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Items: 1 to 50 of 232

1.

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

Erlendsson S, Thorsen TS, Vauquelin G, Ammendrup-Johnsen I, Wirth V, Martinez KL, Teilum K, Gether U, Madsen KL.

Elife. 2019 Jan 3;8. pii: e39180. doi: 10.7554/eLife.39180.

2.

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

Vauquelin G.

Medchemcomm. 2018 Aug 16;9(9):1426-1438. doi: 10.1039/c8md00296g. eCollection 2018 Sep 1. Review.

3.

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

Vauquelin G.

Br J Pharmacol. 2017 Dec;174(23):4233-4246. doi: 10.1111/bph.13989. Epub 2017 Oct 18.

4.

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

de Witte WEA, Vauquelin G, van der Graaf PH, de Lange ECM.

Eur J Pharm Sci. 2017 Nov 15;109S:S83-S89. doi: 10.1016/j.ejps.2017.05.024. Epub 2017 May 12.

5.

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

Vauquelin G.

Br J Clin Pharmacol. 2016 Sep;82(3):673-82. doi: 10.1111/bcp.12996. Epub 2016 May 29. Review.

6.

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

Vauquelin G.

Br J Pharmacol. 2016 Aug;173(15):2319-34. doi: 10.1111/bph.13504. Epub 2016 Jul 4.

7.

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

Engen K, Rosenström U, Axelsson H, Konda V, Dahllund L, Otrocka M, Sigmundsson K, Nikolaou A, Vauquelin G, Hallberg M, Jenmalm Jensen A, Lundbäck T, Larhed M.

Assay Drug Dev Technol. 2016 Apr;14(3):180-93. doi: 10.1089/adt.2016.708.

PMID:
27078680
8.

On the different experimental manifestations of two-state 'induced-fit' binding of drugs to their cellular targets.

Vauquelin G, Van Liefde I, Swinney DC.

Br J Pharmacol. 2016 Apr;173(8):1268-85. doi: 10.1111/bph.13445. Epub 2016 Mar 15. Review.

9.

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

Vauquelin G, Van Liefde I, Swinney DC.

Drug Discov Today Technol. 2015 Oct;17:28-34. doi: 10.1016/j.ddtec.2015.09.001. Epub 2015 Oct 23. Review.

PMID:
26724334
10.

On the 'micro'-pharmacodynamic and pharmacokinetic mechanisms that contribute to long-lasting drug action.

Vauquelin G.

Expert Opin Drug Discov. 2015 Oct;10(10):1085-98. doi: 10.1517/17460441.2015.1067196. Epub 2015 Jul 13. Review.

PMID:
26165720
11.

The Role of Binding Kinetics in GPCR Drug Discovery.

Swinney DC, Haubrich BA, Van Liefde I, Vauquelin G.

Curr Top Med Chem. 2015;15(24):2504-22. Review.

PMID:
26126905
12.

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

Vauquelin G, Hall D, Charlton SJ.

Br J Pharmacol. 2015 May;172(9):2300-15. doi: 10.1111/bph.13053. Epub 2015 Mar 17.

13.

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

Guo D, Venhorst SN, Massink A, van Veldhoven JP, Vauquelin G, IJzerman AP, Heitman LH.

Br J Pharmacol. 2014 Dec;171(23):5295-312. doi: 10.1111/bph.12836. Epub 2014 Sep 5.

14.

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

Swinney DC, Beavis P, Chuang KT, Zheng Y, Lee I, Gee P, Deval J, Rotstein DM, Dioszegi M, Ravendran P, Zhang J, Sankuratri S, Kondru R, Vauquelin G.

Br J Pharmacol. 2014 Jul;171(14):3364-75. doi: 10.1111/bph.12683.

15.

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

Vauquelin G, Bricca G, Van Liefde I.

Fundam Clin Pharmacol. 2014 Oct;28(5):530-43. doi: 10.1111/fcp.12052. Epub 2013 Nov 4.

PMID:
24118041
16.

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

Vauquelin G.

Naunyn Schmiedebergs Arch Pharmacol. 2013 Nov;386(11):949-62. doi: 10.1007/s00210-013-0881-0. Epub 2013 Jun 28.

PMID:
23812645
17.

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

Nikolaou A, Van den Eynde I, Tourwé D, Vauquelin G, Tóth G, Mallareddy JR, Poglitsch M, Van Ginderachter JA, Vanderheyden PM.

Eur J Pharmacol. 2013 Feb 28;702(1-3):93-102. doi: 10.1016/j.ejphar.2013.01.026. Epub 2013 Jan 31.

PMID:
23376157
18.
19.

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

Vauquelin G, Van Liefde I.

Expert Opin Drug Discov. 2012 Jul;7(7):583-95. doi: 10.1517/17460441.2012.687720. Epub 2012 Jun 1. Review.

PMID:
22650795
20.

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

Vauquelin G, Bostoen S, Vanderheyden P, Seeman P.

Naunyn Schmiedebergs Arch Pharmacol. 2012 Apr;385(4):337-72. doi: 10.1007/s00210-012-0734-2. Epub 2012 Feb 14. Review.

PMID:
22331262
21.

Amino triazolo diazepines (Ata) as constrained histidine mimics.

Buysse K, Farard J, Nikolaou A, Vanderheyden P, Vauquelin G, Pedersen DS, Tourwé D, Ballet S.

Org Lett. 2011 Dec 16;13(24):6468-71. doi: 10.1021/ol202767k. Epub 2011 Nov 16.

PMID:
22087642
22.

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

Lukaszuk A, Demaegdt H, Van den Eynde I, Vanderheyden P, Vauquelin G, Tourwé D.

J Pept Sci. 2011 Aug;17(8):545-53. doi: 10.1002/psc.1365. Epub 2011 Apr 28.

PMID:
21538707
23.

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

Demaegdt H, De Backer JP, Lukaszuk A, Tóth G, Szemenyei E, Tourwé D, Vauquelin G.

Fundam Clin Pharmacol. 2012 Apr;26(2):194-7. doi: 10.1111/j.1472-8206.2011.00948.x. Epub 2011 Apr 11.

PMID:
21477268
24.

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

Andersson H, Demaegdt H, Johnsson A, Vauquelin G, Lindeberg G, Hallberg M, Erdelyi M, Karlen A, Hallberg A.

J Med Chem. 2011 Jun 9;54(11):3779-92. doi: 10.1021/jm200036n. Epub 2011 May 9.

PMID:
21476495
25.

Pressor and renal hemodynamic effects of the novel angiotensin A peptide are angiotensin II type 1A receptor dependent.

Yang R, Smolders I, Vanderheyden P, Demaegdt H, Van Eeckhaut A, Vauquelin G, Lukaszuk A, Tourwé D, Chai SY, Albiston AL, Nahmias C, Walther T, Dupont AG.

Hypertension. 2011 May;57(5):956-64. doi: 10.1161/HYPERTENSIONAHA.110.161836. Epub 2011 Apr 4.

PMID:
21464395
26.

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

Demaegdt H, Gard P, De Backer JP, Lukaszuk A, Szemenyei E, Tóth G, Tourwé D, Vauquelin G.

Mol Cell Endocrinol. 2011 Jun 6;339(1-2):34-44. doi: 10.1016/j.mce.2011.03.005. Epub 2011 Mar 30.

PMID:
21457753
27.

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

Andersson H, Demaegdt H, Vauquelin G, Lindeberg G, Karlén A, Hallberg M, Erdélyi M, Hallberg A.

J Med Chem. 2010 Nov 25;53(22):8059-71. doi: 10.1021/jm100793t. Epub 2010 Nov 3.

PMID:
21047126
28.

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

Charlton SJ, Vauquelin G.

Br J Pharmacol. 2010 Nov;161(6):1250-65. doi: 10.1111/j.1476-5381.2010.00863.x. Review.

29.

Estimation of the dissociation rate of unlabelled ligand-receptor complexes by a 'two-step' competition binding approach.

Packeu A, Wennerberg M, Balendran A, Vauquelin G.

Br J Pharmacol. 2010 Nov;161(6):1311-28. doi: 10.1111/j.1476-5381.2010.00931.x.

30.

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

Vauquelin G, Charlton SJ.

Br J Pharmacol. 2010 Oct;161(3):488-508. doi: 10.1111/j.1476-5381.2010.00936.x. Review.

31.

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

Vauquelin G.

Expert Opin Drug Discov. 2010 Oct;5(10):927-41. doi: 10.1517/17460441.2010.512037. Epub 2010 Aug 17.

PMID:
22823988
32.

Binding properties of antagonists to cannabinoid receptors in intact cells.

Wennerberg M, Cheng L, Hjorth S, Clapham JC, Balendran A, Vauquelin G.

Fundam Clin Pharmacol. 2011 Apr;25(2):200-10. doi: 10.1111/j.1472-8206.2010.00843.x.

PMID:
20608998
33.

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

Gutknecht E, Vauquelin G, Dautzenberg FM.

Eur J Pharmacol. 2010 Sep 10;642(1-3):1-9. doi: 10.1016/j.ejphar.2010.05.027. Epub 2010 Jun 8.

PMID:
20594969
34.

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

Rondou P, Skieterska K, Packeu A, Lintermans B, Vanhoenacker P, Vauquelin G, Haegeman G, Van Craenenbroeck K.

Cell Signal. 2010 Jun;22(6):900-13. doi: 10.1016/j.cellsig.2010.01.014. Epub 2010 Jan 25.

PMID:
20100572
35.

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

De Bundel D, Demaegdt H, Lahoutte T, Caveliers V, Kersemans K, Ceulemans AG, Vauquelin G, Clinckers R, Vanderheyden P, Michotte Y, Smolders I.

J Neurochem. 2010 Mar;112(5):1223-34. doi: 10.1111/j.1471-4159.2009.06547.x. Epub 2009 Dec 17.

36.

Antagonist-D2S-dopamine receptor interactions in intact recombinant Chinese hamster ovary cells [corrected].

Packeu A, Béghin T, De Backer JP, Vauquelin G.

Fundam Clin Pharmacol. 2010 Jun;24(3):293-303. doi: 10.1111/j.1472-8206.2009.00777.x. Epub 2009 Dec 9. Erratum in: Fundam Clin Pharmacol. 2010 Aug;24(4):531.

PMID:
20015228
37.

Non-competitive interaction between raclopride and spiperone on human D-receptors in intact Chinese hamster ovary cells.

Packeu A, De Backer JP, Vauquelin G.

Fundam Clin Pharmacol. 2010 Jun;24(3):283-91. doi: 10.1111/j.1472-8206.2009.00793.x. Epub 2009 Nov 10.

PMID:
19909349
38.

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

Lukaszuk A, Demaegdt H, Feytens D, Vanderheyden P, Vauquelin G, Tourwé D.

J Med Chem. 2009 Sep 24;52(18):5612-8. doi: 10.1021/jm900651p.

PMID:
19757839
39.

Unravelling the complex dissociation of [(3)H]-rimonabant from plated CB(1) cannabinoid receptor-expressing cells.

Wennerberg M, Balendran A, Clapham JC, Vauquelin G.

Fundam Clin Pharmacol. 2010 Apr;24(2):181-7. doi: 10.1111/j.1472-8206.2009.00756.x. Epub 2009 Aug 21.

PMID:
19702692
40.

Ligands, their receptors and ... plasma membranes.

Vauquelin G, Packeu A.

Mol Cell Endocrinol. 2009 Nov 13;311(1-2):1-10. doi: 10.1016/j.mce.2009.07.022. Epub 2009 Jul 30. Review.

PMID:
19647036
41.

Selective labeling of IRAP by the tritiated AT(4) receptor ligand [3H]Angiotensin IV and its stable analog [3H]AL-11.

Demaegdt H, Lukaszuk A, De Buyser E, De Backer JP, Szemenyei E, Tóth G, Chakravarthy S, Panicker M, Michotte Y, Tourwé D, Vauquelin G.

Mol Cell Endocrinol. 2009 Nov 13;311(1-2):77-86. doi: 10.1016/j.mce.2009.07.020. Epub 2009 Jul 28.

PMID:
19643163
42.

Molecular mechanisms for the persistent bronchodilatory effect of the beta 2-adrenoceptor agonist salmeterol.

Szczuka A, Wennerberg M, Packeu A, Vauquelin G.

Br J Pharmacol. 2009 Sep;158(1):183-94. doi: 10.1111/j.1476-5381.2009.00296.x. Epub 2009 Jul 7.

43.

Molecular mechanisms of corticotropin-releasing factor receptor-induced calcium signaling.

Gutknecht E, Van der Linden I, Van Kolen K, Verhoeven KF, Vauquelin G, Dautzenberg FM.

Mol Pharmacol. 2009 Mar;75(3):648-57. doi: 10.1124/mol.108.050427. Epub 2008 Dec 19.

PMID:
19098121
44.

Sartan-AT1 receptor interactions: in vitro evidence for insurmountable antagonism and inverse agonism.

Van Liefde I, Vauquelin G.

Mol Cell Endocrinol. 2009 Apr 29;302(2):237-43. doi: 10.1016/j.mce.2008.06.006. Epub 2008 Jun 21. Review.

PMID:
18620019
45.

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

Andersson H, Demaegdt H, Vauquelin G, Lindeberg G, Karlén A, Hallberg M.

Bioorg Med Chem. 2008 Jul 15;16(14):6924-35. doi: 10.1016/j.bmc.2008.05.046. Epub 2008 May 27.

PMID:
18556208
46.

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

Demaegdt H, Smitz L, De Backer JP, Le MT, Bauwens M, Szemenyei E, Tóth G, Michotte Y, Vanderheyden P, Vauquelin G.

Br J Pharmacol. 2008 Jun;154(4):872-81. doi: 10.1038/bjp.2008.117. Epub 2008 Apr 21.

47.

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

Packeu A, De Backer JP, Van Liefde I, Vanderheyden PM, Vauquelin G.

Biochem Pharmacol. 2008 Jun 1;75(11):2192-203. doi: 10.1016/j.bcp.2008.03.001. Epub 2008 Mar 14.

PMID:
18436192
48.

Beta-homo-amino acid scan of angiotensin IV.

Lukaszuk A, Demaegdt H, Szemenyei E, Tóth G, Tymecka D, Misicka A, Karoyan P, Vanderheyden P, Vauquelin G, Tourwé D.

J Med Chem. 2008 Apr 10;51(7):2291-6. doi: 10.1021/jm701490g. Epub 2008 Mar 15.

PMID:
18386881
49.

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

Stragier B, De Bundel D, Sarre S, Smolders I, Vauquelin G, Dupont A, Michotte Y, Vanderheyden P.

Heart Fail Rev. 2008 Sep;13(3):321-37. Epub 2007 Nov 8. Review.

PMID:
17990104
50.

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