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Items: 1 to 50 of 90

1.

Affinity, binding kinetics and functional characterization of draflazine analogues for human equilibrative nucleoside transporter 1 (SLC29A1).

Vlachodimou A, Konstantinopoulou K, IJzerman AP, Heitman LH.

Biochem Pharmacol. 2020 Feb;172:113747. doi: 10.1016/j.bcp.2019.113747. Epub 2019 Dec 10.

2.

Synthesis and Pharmacological Evaluation of Triazolopyrimidinone Derivatives as Noncompetitive, Intracellular Antagonists for CC Chemokine Receptors 2 and 5.

Ortiz Zacarías NV, van Veldhoven JPD, den Hollander LS, Dogan B, Openy J, Hsiao YY, Lenselink EB, Heitman LH, IJzerman AP.

J Med Chem. 2019 Dec 26;62(24):11035-11053. doi: 10.1021/acs.jmedchem.9b00742. Epub 2019 Dec 13.

3.

Label-free detection of transporter activity via GPCR signalling in living cells: A case for SLC29A1, the equilibrative nucleoside transporter 1.

Vlachodimou A, IJzerman AP, Heitman LH.

Sci Rep. 2019 Sep 24;9(1):13802. doi: 10.1038/s41598-019-48829-3.

4.

LUF7244, an allosteric modulator/activator of Kv 11.1 channels, counteracts dofetilide-induced torsades de pointes arrhythmia in the chronic atrioventricular block dog model.

Qile M, Beekman HDM, Sprenkeler DJ, Houtman MJC, van Ham WB, Stary-Weinzinger A, Beyl S, Hering S, van den Berg DJ, de Lange ECM, Heitman LH, IJzerman AP, Vos MA, van der Heyden MAG.

Br J Pharmacol. 2019 Oct;176(19):3871-3885. doi: 10.1111/bph.14798. Epub 2019 Aug 30.

5.

A live cell NanoBRET binding assay allows the study of ligand-binding kinetics to the adenosine A3 receptor.

Bouzo-Lorenzo M, Stoddart LA, Xia L, IJzerman AP, Heitman LH, Briddon SJ, Hill SJ.

Purinergic Signal. 2019 Jun;15(2):139-153. doi: 10.1007/s11302-019-09650-9. Epub 2019 Mar 27.

6.

Long residence time adenosine A1 receptor agonists produce sustained wash-resistant antilipolytic effect in rat adipocytes.

Yun Y, Chen J, Liu R, Chen W, Liu C, Wang R, Hou Z, Yu Z, Sun Y, IJzerman AP, Heitman LH, Yin X, Guo D.

Biochem Pharmacol. 2019 Jun;164:45-52. doi: 10.1016/j.bcp.2019.03.032. Epub 2019 Mar 21.

PMID:
30905656
7.

Development of Covalent Ligands for G Protein-Coupled Receptors: A Case for the Human Adenosine A3 Receptor.

Yang X, van Veldhoven JPD, Offringa J, Kuiper BJ, Lenselink EB, Heitman LH, van der Es D, IJzerman AP.

J Med Chem. 2019 Apr 11;62(7):3539-3552. doi: 10.1021/acs.jmedchem.8b02026. Epub 2019 Mar 28.

8.

Label-free impedance-based whole cell assay to study GPCR pharmacology.

Doornbos MLJ, Heitman LH.

Methods Cell Biol. 2019;149:179-194. doi: 10.1016/bs.mcb.2018.08.003. Epub 2018 Sep 11.

PMID:
30616818
9.

Pyrrolone Derivatives as Intracellular Allosteric Modulators for Chemokine Receptors: Selective and Dual-Targeting Inhibitors of CC Chemokine Receptors 1 and 2.

Ortiz Zacarías NV, van Veldhoven JPD, Portner L, van Spronsen E, Ullo S, Veenhuizen M, van der Velden WJC, Zweemer AJM, Kreekel RM, Oenema K, Lenselink EB, Heitman LH, IJzerman AP.

J Med Chem. 2018 Oct 25;61(20):9146-9161. doi: 10.1021/acs.jmedchem.8b00605. Epub 2018 Oct 11.

10.

Bioisosteric replacement of central 1,2,4-oxadiazole ring of high affinity CB2 ligands by regioisomeric 1,3,4-oxadiazole ring.

Heimann D, Lueg C, de Vries H, Frehland B, Schepmann D, Heitman LH, Wünsch B.

Medchemcomm. 2017 Jul 19;8(8):1697-1705. doi: 10.1039/c7md00296c. eCollection 2017 Aug 1.

11.

An Affinity-Based Probe for the Human Adenosine A2A Receptor.

Yang X, Michiels TJM, de Jong C, Soethoudt M, Dekker N, Gordon E, van der Stelt M, Heitman LH, van der Es D, IJzerman AP.

J Med Chem. 2018 Sep 13;61(17):7892-7901. doi: 10.1021/acs.jmedchem.8b00860. Epub 2018 Aug 21.

12.

Impact of allosteric modulation: Exploring the binding kinetics of glutamate and other orthosteric ligands of the metabotropic glutamate receptor 2.

Doornbos MLJ, Vermond SC, Lavreysen H, Tresadern G, IJzerman AP, Heitman LH.

Biochem Pharmacol. 2018 Sep;155:356-365. doi: 10.1016/j.bcp.2018.07.014. Epub 2018 Jul 17.

13.

Development of a Cannabinoid-Based Photoaffinity Probe to Determine the Δ8/9-Tetrahydrocannabinol Protein Interaction Landscape in Neuroblastoma Cells.

Soethoudt M, Alachouzos G, van Rooden EJ, Moya-Garzón MD, van den Berg RJBHN, Heitman LH, van der Stelt M.

Cannabis Cannabinoid Res. 2018 Jul 1;3(1):136-151. doi: 10.1089/can.2018.0003. eCollection 2018.

14.

Intracellular Receptor Modulation: Novel Approach to Target GPCRs.

Ortiz Zacarías NV, Lenselink EB, IJzerman AP, Handel TM, Heitman LH.

Trends Pharmacol Sci. 2018 Jun;39(6):547-559. doi: 10.1016/j.tips.2018.03.002. Epub 2018 Apr 10. Review.

PMID:
29653834
15.

Constitutive activity of the metabotropic glutamate receptor 2 explored with a whole-cell label-free biosensor.

Doornbos MLJ, Van der Linden I, Vereyken L, Tresadern G, IJzerman AP, Lavreysen H, Heitman LH.

Biochem Pharmacol. 2018 Jun;152:201-210. doi: 10.1016/j.bcp.2018.03.026. Epub 2018 Mar 30.

16.

Structure-kinetic relationship studies of cannabinoid CB2 receptor agonists reveal substituent-specific lipophilic effects on residence time.

Soethoudt M, Hoorens MWH, Doelman W, Martella A, van der Stelt M, Heitman LH.

Biochem Pharmacol. 2018 Jun;152:129-142. doi: 10.1016/j.bcp.2018.03.018. Epub 2018 Mar 21.

17.

Covalent Allosteric Probe for the Metabotropic Glutamate Receptor 2: Design, Synthesis, and Pharmacological Characterization.

Doornbos MLJ, Wang X, Vermond SC, Peeters L, Pérez-Benito L, Trabanco AA, Lavreysen H, Cid JM, Heitman LH, Tresadern G, IJzerman AP.

J Med Chem. 2019 Jan 10;62(1):223-233. doi: 10.1021/acs.jmedchem.8b00051. Epub 2018 Mar 7.

18.

A two-state model for the kinetics of competitive radioligand binding.

Guo D, Peletier LA, Bridge L, Keur W, de Vries H, Zweemer A, Heitman LH, IJzerman AP.

Br J Pharmacol. 2018 May;175(10):1719-1730. doi: 10.1111/bph.14184. Epub 2018 Apr 17.

19.

Selective Photoaffinity Probe That Enables Assessment of Cannabinoid CB2 Receptor Expression and Ligand Engagement in Human Cells.

Soethoudt M, Stolze SC, Westphal MV, van Stralen L, Martella A, van Rooden EJ, Guba W, Varga ZV, Deng H, van Kasteren SI, Grether U, IJzerman AP, Pacher P, Carreira EM, Overkleeft HS, Ioan-Facsinay A, Heitman LH, van der Stelt M.

J Am Chem Soc. 2018 May 16;140(19):6067-6075. doi: 10.1021/jacs.7b11281. Epub 2018 Feb 16.

20.

Optimization of the metabolic stability of a fluorinated cannabinoid receptor subtype 2 (CB2) ligand designed for PET studies.

Heimann D, Börgel F, de Vries H, Patberg M, Jan-Smith E, Frehland B, Schepmann D, Heitman LH, Wünsch B.

Eur J Med Chem. 2018 Feb 25;146:409-422. doi: 10.1016/j.ejmech.2018.01.048. Epub 2018 Jan 31.

PMID:
29407967
21.

A binding kinetics study of human adenosine A3 receptor agonists.

Xia L, Kyrizaki A, Tosh DK, van Duijl TT, Roorda JC, Jacobson KA, IJzerman AP, Heitman LH.

Biochem Pharmacol. 2018 Jul;153:248-259. doi: 10.1016/j.bcp.2017.12.026. Epub 2018 Jan 3.

22.

Structural Mapping of Adenosine Receptor Mutations: Ligand Binding and Signaling Mechanisms.

Jespers W, Schiedel AC, Heitman LH, Cooke RM, Kleene L, van Westen GJP, Gloriam DE, Müller CE, Sotelo E, Gutiérrez-de-Terán H.

Trends Pharmacol Sci. 2018 Jan;39(1):75-89. doi: 10.1016/j.tips.2017.11.001. Epub 2017 Dec 5. Review.

PMID:
29203139
23.

Optimization of pharmacokinetic properties by modification of a carbazole-based cannabinoid receptor subtype 2 (CB2) ligand.

Heimann D, Börgel F, de Vries H, Bachmann K, Rose VE, Frehland B, Schepmann D, Heitman LH, Wünsch B.

Eur J Med Chem. 2018 Jan 1;143:1436-1447. doi: 10.1016/j.ejmech.2017.10.049. Epub 2017 Oct 16.

PMID:
29126730
24.

Structure-Affinity Relationships and Structure-Kinetic Relationships of 1,2-Diarylimidazol-4-carboxamide Derivatives as Human Cannabinoid 1 Receptor Antagonists.

Xia L, de Vries H, Lenselink EB, Louvel J, Waring MJ, Cheng L, Pahlén S, Petersson MJ, Schell P, Olsson RI, Heitman LH, Sheppard RJ, IJzerman AP.

J Med Chem. 2017 Dec 14;60(23):9545-9564. doi: 10.1021/acs.jmedchem.7b00861. Epub 2017 Nov 21.

25.

Kinetics of human cannabinoid 1 (CB1) receptor antagonists: Structure-kinetics relationships (SKR) and implications for insurmountable antagonism.

Xia L, de Vries H, Yang X, Lenselink EB, Kyrizaki A, Barth F, Louvel J, Dreyer MK, van der Es D, IJzerman AP, Heitman LH.

Biochem Pharmacol. 2018 May;151:166-179. doi: 10.1016/j.bcp.2017.10.014. Epub 2017 Nov 2.

26.

From receptor binding kinetics to signal transduction; a missing link in predicting in vivo drug-action.

Nederpelt I, Kuzikov M, de Witte WEA, Schnider P, Tuijt B, Gul S, IJzerman AP, de Lange ECM, Heitman LH.

Sci Rep. 2017 Oct 26;7(1):14169. doi: 10.1038/s41598-017-14257-4.

27.

Structure-Affinity Relationships and Structure-Kinetics Relationships of Pyrido[2,1-f]purine-2,4-dione Derivatives as Human Adenosine A3 Receptor Antagonists.

Xia L, Burger WAC, van Veldhoven JPD, Kuiper BJ, van Duijl TT, Lenselink EB, Paasman E, Heitman LH, IJzerman AP.

J Med Chem. 2017 Sep 14;60(17):7555-7568. doi: 10.1021/acs.jmedchem.7b00950. Epub 2017 Aug 30.

28.

Label-free technology and patient cells: from early drug development to precision medicine.

Hillger JM, Lieuw WL, Heitman LH, IJzerman AP.

Drug Discov Today. 2017 Dec;22(12):1808-1815. doi: 10.1016/j.drudis.2017.07.015. Epub 2017 Aug 1. Review.

29.

A Novel Selective Inverse Agonist of the CB2 Receptor as a Radiolabeled Tool Compound for Kinetic Binding Studies.

Martella A, Sijben H, Rufer AC, Grether U, Fingerle J, Ullmer C, Hartung T, IJzerman AP, van der Stelt M, Heitman LH.

Mol Pharmacol. 2017 Oct;92(4):389-400. doi: 10.1124/mol.117.108605. Epub 2017 Jul 26.

PMID:
28747489
30.

Discovery and Kinetic Profiling of 7-Aryl-1,2,4-triazolo[4,3-a]pyridines: Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 2.

Doornbos MLJ, Cid JM, Haubrich J, Nunes A, van de Sande JW, Vermond SC, Mulder-Krieger T, Trabanco AA, Ahnaou A, Drinkenburg WH, Lavreysen H, Heitman LH, IJzerman AP, Tresadern G.

J Med Chem. 2017 Aug 10;60(15):6704-6720. doi: 10.1021/acs.jmedchem.7b00669. Epub 2017 Aug 1.

PMID:
28704052
31.

Synthesis and biological evaluation of chemokine receptor ligands with 2-benzazepine scaffold.

Thum S, Kokornaczyk AK, Seki T, De Maria M, Ortiz Zacarias NV, de Vries H, Weiss C, Koch M, Schepmann D, Kitamura M, Tschammer N, Heitman LH, Junker A, Wünsch B.

Eur J Med Chem. 2017 Jul 28;135:401-413. doi: 10.1016/j.ejmech.2017.04.046. Epub 2017 Apr 22.

PMID:
28463783
32.

Kinetics for Drug Discovery: an industry-driven effort to target drug residence time.

Schuetz DA, de Witte WEA, Wong YC, Knasmueller B, Richter L, Kokh DB, Sadiq SK, Bosma R, Nederpelt I, Heitman LH, Segala E, Amaral M, Guo D, Andres D, Georgi V, Stoddart LA, Hill S, Cooke RM, De Graaf C, Leurs R, Frech M, Wade RC, de Lange ECM, IJzerman AP, Müller-Fahrnow A, Ecker GF.

Drug Discov Today. 2017 Jun;22(6):896-911. doi: 10.1016/j.drudis.2017.02.002. Epub 2017 Apr 13. Review.

PMID:
28412474
33.

A novel CCR2 antagonist inhibits atherogenesis in apoE deficient mice by achieving high receptor occupancy.

Bot I, Ortiz Zacarías NV, de Witte WE, de Vries H, van Santbrink PJ, van der Velden D, Kröner MJ, van der Berg DJ, Stamos D, de Lange EC, Kuiper J, IJzerman AP, Heitman LH.

Sci Rep. 2017 Mar 3;7(1):52. doi: 10.1038/s41598-017-00104-z.

34.

Phenotypic screening of cannabinoid receptor 2 ligands shows different sensitivity to genotype.

Hillger JM, le Roy B, Wang Z, Mulder-Krieger T, Boomsma DI, Slagboom PE, Danen EHJ, IJzerman AP, Heitman LH.

Biochem Pharmacol. 2017 Apr 15;130:60-70. doi: 10.1016/j.bcp.2017.01.014. Epub 2017 Jan 31.

35.

Cannabinoid CB2 receptor ligand profiling reveals biased signalling and off-target activity.

Soethoudt M, Grether U, Fingerle J, Grim TW, Fezza F, de Petrocellis L, Ullmer C, Rothenhäusler B, Perret C, van Gils N, Finlay D, MacDonald C, Chicca A, Gens MD, Stuart J, de Vries H, Mastrangelo N, Xia L, Alachouzos G, Baggelaar MP, Martella A, Mock ED, Deng H, Heitman LH, Connor M, Di Marzo V, Gertsch J, Lichtman AH, Maccarrone M, Pacher P, Glass M, van der Stelt M.

Nat Commun. 2017 Jan 3;8:13958. doi: 10.1038/ncomms13958.

36.

Structure of CC chemokine receptor 2 with orthosteric and allosteric antagonists.

Zheng Y, Qin L, Zacarías NV, de Vries H, Han GW, Gustavsson M, Dabros M, Zhao C, Cherney RJ, Carter P, Stamos D, Abagyan R, Cherezov V, Stevens RC, IJzerman AP, Heitman LH, Tebben A, Kufareva I, Handel TM.

Nature. 2016 Dec 15;540(7633):458-461. doi: 10.1038/nature20605. Epub 2016 Dec 7.

37.

Kinetic Profile of Neuropeptide-Receptor Interactions.

Nederpelt I, Bunnik J, IJzerman AP, Heitman LH.

Trends Neurosci. 2016 Dec;39(12):830-839. doi: 10.1016/j.tins.2016.09.008. Epub 2016 Oct 25. Review.

PMID:
27793433
38.

The Added Value of Assessing Ligand-Receptor Binding Kinetics in Drug Discovery.

Guo D, Heitman LH, IJzerman AP.

ACS Med Chem Lett. 2016 Aug 19;7(9):819-21. doi: 10.1021/acsmedchemlett.6b00273. eCollection 2016 Sep 8.

39.

Kinetic binding and activation profiles of endogenous tachykinins targeting the NK1 receptor.

Nederpelt I, Bleeker D, Tuijt B, IJzerman AP, Heitman LH.

Biochem Pharmacol. 2016 Oct 15;118:88-95. doi: 10.1016/j.bcp.2016.08.004. Epub 2016 Aug 5.

PMID:
27501920
40.

Controlling the Dissociation of Ligands from the Adenosine A2A Receptor through Modulation of Salt Bridge Strength.

Segala E, Guo D, Cheng RK, Bortolato A, Deflorian F, Doré AS, Errey JC, Heitman LH, IJzerman AP, Marshall FH, Cooke RM.

J Med Chem. 2016 Jul 14;59(13):6470-9. doi: 10.1021/acs.jmedchem.6b00653. Epub 2016 Jul 1.

PMID:
27312113
41.

Getting personal: Endogenous adenosine receptor signaling in lymphoblastoid cell lines.

Hillger JM, Diehl C, van Spronsen E, Boomsma DI, Slagboom PE, Heitman LH, IJzerman AP.

Biochem Pharmacol. 2016 Sep 1;115:114-22. doi: 10.1016/j.bcp.2016.06.006. Epub 2016 Jun 11.

PMID:
27297283
42.

Protocol to Study β-Arrestin Recruitment by CB1 and CB2 Cannabinoid Receptors.

Soethoudt M, van Gils N, van der Stelt M, Heitman LH.

Methods Mol Biol. 2016;1412:103-11. doi: 10.1007/978-1-4939-3539-0_11.

PMID:
27245896
43.

Kinetic Aspects of the Interaction between Ligand and G Protein-Coupled Receptor: The Case of the Adenosine Receptors.

Guo D, Heitman LH, IJzerman AP.

Chem Rev. 2017 Jan 11;117(1):38-66. doi: 10.1021/acs.chemrev.6b00025. Epub 2016 Apr 18.

PMID:
27088232
44.

Allosteric Modulation of Kv11.1 (hERG) Channels Protects Against Drug-Induced Ventricular Arrhythmias.

Yu Z, Liu J, van Veldhoven JP, IJzerman AP, Schalij MJ, Pijnappels DA, Heitman LH, de Vries AA.

Circ Arrhythm Electrophysiol. 2016 Apr;9(4):e003439. doi: 10.1161/CIRCEP.115.003439.

PMID:
27071825
45.

Equilibrium and kinetic selectivity profiling on the human adenosine receptors.

Guo D, Dijksteel GS, van Duijl T, Heezen M, Heitman LH, IJzerman AP.

Biochem Pharmacol. 2016 Apr 1;105:34-41. doi: 10.1016/j.bcp.2016.02.018. Epub 2016 Feb 27.

PMID:
26930564
46.

Molecular Basis of Ligand Dissociation from the Adenosine A2A Receptor.

Guo D, Pan AC, Dror RO, Mocking T, Liu R, Heitman LH, Shaw DE, IJzerman AP.

Mol Pharmacol. 2016 May;89(5):485-91. doi: 10.1124/mol.115.102657. Epub 2016 Feb 12.

PMID:
26873858
47.

Persistent GnRH receptor activation in pituitary αT3-1 cells analyzed with a label-free technology.

Nederpelt I, Vergroesen RD, IJzerman AP, Heitman LH.

Biosens Bioelectron. 2016 May 15;79:721-7. doi: 10.1016/j.bios.2015.12.066. Epub 2015 Dec 21.

PMID:
26774084
48.

Scintillation proximity assay (SPA) as a new approach to determine a ligand's kinetic profile. A case in point for the adenosine A1 receptor.

Xia L, de Vries H, IJzerman AP, Heitman LH.

Purinergic Signal. 2016 Mar;12(1):115-26. doi: 10.1007/s11302-015-9485-0. Epub 2015 Dec 9.

49.

Molecular mechanism of positive allosteric modulation of the metabotropic glutamate receptor 2 by JNJ-46281222.

Doornbos ML, Pérez-Benito L, Tresadern G, Mulder-Krieger T, Biesmans I, Trabanco AA, Cid JM, Lavreysen H, IJzerman AP, Heitman LH.

Br J Pharmacol. 2016 Feb;173(3):588-600. doi: 10.1111/bph.13390. Epub 2016 Jan 13.

50.

Synthesis and biological evaluation of negative allosteric modulators of the Kv11.1(hERG) channel.

Yu Z, van Veldhoven JP, 't Hart IM, Kopf AH, Heitman LH, IJzerman AP.

Eur J Med Chem. 2015 Dec 1;106:50-9. doi: 10.1016/j.ejmech.2015.10.032. Epub 2015 Oct 21.

PMID:
26519929

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