Works by Heitman, Laura H.

Results: 43

A monoacylglycerol lipase inhibitor showing therapeutic efficacy in mice without central side effects or dependence.

Published in:

Nature Communications, 2023, v. 14, n. 1, p. 1, doi. 10.1038/s41467-023-43606-3

By:

Jiang, Ming;
Huizenga, Mirjam C. W.;
Wirt, Jonah L.;
Paloczi, Janos;
Amedi, Avand;
van den Berg, Richard J. B. H. N.;
Benz, Joerg;
Collin, Ludovic;
Deng, Hui;
Di, Xinyu;
Driever, Wouter F.;
Florea, Bogdan I.;
Grether, Uwe;
Janssen, Antonius P. A.;
Hankemeier, Thomas;
Heitman, Laura H.;
Lam, Tsang-Wai;
Mohr, Florian;
Pavlovic, Anto;
Ruf, Iris

Publication type:

Article

A multiple classifier system identifies novel cannabinoid CB2 receptor ligands.

Published in:

Journal of Cheminformatics, 2019, v. 11, n. 1, p. N.PAG, doi. 10.1186/s13321-019-0389-9

By:

Ruano-Ordás, David;
Burggraaff, Lindsey;
Liu, Rongfang;
van der Horst, Cas;
Heitman, Laura H.;
Emmerich, Michael T. M.;
Mendez, Jose R.;
Yevseyeva, Iryna;
van Westen, Gerard J. P.

Publication type:

Article

Pharmacological characterization of allosteric modulators: A case for chemokine receptors.

Published in:

Medicinal Research Reviews, 2024, v. 44, n. 5, p. 2291, doi. 10.1002/med.22043

By:

den Hollander, Lisa S.;
IJzerman, Adriaan P.;
Heitman, Laura H.

Publication type:

Article

Cancer-Associated Mutations of the Adenosine A 2A Receptor Have Diverse Influences on Ligand Binding and Receptor Functions.

Published in:

Molecules, 2022, v. 27, n. 15, p. 4676, doi. 10.3390/molecules27154676

By:

Feng, Chenlin;
Wang, Xuesong;
Jespers, Willem;
Liu, Rongfang;
Zamarbide Losada, Sofía Denise;
Gorostiola González, Marina;
van Westen, Gerard J. P.;
Danen, Erik H. J.;
Heitman, Laura H.

Publication type:

Article

Cancer-Related Somatic Mutations in Transmembrane Helices Alter Adenosine A1 Receptor Pharmacology.

Published in:

Molecules, 2022, v. 27, n. 12, p. 3742, doi. 10.3390/molecules27123742

By:

Wang, Xuesong;
Jespers, Willem;
Wolff, Kim A. N.;
Buytelaar, Jill;
IJzerman, Adriaan P.;
van Westen, Gerard J. P.;
Heitman, Laura H.

Publication type:

Article

Development of Bicyclo[3.1.0]hexane-Based A 3 Receptor Ligands: Closing the Gaps in the Structure–Affinity Relationships.

Published in:

Molecules, 2022, v. 27, n. 7, p. 2283, doi. 10.3390/molecules27072283

By:

Lemmerhirt, Jan Phillip;
Isaak, Andreas;
Liu, Rongfang;
Kock, Max;
Daniliuc, Constantin G.;
Jacobson, Kenneth A.;
Heitman, Laura H.;
Junker, Anna

Publication type:

Article

Label-free high-throughput screening assay for the identification of norepinephrine transporter (NET/SLC6A2) inhibitors.

Published in:

Scientific Reports, 2021, v. 11, n. 1, p. 1, doi. 10.1038/s41598-021-91700-7

By:

Sijben, Hubert J.;
van Oostveen, Wieke M.;
Hartog, Peter B. R.;
Stucchi, Laura;
Rossignoli, Andrea;
Maresca, Giovanna;
Scarabottolo, Lia;
IJzerman, Adriaan P.;
Heitman, Laura H.

Publication type:

Article

A study of the dopamine transporter using the TRACT assay, a novel in vitro tool for solute carrier drug discovery.

Published in:

Scientific Reports, 2021, v. 10, n. 1, p. 1, doi. 10.1038/s41598-020-79218-w

By:

Sijben, Hubert J.;
van den Berg, Julie J. E.;
Broekhuis, Jeremy D.;
IJzerman, Adriaan P.;
Heitman, Laura H.

Publication type:

Article

3DDPDs: describing protein dynamics for proteochemometric bioactivity prediction. A case for (mutant) G protein-coupled receptors.

Published in:

Journal of Cheminformatics, 2023, v. 15, n. 1, p. 1, doi. 10.1186/s13321-023-00745-5

By:

Gorostiola González, Marina;
van den Broek, Remco L.;
Braun, Thomas G. M.;
Chatzopoulou, Magdalini;
Jespers, Willem;
IJzerman, Adriaan P.;
Heitman, Laura H.;
van Westen, Gerard J. P.

Publication type:

Article

The 17th EFMC Short Course on Medicinal Chemistry on Small Molecule Protein Degraders.

Published in:

ChemMedChem, 2023, v. 18, n. 20, p. 1, doi. 10.1002/cmdc.202300464

By:

Ciulli, Alessio;
O'Connor, Suzanne;
Chung, Chun‐Wa;
Hartung, Ingo V.;
Testa, Andrea;
Daniels, Danette L.;
Heitman, Laura H.

Publication type:

Article

Development of the First Potential Nonpeptidic Positron Emission Tomography Tracer for the Imaging of CCR2 Receptors.

Published in:

ChemMedChem, 2021, v. 16, n. 4, p. 640, doi. 10.1002/cmdc.202000728

By:

Wagner, Stefan;
Moura Gatti, Fernando;
Silva, Daniel G.;
Ortiz Zacarias, Natalia V.;
Zweemer, Annelien J. M.;
Hermann, Sven;
De Maria, Monica;
Koch, Michael;
Weiss, Christina;
Schepmann, Dirk;
Heitman, Laura H.;
Tschammer, Nuska;
Kopka, Klaus;
Junker, Anna

Publication type:

Article

Discovery of a Photoaffinity Probe that Captures the Active Conformation of the Cannabinoid CB2 Receptor.

Published in:

ChemBioChem, 2024, v. 25, n. 7, p. 1, doi. 10.1002/cbic.202300785

By:

De Paus, Laura V.;
An, Yu;
Janssen, Antonius P. A.;
van den Berg, Richard J. B. H. N.;
Heitman, Laura H.;
van der Stelt, Mario

Publication type:

Article

Impedance-Based Phenotypic Readout of Transporter Function: A Case for Glutamate Transporters.

Published in:

Frontiers in Pharmacology, 2022, v. 13, p. 1, doi. 10.3389/fphar.2022.872335

By:

Sijben, Hubert J.;
Dall' Acqua, Laura;
Liu, Rongfang;
Jarret, Abigail;
Christodoulaki, Eirini;
Onstein, Svenja;
Wolf, Gernot;
Verburgt, Simone J.;
Le Dévédec, Sylvia E.;
Wiedmer, Tabea;
Superti-Furga, Giulio;
IJzerman, Adriaan P.;
Heitman, Laura H.

Publication type:

Article

The Role of Target Binding Kinetics in Drug Discovery.

Published in:

ChemMedChem, 2015, v. 10, n. 11, p. 1793, doi. 10.1002/cmdc.201500310

By:

Guo, Dong;
Heitman, Laura H.;
IJzerman, Adriaan P.

Publication type:

Article

Evaluation of (4-Arylpiperidin-1-yl)cyclopentanecarboxamides As High-Affinity and Long-Residence-Time Antagonists for the CCR2 Receptor.

Published in:

ChemMedChem, 2015, v. 10, n. 7, p. 1249, doi. 10.1002/cmdc.201500058

By:

Vilums, Maris;
Zweemer, Annelien J. M.;
Dilanchian, Arian;
van Veldhoven, Jacobus P. D.;
de Vries, Henk;
Brussee, Johannes;
Saunders, John;
Stamos, Dean;
Heitman, Laura H.;
IJzerman, Adriaan P.

Publication type:

Article

Binding Kinetics of ZM241385 Derivatives at the Human Adenosine A2A Receptor.

Published in:

ChemMedChem, 2014, v. 9, n. 4, p. 752, doi. 10.1002/cmdc.201300474

By:

Guo, Dong;
Xia, Lizi;
van Veldhoven, Jacobus P. D.;
Hazeu, Marc;
Mocking, Tamara;
Brussee, Johannes;
IJzerman, Adriaan P.;
Heitman, Laura H.

Publication type:

Article

Discovery of Selective Luteinizing Hormone Receptor Agonists Using the Bivalent Ligand Method.

Published in:

ChemMedChem, 2009, v. 4, n. 7, p. 1189, doi. 10.1002/cmdc.200900058

By:

Bonger, Kimberly M.;
van den Berg, Richard J. B. H. N.;
Knijnenburg, Annemiek D.;
Heitman, Laura H.;
van Koppen, Chris J.;
Timmers, Cornelis M.;
Overkleeft, Herman S.;
van der Marel, Gijsbert A.

Publication type:

Article

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

Published in:

Scientific Reports, 2019, v. 9, n. 1, p. N.PAG, doi. 10.1038/s41598-019-48829-3

By:

Vlachodimou, Anna;
IJzerman, Adriaan P.;
Heitman, Laura H.

Publication type:

Article

An Overview of Cell-Based Assay Platforms for the Solute Carrier Family of Transporters.

Published in:

Frontiers in Pharmacology, 2021, v. 12, p. 1, doi. 10.3389/fphar.2021.722889

By:

Dvorak, Vojtech;
Wiedmer, Tabea;
Ingles-Prieto, Alvaro;
Altermatt, Patrick;
Batoulis, Helena;
Bärenz, Felix;
Bender, Eckhard;
Digles, Daniela;
Dürrenberger, Franz;
Heitman, Laura H.;
IJzerman, Adriaan P.;
Kell, Douglas B.;
Kickinger, Stefanie;
Körzö, Daniel;
Leippe, Philipp;
Licher, Thomas;
Manolova, Vania;
Rizzetto, Riccardo;
Sassone, Francesca;
Scarabottolo, Lia

Publication type:

Article

Allosteric modulation, thermodynamics and binding to wild-type and mutant (T277A) adenosine A1 receptors of LUF5831, a novel nonadenosine-like agonist.

Published in:

2006

By:

Heitman, Laura H.;
Mulder-Krieger, Thea;
Spanjersberg, Ronald F.;
von Frijtag Drabbe Künzel, Jacobien K.;
Dalpiaz, Alessandro;
IJzerman, Adriaan P.;
von Frijtag Drabbe Künzel, Jacobien K

Publication type:

journal article

Identification of V6.51L as a selectivity hotspot in stereoselective A2B adenosine receptor antagonist recognition.

Published in:

Scientific Reports, 2021, v. 11, n. 1, p. 1, doi. 10.1038/s41598-021-93419-x

By:

Wang, Xuesong;
Jespers, Willem;
Prieto-Díaz, Rubén;
Majellaro, Maria;
IJzerman, Adriaan P.;
van Westen, Gerard J. P.;
Sotelo, Eddy;
Heitman, Laura H.;
Gutiérrez-de-Terán, Hugo

Publication type:

Article

Mechanistic models enable the rational use of in vitro drug-target binding kinetics for better drug effects in patients.

Published in:

Expert Opinion on Drug Discovery, 2016, v. 11, n. 1, p. 45, doi. 10.1517/17460441.2016.1100163

By:

de Witte, Wilhelmus EA;
Wong, Yin Cheong;
Nederpelt, Indira;
Heitman, Laura H;
Danhof, Meindert;
van der Graaf, Piet H;
Gilissen, Ron AHJ;
de Lange, Elizabeth C.M.

Publication type:

Article

Inducing Receptor Degradation as a Novel Approach to Target CC Chemokine Receptor 2 (CCR2).

Published in:

International Journal of Molecular Sciences, 2024, v. 25, n. 16, p. 8984, doi. 10.3390/ijms25168984

By:

Ortiz Zacarías, Natalia V.;
Röth, Sascha;
Broekhuis, Jeremy D.;
van der Es, Daan;
Moreau, Kevin;
Heitman, Laura H.

Publication type:

Article

Computational Characterization of Membrane Proteins as Anticancer Targets: Current Challenges and Opportunities.

Published in:

International Journal of Molecular Sciences, 2024, v. 25, n. 7, p. 3698, doi. 10.3390/ijms25073698

By:

Gorostiola González, Marina;
Rakers, Pepijn R. J.;
Jespers, Willem;
IJzerman, Adriaan P.;
Heitman, Laura H.;
van Westen, Gerard J. P.

Publication type:

Article

MPP + -Induced Changes in Cellular Impedance as a Measure for Organic Cation Transporter (SLC22A1-3) Activity and Inhibition.

Published in:

International Journal of Molecular Sciences, 2022, v. 23, n. 3, p. 1203, doi. 10.3390/ijms23031203

By:

Mocking, Tamara A. M.;
Sijben, Hubert J.;
Vermeulen, Yimé W.;
IJzerman, Adriaan P.;
Heitman, Laura H.

Publication type:

Article

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

Published in:

2019

By:

Qile, Muge;
Beekman, Henriette D.M.;
Sprenkeler, David J.;
Houtman, Marien J.C.;
Ham, Willem B.;
Stary‐Weinzinger, Anna;
Beyl, Stanislav;
Hering, Steffen;
Berg, Dirk‐Jan;
Lange, Elizabeth C.M.;
Heitman, Laura H.;
IJzerman, Ad P.;
Vos, Marc A.;
Heyden, Marcel A.G.;
van Ham, Willem B;
Stary-Weinzinger, Anna;
van den Berg, Dirk-Jan;
de Lange, Elizabeth C M;
van der Heyden, Marcel A G

Publication type:

journal article

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

Published in:

2018

By:

Guo, Dong;
Peletier, Lambertus A.;
Bridge, Lloyd;
Keur, Wesley;
de Vries, Henk;
Zweemer, Annelien;
Heitman, Laura H.;
IJzerman, Adriaan P.

Publication type:

journal article

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

Published in:

2016

By:

Doornbos, Maarten L J;
Pérez ‐ Benito, Laura;
Tresadern, Gary;
Mulder ‐ Krieger, Thea;
Biesmans, Ilse;
Trabanco, Andrés A;
Cid, Jose María;
Lavreysen, Hilde;
IJzerman, Adriaan P;
Heitman, Laura H;
Pérez-Benito, Laura;
Mulder-Krieger, Thea;
Trabanco, Andrés A;
Cid, Jose María

Publication type:

journal article

Characterization of 12 GnRH peptide agonists - a kinetic perspective.

Published in:

2016

By:

Nederpelt, Indira;
Georgi, Victoria;
Schiele, Felix;
Nowak ‐ Reppel, Katrin;
Fernández ‐ Montalván, Amaury E.;
IJzerman, Adriaan P.;
Heitman, Laura H.;
Nowak-Reppel, Katrin;
Fernández-Montalván, Amaury E

Publication type:

journal article

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

Published in:

2014

By:

Guo, Dong;
Venhorst, Suzanne N;
Massink, Arnault;
van Veldhoven, Jacobus P D;
Vauquelin, Georges;
IJzerman, Adriaan P;
Heitman, Laura H

Publication type:

journal article

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

Published in:

British Journal of Pharmacology, 2014, v. 171, n. 23, p. 5295, doi. 10.1111/bph.12836

By:

Guo, Dong;
Venhorst, Suzanne N;
Massink, Arnault;
Veldhoven, Jacobus P D;
Vauquelin, Georges;
IJzerman, Adriaan P;
Heitman, Laura H

Publication type:

Article

Functional efficacy of adenosine A₂A receptor agonists is positively correlated to their receptor residence time.

Published in:

2012

By:

Guo D;
Mulder-Krieger T;
IJzerman AP;
Heitman LH;
Guo, Dong;
Mulder-Krieger, Thea;
IJzerman, Adriaan P;
Heitman, Laura H

Publication type:

journal article

Functional efficacy of adenosine A2A receptor agonists is positively correlated to their receptor residence time.

Published in:

British Journal of Pharmacology, 2012, v. 166, n. 6, p. 1846, doi. 10.1111/j.1476-5381.2012.01897.x

By:

Guo, Dong;
Mulder-Krieger, Thea;
IJzerman, Adriaan P;
Heitman, Laura H

Publication type:

Article

Deciphering conformational selectivity in the A2A adenosine G protein-coupled receptor by free energy simulations.

Published in:

PLoS Computational Biology, 2021, v. 17, n. 11, p. 1, doi. 10.1371/journal.pcbi.1009152

By:

Jespers, Willem;
Heitman, Laura H.;
IJzerman, Adriaan P.;
Sotelo, Eddy;
van Westen, Gerard J. P.;
Åqvist, Johan;
Gutiérrez-de-Terán, Hugo

Publication type:

Article

A universal cannabinoid CB1 and CB2 receptor TR-FRET kinetic ligand-binding assay.

Published in:

Frontiers in Pharmacology, 2025, p. 1, doi. 10.3389/fphar.2025.1469986

By:

Borrega-Roman, Leire;
Hoare, Bradley L.;
Kosar, Miroslav;
Sarott, Roman C.;
Patej, Kacper J.;
Bouma, Jara;
Scott-Dennis, Morgan;
Koers, Eline J.;
Gazzi, Thais;
Mach, Leonard;
Barrondo, Sergio;
Sallés, Joan;
Guba, Wolfgang;
Kusznir, Eric;
Nazaré, Marc;
Rufer, Arne C.;
Grether, Uwe;
Heitman, Laura H.;
Carreira, Erick M.;
Sykes, David A.

Publication type:

Article

Label-free detection of prostaglandin transporter (SLCO2A1) function and inhibition: insights by wound healing and TRACT assays.

Published in:

Frontiers in Pharmacology, 2024, p. 1, doi. 10.3389/fphar.2024.1372109

By:

Mocking, Tamara A. M.;
van Oostveen, Wieke M.;
van Veldhoven, Jacobus P. D.;
Minnee, Hugo;
Fehres, Cynthia M.;
Whitehurst, Charles E.;
Jzerman, Adriaan P. I.;
Heitman, Laura H.

Publication type:

Article

Indanes-Properties, Preparation, and Presence in Ligands for G Protein Coupled Receptors.

Published in:

Medicinal Research Reviews, 2015, v. 35, n. 6, p. 1097, doi. 10.1002/med.21352

By:

Vilums, Maris;
Heuberger, Jules;
Heitman, Laura H.;
IJzerman, Adriaan P.

Publication type:

Article

Drug-Target Residence Time-A Case for G Protein-Coupled Receptors.

Published in:

Medicinal Research Reviews, 2014, v. 34, n. 4, p. 856, doi. 10.1002/med.21307

By:

Guo, Dong;
Hillger, Julia M.;
IJzerman, Adriaan P.;
Heitman, Laura H.

Publication type:

Article

G protein-coupled receptors of the hypothalamic-pituitary-gonadal axis: A case for gnrh, LH, FSH, and GPR54 receptor ligands.

Published in:

Medicinal Research Reviews, 2008, v. 28, n. 6, p. 975, doi. 10.1002/med.20129

By:

Heitman, Laura H.;
IJzerman, Adriaan P.

Publication type:

Article

Molecular insights into disease-associated glutamate transporter (EAAT1 / SLC1A3) variants using in silico and in vitro approaches.

Published in:

Frontiers in Molecular Biosciences, 2023, p. 1, doi. 10.3389/fmolb.2023.1286673

By:

González, Marina Gorostiola;
Sijben, Hubert J.;
Acqua, Laura Dall';
Rongfang Liu;
IJzerman, Adriaan P.;
Heitman, Laura H.;
van Westen, Gerard J. P.

Publication type:

Article

Enhancing Drug Discovery and Development through the Integration of Medicinal Chemistry, Chemical Biology, and Academia-Industry Partnerships: Insights from Roche's Endocannabinoid System Projects.

Published in:

Chimia, 2024, v. 78, n. 7/8, p. 499, doi. 10.2533/chimia.2024.499

By:

Aebia, Johannes;
Atza, Kenneth;
Ametamey, Simon M.;
Benza, Jörg;
Blaising, Julie;
Butini, Stefania;
Campiani, Giuseppe;
Carreira, Erick M.;
Collin, Ludovic;
de Lago, Eva;
Gazzi, Thais;
Gertsch, Jürg;
Gobbi, Luca;
Guba, Wolfgang;
Fernández-Ruize, Javier;
Fingerle, Jürgen;
Haider, Ahmed;
Yingfang He;
Heitman, Laura H.;
Honer, Michael

Publication type:

Article

Targeting the CCL2–CCR2 axis for atheroprotection.

Published in:

European Heart Journal, 2022, v. 43, n. 19, p. 1799, doi. 10.1093/eurheartj/ehac094

By:

Georgakis, Marios K;
Bernhagen, Jürgen;
Heitman, Laura H;
Weber, Christian;
Dichgans, Martin

Publication type:

Article

Cancer‐related somatic mutations alter adenosine A1 receptor pharmacology—A focus on mutations in the loops and C‐terminus.

Published in:

FASEB Journal, 2022, v. 36, n. 6, p. 1, doi. 10.1096/fj.202200203RR

By:

Wang, Xuesong;
Jespers, Willem;
de Waal, Just J.;
Wolff, Kim A. N.;
van Uden, Liedeke;
IJzerman, Adriaan P.;
van Westen, Gerard J. P.;
Heitman, Laura H.

Publication type:

Article