger, 1989, Journal of neurochemistry.

Inhibition of Angiotensin II-Induced Inositol Phosphate Production by Triacid Nonpeptide Antagonists in CHO Cells Expressing Human AT1 Receptors

G. Vauquelin, P. Vanderheyden, F. Fierens, 2000, Pharmaceutical Research.

Binding characteristics of [3H]-irbesartan to human recombinant angiotensin type 1 receptors

G. Vauquelin, P. Vanderheyden, J. De Backer, 2000, Journal of the renin-angiotensin-aldosterone system : JRAAS.

Binding of the antagonist [3H]candesartan to angiotensin II AT1 receptor-transfected [correction of tranfected] Chinese hamster ovary cells.

G. Vauquelin, P. Vanderheyden, J. De Backer, 1999, European journal of pharmacology.

In vitro inhibition of [3H]-angiotensin II binding on the human AT1 receptor by proanthocyanidins from Guazuma ulmifolia bark.

Mahabir P. Gupta, C. Caballero-George, M. Claeys, 2002, Planta medica.

Cyclic AMP content and invasive capacity of metastatic variants of the BW-5147 murine T-cell lymphoma.

H. Verschueren, P. De Baetselier, G. Vauquelin, 1990, Life Science.

Dual effect of N-ethylmaleimide on agonist binding to bovine heart muscarinic receptors.

G. Vauquelin, G. Ebinger, P. Vanderheyden, 1990, Archives internationales de pharmacodynamie et de therapie.

The Role of Binding Kinetics in GPCR Drug Discovery.

D. Swinney, G. Vauquelin, Brad A. Haubrich, 2015, Current topics in medicinal chemistry.

Glycoprotein nature of α2‐adrenergic receptors labeled with p‐azido[3H] clonidine in calf retina membranes

G. Vauquelin, A. Convents, D. Convents, 1988, FEBS Letters.

Angiotensin AT4 receptor ligand interaction with cystinyl aminopeptidase and aminopeptidase N: [125I]Angiotensin IV only binds to the cystinyl aminopeptidase apo-enzyme.

Minh Tam Le, Patrick Vanderheyden, Yvette Michotte, 2006, European journal of pharmacology.

Evidence for a widespread dopaminergic innervation of the human cerebral neocortex

G. Vauquelin, J. Keyser, G. Ebinger, 1989, Neuroscience Letters.

Metal ion modulation of cystinyl aminopeptidase.

Y. Michotte, V. Kersemans, G. Vauquelin, 2005, The Biochemical journal.

(±)Tetrahydroanisocycline and (±)tetrahydropalmatine binding to D1 and D2 dopaminergic receptors in human putamen

G. Vauquelin, J. Keyser, M. Vanhaelen, 1989, Neurochemistry International.

Lys 199 mutation of the human angiotensin type 1 receptor differentially affects the binding of surmountable and insurmountable non-peptide antagonists

A. IJzerman, L. Hunyady, G. Vauquelin, 2000, Journal of the renin-angiotensin-aldosterone system : JRAAS.

D1 dopamine receptors in human putamen, frontal cortex and calf retina: differences in guanine nucleotide regulation of agonist binding and adenylate cyclase stimulation

G. Vauquelin, R. Dierckx, J. Keyser, 1988, Brain Research.

Autoradiographic distribution of D3-type dopamine receptors in human brain using [3H]7-hydroxy-N,N-di-n-propyl-2-aminotetralin

G. Vauquelin, N. Wilczak, G. Vauquelin, 1994, Brain Research.

AT1 receptor antagonists.

G. Vauquelin, P. Vanderheyden, J. De Backer, 2004, Current Medicinal Chemistry - Cardiovascular & Hematological Agents.

The replacement of His(4) in angiotensin IV by conformationally constrained residues provides highly potent and selective analogues.

G. Vauquelin, D. Tourwé, P. Vanderheyden, 2009, Journal of medicinal chemistry.

Radioligand binding to intact cells as a tool for extended drug screening in a representative physiological context.

D. Swinney, G. Vauquelin, I. Van Liefde, 2015, Drug discovery today. Technologies.

Insurmountable AT1 receptor antagonism: fitting models with experimental data

G. Vauquelin, Frederik FierensIlse, VerheijenPatrick Vanderheyden, 2001 .

Binding of the antagonist []candesartan to angiotensin II AT1 receptor-tranfected Chinese hamster ovary cells

G. Vauquelin, P. Vanderheyden, F. Fierens, 1999 .

Competition between induced fit- and conformational selection binding: how different flux-based approaches help clarifying their interplay

D. Maes, G. Vauquelin, 2023, bioRxiv.

Non‐competitive interaction between raclopride and spiperone on human D2L‐receptors in intact Chinese hamster ovary cells

G. Vauquelin, A. Packeu, J. De Backer, 2009, Fundamental & clinical pharmacology.

Tight binding of the angiotensin AT(1) receptor antagonist.

G. Vauquelin, P. Vanderheyden, T. Thekkumkara, 2001, Biochemical Pharmacology.

D2 dopamine receptors in the human brain: heterogeneity based on differences in guanine nucleotide effect on agonist binding, and their presence on corticostriatal nerve terminals

G. Vauquelin, J. Keyser, G. Ebinger, 1989, Brain Research.

A two-state model of antagonist-AT1 receptor interaction: further support by binding studies at low temperature.

G. Vauquelin, P. Vanderheyden, J. De Backer, 2003, Biochemical pharmacology.

Exploring avidity: understanding the potential gains in functional affinity and target residence time of bivalent and heterobivalent ligands

S. Charlton, G. Vauquelin, 2013, British journal of pharmacology.