Laura Heitman
Professor Molecular Pharmacology
- Name
- Prof.dr. L.H. Heitman
- Telephone
- +31 71 527 4558
- l.h.heitman@lacdr.leidenuniv.nl
- ORCID iD
- 0000-0002-1381-8464
Prof. dr. Laura H. Heitman is Professor of Molecular Pharmacology at the Division of Drug Discovery and Safety at the Leiden Academic Centre for Drug Research (LACDR, Leiden University). Moreover, since January 2019 her research group is part of Oncode Institute. Her research interests are mainly focused on understanding and improving drug-receptor interactions, to ultimately make medicines work better. Specifically, she focuses on novel concepts for drug action, such as target binding kinetics and allosteric modulation and studies these on membrane proteins, mostly G protein-coupled receptors (GPCRs). Her research can basically be split in two lines: 1) Intervening with receptor function by small molecules, and 2) Understanding (variant) receptor pharmacology.
More information about Laura Heitman
PhD Candidates
News
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The molecular secrets of medicinal cannabis -
Drug discovery 3.0: more effective and humane -
How Oncode-PACT is bringing new cancer medicines closer with 325 million in Growth Fund money -
Laura Heitman appointed as Professor of Molecular Pharmacology -
A multi-million grant to keep the biological clock healthy -
Laura Heitman uses her expertise to fight cancer -
Laura Heitman nominated for Prix Galien -
Laura Heitman has received two awards at the EFMC-ISMC 2018 -
Profiling programme about body’s own marijuana brings institutes together -
Rethinking drug discovery: Vidi grant for Laura Heitman -
Vidis for nine Leiden researchers -
Two-pronged attack on infectious diseases
Former PhD Candidates
In the Heitman group, different expertise and research domains are combined, such as molecular biology, pharmacology, organic and computational chemistry. They have selected membrane-bound proteins, such as G protein-coupled receptors (GPCRs), as many drugs act via these. Over the years, an array of novel in vitro equilibrium and kinetic binding assays have been developed, as well as (label-free) functional assays to investigate “Novel receptor concepts” to target these membrane proteins, with the ultimate aim to make medicines work better. Examples of such concepts are ‘Allosteric modulation’ and ‘Drug-target binding kinetics’, which can both lead to so-called insurmountable antagonism, i.e. antagonists that cannot be disrupted/counteracted by high local concentrations of the endogenous receptor agonist that is often causal to the disease state. Although many of my projects are in principle ‘disease-agnostic’, her group does have research line around “GPCRs and Cancer”, as it is more and more clear that GPCRs (and their variants) have a role in cancer. To reach her scientific aims, her team collaborates with crystallographers, cell biologists and in vivo pharmacologists, both from academia and pharmaceutical industry.
Prof. Heitman is the recipient of multiple awards, including the ‘2017 MedChemComm Emerging Investigator’-award, runner up for the ‘2018 EFMC Young Medicinal Chemist in Academia’-award and ‘2022 TOPX Female to Follow in Life Sciences-award’. She has obtained several competitive research grants, all allowing her to study these novel, clinically relevant and highly translational concepts for drug action. Specifically, her work is funded by the Dutch Cancer Society (Oncode – for personal excellence), Dutch Organization of Scientific Research (VENI, VIDI – both for personal excellence, NWA-BioClock), Chinese Scholarship Council, EU-Innovative Medicines Initiative (large consortia: K4DD and RESOLUTE), and through collaborations with pharmaceutical industry. Her current research team consists of one assistant professor, 10 PhD students, two Post-Docs and two technicians, and she has successfully graduated 14 PhD students so far, who all have been selected for exciting new positions.
Her research activities have currently led to an authorship on over 120 papers in this field, including one in Science (2012) and one in Nature (2016), where she is first or senior/corresponding author on 40 of these. Currently, her H-index is 38 and the total number of citations is over 5000 (both according to Google Scholar). Moreover, she is a frequently invited speaker (>70 lectures) at conferences in her field (e.g. drug discovery, medicinal chemistry, GPCRs), but also at pharmaceutical companies, universities and knowledge institutes. As a teacher she is active in all years of the bachelor and master Bio-Pharmaceutical Sciences (BPS) and in the master of Pharmacy, all at Leiden University. She is a consultant on molecular pharmacology of GPCRs for several biotech companies. She is a member of several committees and boards, e.g. the Scientific Advisory Board of the Centre for Human Drug Research in Leiden, the Division of Medicinal Chemistry and Chemical Biology (MCCB) committee from the Royal Dutch Chemistry Society, the Dutch Society for Pharmacology. Lastly, she is chair and local organizer of the European Federation for Medicinal Chemistry and Chemical Biology (EFMC) Short Courses on Medicinal Chemistry, which are organized yearly.
Twitter: https://twitter.com/Heitman_lab
LinkedIn: https://nl.linkedin.com/in/laura-heitman-293347b
Laura's search for better medicines
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Professor Molecular Pharmacology
- Science
- Leiden Academic Centre for Drug Research
- LACDR/Medicinal Chemistry
- Bouma, J., Broekhuis J.D., Horst C. van der, Kumar P., Ligresti A., Stelt M. van der & Heitman L.H. (2023), Dual allosteric and orthosteric pharmacology of synthetic analog cannabidiol-dimethylheptyl, but not cannabidiol, on the cannabinoid CB2 receptor, Biochemical Pharmacology 218: 115924.
- Ciulli A., O'Connor S., Chung C.W., Hartung I.V., Testa A., Daniels D.L. & Heitman L.H. (2023), The 17th EFMC short course on medicinal chemistry on small molecule protein degraders, ChemMedChem 18(20): e202300464.
- Gorostiola González M., Broek R.L. van den, Braun T.G.M., Chatzopoulou M., Jespers W., IJzerman A.P., Heitman L.H. & Westen G.J.P. van (2023), 3DDPDs: describing protein dynamics for proteochemometric bioactivity prediction. A case for (mutant) G protein-coupled receptors, Journal of cheminformatics 15(1): 74.
- Beerkens B.L.H., Snijders I.M., Snoeck J., Liu R., Tool A.T.J., Le Dévédec S.E., Jespers W., Kuijpers T.W., Westen G.J.P. van, Heitman L.H., IJzerman A.P. & Es D. van der (2023), Development of an affinity-based probe to profile endogenous human adenosine A3 receptor expression, Journal of Medicinal Chemistry 66(16): 11399-11413.
- Vlachodimou A., Bouma J., Cleyn M. de, Berthelot D., Pype S., Bosmans J.P., Vlijmen H. van, Wroblowski B., Heitman L.H. & IJzerman A.P. (2023), Kinetic profiling of novel spirobenzo-oxazinepiperidinone derivatives as equilibrative nucleoside transporter 1 inhibitors, Purinergic Signalling : .
- Pham V., Habben Jansen M.C.C., Thompson G., Heitman L.H., Christopoulos A., Thal D.M. & Valant C. (2023), Role of conserved tyrosine lid residues in the activation of the M2 muscarinic acetylcholine receptor, Molecular Pharmacology 104(3): 92-104.
- Heitman L.H., IJzerman A.P., McArdle C.A. & Pawson A.J. (2023), Gonadotrophin-releasing hormone receptors in GtoPdb v.2023.1, IUPHAR/BPS Guide to Pharmacology CITE 2023(1): .
- Siutkina A.I.: Kalinina S., Liu R., Heitman L.H., Junker A., Daniliuc C.G. & Kalinin D.V. (2023), Microwave-assisted synthesis, structure, and preliminary biological evaluation of novel 6-methoxy-5,6-dihydro-5-azapurines, ACS Omega 8(15): 14097-14112.
- Hollander L.S. den, Béquignon O.J.M., Wang X., Wezel K. van, Broekhuis J.D., Gorostiola Gonzalez M., Visser K.E. de, IJzerman A.P., Westen G.J.P. van & Heitman L.H. (2023), Corrigendum to "Impact of cancer-associated mutations in CC chemokine receptor 2 on receptor function and antagonism" [Biochem. Pharmacol. 208 (2023) 115399], Biochemical Pharmacology 209: 115540 (115450).
- Bongers B.J., Sijben H.J., Hartog P.B.R., Tarnovskiy A., IJzerman A.P., Heitman L.H. & Westen G.J.P. van (2023), Proteochemometric modeling identifies chemically diverse norepinephrine transporter inhibitors, Journal of Chemical Information and Modeling 63(6): 1745-1755.
- Li X., Chang H., Bouma J., Paus L.V. de, Mukhopadhyay P., Paloczi J., Mustafa M., Horst C. van der, Kumar S.S., Wu L., Yu Y., Berg R.J.B.H.N. van den, Janssen A.P.A., Lichtman A., Liu Z.J., Pacher P., Stelt M. van der, Heitman L.H. & Hua T. (2023), Structural basis of selective cannabinoid CB2 receptor activation, Nature Communications 14(1): 1447.
- Hollander L.S. den, Béquignon O.J.M., Wang X., Wezel K. van, Broekhuis J., Gorostiola González M., Visser K.E. de, IJzerman A.P., Westen G.J.P. van & Heitman L.H. (2022), Impact of cancer-associated mutations in CC chemokine receptor 2 on receptor function and antagonism, Biochemical Pharmacology 208: 115399.
- Bongers B.J., Gorostiola González M., Wang X., Vlijmen H. van, Jespers W., Gutiérrez-de-Terán H., Ye K., IJzerman A.P., Heitman L.H. & Westen G.J.P. van (2022), Pan-cancer functional analysis of somatic mutations in G protein-coupled receptors, Scientific Reports 12(1): 21534.
- Beerkens B.L.H., Koc C., Liu R., Florea B.I., Le Dévédec S.E., Heitman L.H., IJzerman A.P. & Es D. van der (2022), A chemical biological approach to study G protein-coupled receptors: labeling the adenosine A1 receptor using an electrophilic covalent probe, ACS Chemical Biology 17(11): 3131-3139.
- Bouma J., Soethoudt M., Gils N. van, Xia L., Stelt M van der & Heitman L.H. (2022), Cellular assay to study β-arrestin recruitment by the cannabinoid receptors 1 and 2. In: Maccarrone M. (Ed.) Endocannabinoid Signaling. Methods in Molecular Biology no. 2576 New York, U.S.A.: Humana. 189-199.
- Wang X., Westen G.J.P. van, IJzerman A.P. & Heitman L.H. (2022), G protein-coupled receptors and their mutations in cancer: a focus on adenosine receptors. In: Gilchrist A. (Ed.) GPCRs as therapeutic targets.: John Wiley & Sons. 631-676.
- Feng C.L., Wang X., Jespers W., Liu R., Zamarbide Losada S.D., Gorostiola Gonzalez M., Westen G.J.P. van, Danen E.H.J. & Heitman L.H. (2022), Cancer-associated mutations of the adenosine A2A receptor have diverse influences on ligand binding and receptor functions, Molecules 27(15): 4676.
- Gorostiola Gonzalez M., Janssen A.P.A., IJzerman A.P., Heitman L.H. & Westen G.J.P. van (2022), Oncological drug discovery: AI meets structure-based computational research, Drug Discovery Today 27(6): 1661-1670.
- Vlachodimou A., Vries H. de, Pasoli M., Goudswaard M., Kim S.A., Kim Y.C., Scortichini M., Marshall M., Linden J., Heitman L.H., Jacobson K.A. & IJzerman A.P. (2022), Kinetic profiling and functional characterization of 8-phenylxanthine derivatives as A2B adenosine receptor antagonists, Biochemical Pharmacology 200: 115027.
- Wang X., Jespers W., Wolff K.A.N., Buytelaar J., IJzerman A.P., Westen G.J.P. van & Heitman L.H. (2022), Cancer-related somatic mutations in transmembrane helices alter adenosine A1 receptor pharmacology, Molecules 27(12): 3742.
- Wang X., Jespers W., Waal J.J. de, Wolff K.A.N., Uden L. van, IJzerman A.P., Westen G.J.P. van & Heitman L.H. (2022), Cancer-related somatic mutations alter adenosine A1 receptor pharmacology: a focus on mutations in the loops and C- terminus, The FASEB Journal 36(6): e22358.
- Sijben H.J., Dall’ Acqua L., Liu R., Jarret A., Christodoulaki E., Onstein S., Wolf G., Verburgt S.J., Le Dévédec S.E., Wiedmer T., Superti-Furga G., IJzerman A.P. & Heitman L.H. (2022), Impedance-based phenotypic readout of transporter function: a case for glutamate transporters, Frontiers in Pharmacology 13: 872335.
- Georgakis M.K., Bernhagen J., Heitman L.H., Weber C. & Dichgans M. (2022), Targeting the CCL2–CCR2 axis for atheroprotection, European Heart Journal 43(19): 1799-1808.
- Lemmerhirt J.P., Isaak A., Liu R., Kock M., Daniliuc C.G., Jacobson K.A., Heitman L.H. & Junker A. (2022), Development of Bicyclo[3.1.0]hexane-based A3 receptor ligands: closing the gaps in the structure–affinity relationships, Molecules 27(7): 2283.
- Sijben H.J., Superti-Furga G., IJzerman A.P. & Heitman L.H. (2022), Targeting solute carriers to modulate receptor-ligand interactions, Trends in Pharmacological Sciences 43(5): 358-361.
- Kissel T., Ge C., Hafkenscheid L., Kwekkeboom J.C., Slot L.M., Cavallari M., He Y., Schie K.A. van, Vergroesen R.D., Kampstra A.S.B., Reijm S., Stoeken-Rijsbergen G., Koeleman C., Voortman L.M., Heitman L.H., Xu B., Pruijn G.J.M., Wuhrer M., Rispens T., Huizinga T.J.W., Scherer H.U., Reth M., Holmdahl R. & Toes R.E.M. (2022), Surface Ig variable domain glycosylation affects autoantigen binding and acts as threshold for human autoreactive B cell activation, Science Advances 8(6): 1-21 (eabm1759).
- Mocking T.A.M., Sijben H.J., Vermeulen Y., IJzerman A.P. & Heitman L.H. (2022), MPP+-induced changes in cellular impedance as a measure for organic cation transporter (SLC22A1-3) activity and inhibition, International Journal of Molecular Sciences 23(3): 1203.
- Beerkens B.L.H., Wang X., Avgeropoulou M., Adistia L.N., Veldhoven J.P.D. van, Jespers W., Liu R., Heitman L.H., IJzerman A.P. & Es D. van der (2022), Development of subtype-selective covalent ligands for the adenosine A2B receptor by tuning the reactive group, RSC Medicinal Chemistry 13(7): 850-856.
- Jespers W., Heitman L.H., IJzerman A.P., Sotelo E., Westen G.J.P. van, Aqvist J. & Gutiérrez-de-Terán H. (2021), Deciphering conformational selectivity in the A2A adenosine G protein-coupled receptor by free energy simulations, PLoS Computational Biology 17(11): e1009152.
- Patberg M., Isaak A., Füsser F., Ortiz Zacarías N.V., Vinnenberg L., Schulte J., Michetti L., Grey L., Horst C. van der, Hundehege P., Koch O., Heitman L.H., Budde T. & Junker A. (2021), Piperazine squaric acid diamides, a novel class of allosteric P2X7 receptor antagonists, European Journal of Medicinal Chemistry 226.
- Ortiz Zacarías N.V., Bemelmans M.P., Handel T.M., Visser K.E. de & Heitman L.H. (2021), Anticancer opportunities at every stage of chemokine function, Trends in Pharmacological Sciences 42(11): 912-928.
- Dvorakm V., Wiedmer T., Ingles-Prieto A., Altermatt P., Batoulis H, Bärenz F., Bender E., Digles D., Dürrenberger F., Heitman L.H., IJzerman A.P., Kell D.B., Kickinger S., Körzö D., Leippe P., Licher T., Manolova V., Rizzetto R., Sassone F., Scarabottolo L., Schlessinger A., Schneider V., Sijben H.J., Steck A.L., Sundström H., Tremolada S., Wilhelm M., Wright Muelas M., Zindel D., Steppan C.M. & Superti-Furga G. (2021), An overview of cell-based assay platforms for the solute carrier family of transporters, Frontiers in Pharmacology 12: 722889.
- Wang X., Jespers W., Prieto-Díaz R., Majellaro M., IJzerman A.P., Westen G.J.P. van, Sotelo E. & Heitman L.H. (2021), Identification of V6.51L as a selectivity hotspot in stereoselective A2B adenosine receptor antagonist recognition, Scientific Reports 11.
- Sijben H.J., Oostveen W.M. van, Hartog P.B.R., Stucchi L., Rossignoli A., Maresca G., Scarabottolo. L., IJzerman A.P. & Heitman L.H. (2021), Label-free high-throughput screening assay for the identification of norepinephrine transporter (NET/SLC6A2) inhibitors, Scientific Reports 11.
- Mohr F., Hurrle T., Burggraaff L., Langer L., Bemelmans M.P., Knab M., Nieger M., Westen G.J.P. van, Heitman L.H. & Bräse S. (2021), Synthesis and SAR evaluation of coumarin derivatives as potent cannabinoid receptor agonists, European Journal of Medicinal Chemistry 220.
- Amelia T., Veldhoven J.P.D. van, Falsini M., Liu R., Heitman L.H., Westen G.J.P. van, Segala E., Verdon G., Cheng R.K.Y., Cooke R.M., Es D. van der & IJzerman A.P. (2021), Crystal structure and subsequent ligand design of a nonriboside partial agonist bound to the adenosine A2A receptor, Journal of Medicinal Chemistry 64(7): 3827-3842.
- Ortiz Zacarías N.V., Chahal K.K., Šimková T., Horst C. van der, Zheng Y., Inoue A., Theunissen E., Mallee L., Es D. van der, Louvel J., IJzerman A.P., Handel T.M., Kufareva I. & Heitman L.H. (2021), Design and characterization of an intracellular covalent ligand for CC chemokine receptor 2, Journal of Medicinal Chemistry 64(5): 2608-2621.
- Sijben H.J., Berg J.E. van den, Broekhuis J.D., IJzerman A.P. & Heitman L.H. (2021), A study of the dopamine transporter using the TRACT assay, a novel in vitro tool for solute carrier drug discovery, Scientific Reports 11.
- Wang X., Westen G.J.P. van, Heitman L.H. & IJzerman A.P. (2021), G protein-coupled receptors expressed and studied in yeast. The adenosine receptor as a prime example, Biochemical Pharmacology 187: 114370.
- Yang X., Heitman L.H., IJzerman A.P. & Es D. van der (2021), Molecular probes for the human adenosine receptors, Purinergic Signalling 17: 85-108.
- Sommer F., Ortiz Zacarías N.V., Heitman L.H. & Meijer A.H. (2020), Inhibition of macrophage migration in zebrafish larvae demonstrates in vivo efficacy of human CCR2 inhibitors, Developmental and Comparative Immunology 116: 103932.
- Wagner S., Moura Gatti F., Silva D.G. de, Ortiz Zacarias N.V., Zweemer A.J.M., Hermann S., Maria M. de, Koch M., Weiss C., Schepmann D., Heitman L.H., Tschammer N., Kopka K. & Junker A. (2021), Development of the first potential nonpeptidic positron emission tomography tracer for the imaging of CCR2 receptors, ChemMedChem 16(4): 640-645.
- Superti-Furga G., Lackner D., Wiedmer T., Ingles-Prieto A., Barbosa B., Girardi E., Goldmann U., Gürtl B., Klavins K., Klimek C., Lindinger S., Liñeiro-Retes E., Müller A.C., Onstein S., Redinger G., Reil D., Sedlyarov V., Wolf G., Crawford M., Everley R., Hepworth D., Liu S., Noell S., Piotrowski M., Stanton R., Zhang H., Corallino S., Faedo A., Insidioso M., Maresca G., Redaelli L., Sassone F., Scarabottolo L., Stucchi M., Tarroni P., Tremolada S., Batoulis H., Becker A., Bender E., Chang Y.N., Ehrmann A., Müller-Fahrnow A., Pütter V., Zindel D., Hamilton B., Lenter M., Santacruz D., Viollet C., Whitehurst C., Johnsson K., Leippe P., Baumgarten B., Chang L., Ibig Y., Pfeifer M., Reinhardt J., Schönbett J., Selzer P., Seuwen K., Bettembourg C., Biton B., Czech J., de Foucauld H., Didier M., Licher T., Mikol V., Pommereau A., Puech F., Yaligara V., Edwards A., Bongers B.J., Heitman L.H., Ijzerman A.P., Sijben H.J., Westen G.J.P. van, Grixti J., Kell D.B., Mughal F., Swainston N., Wright-Muelas M., Bohstedt T., Burgess-Brown N., Carpenter L., Dürr K., Hansen J., Scacioc A., Banci G., Colas C., Digles D., Ecker G., Füzi B., Gamsjäger V., Grandits M., Martini R., Troger F., Altermatt P., Doucerain C., Dürrenberger F., Manolova V., Steck A.L., Sundström H., Wilhelm M. & Steppan C.M. (2020), The RESOLUTE consortium: unlocking SLC transporters for drug discovery, Nature Reviews Drug Discovery 19(7): 429-430.
- Wang X. Jespers W. Bongers B.J. Habben Jansen M.C.C. Stangenberger C.M. Dilweg M.A. Gutiérrez-de-Terán H. IJzerman A.P. Heitman L.H. Westen G.J.P. van (2020), Characterization of cancer-related somatic mutations in the adenosine A2B receptor, European Journal of Pharmacology 880: 173126.
- Qile M., Ji Y., Golden T.D., Houtman M.J.C., Romunde F., Fransen D., Ham W.B. van, IJzerman A.P., January C.T., Heitman L.H., Stary-Weinzinger A., Delisle B.P. & Heyden M.A.G. van der (2020), LUF7244 plus Dofetilide Rescues Aberrant Kv11.1 Trafficking and Produces Functional IKv11.1, Molecular Pharmacology 97(6): 355-364.
- Yang X. Dilweg M.A. Osemwengie D. Burggraaff L. Es D. van der Heitman L.H. IJzerman A.P. (2020), Design and pharmacological profile of a novel covalent partial agonist for the adenosine A1 receptor, Biochemical Pharmacology 180: 114144.
- Velden W.J.C. van der, Heitman L.H. & Rosenkilde M.M. (2020), Perspective: implications of ligand-receptor binding kinetics for therapeutic targeting of G protein-coupled receptors, ACS Pharmacology & Translational Science 3(2): 179-189.
- Vlachodimou A., Konstantinopoulou K., IJzerman A.P. & Heitman L.H. (2020), Affinity, binding kinetics and functional characterization of draflazine analogues for human equilibrative nucleoside transporter 1 (SLC29A1), Biochemical Pharmacology 172: 113747.
- Doornbos M.L.J. & Heitman L.H. (2019), Label-free impedance-based whole cell assay to study GPCR pharmacology. In: Shukla A.K. (Ed.), G Protein-Coupled Receptors, Part B. Methods in Cell Biology no. Volume 149: Elsevier. 179-194.
- Ortiz Zacarías N.V., Veldhoven J.P.D. van, Hollander L.S. den, Dogan B., Openy J., Hsiao Y.Y., Lenselink E.B., Heitman L.H. & IJzerman A.P. (2019), Synthesis and Pharmacological Evaluation of Triazolopyrimidinone Derivatives as Noncompetitive, Intracellular Antagonists for CC Chemokine Receptors 2 and 5, Journal of Medicinal Chemistry 62(24): 11035-11053.
- Ruano‑Ordás D., Burggraaff L., Liu R., Horst C. van der, Heitman L.H., Emmerich M.T.M., Mendez J.R., Yevseyeva I. & Westen G.J.P. van (2019), A multiple classifier system identifies novel cannabinoid CB2 receptor ligands, Journal of Cheminformatics 11: 66.
- Qile M., Beekman H.D.M., Sprenkeler D.J., Houtman M.J.C., Ham W.B. van, Stary-Weinzinger A., Beyl S., Hering S., Berg D.J. van den, Lange E.C.M. de, Heitman L.H., IJzerman A.P., Vos M.A. & Heyden M.A.G. van der (2019), LUF7244, an allosteric modulator/activator of Kv11.1 channels, counteracts dofetilide‐induced torsades de pointes arrhythmia in the chronic atrioventricular block dog model, British Journal of Pharmacology 176(19): 3871-3885.
- Vlachodimou A., IJzerman A.P. & Heitman L.H. (2019), Label-free detection of transporter activity via GPCR signalling in living cells: A case for SLC29A1, the equilibrative nucleoside transporter 1, Scientific Reports 9(1): 13802.
- Bouzo-Lorenzo M., Stoddart L.A., Xia L., IJzerman A.P., Heitman L.H., Briddon S.J. & Hill S.J. (2019), A live cell NanoBRET binding assay allows the study of ligand-binding kinetics to the adenosine A(3) receptor, Purinergic Signalling 15(2): 139-153.
- Yang X., Veldhoven J.P.D. van, Offringa J., Kuiper B.J., Lenselink E.B., Heitman L.H., Es D. van der & IJzerman A.P. (2019), Development of Covalent Ligands for G Protein-Coupled Receptors: A Case for the Human Adenosine A3 Receptor, Journal of Medicinal Chemistry 62(7): 3539-3552.
- Yun Y., Chen J., Liu R., Chen W., Liu C., Wang R., Hou Z., Yu Z., Sun Y., IJzerman A.P., Heitman L.H., Yin X. & Guo D. (2019), Long residence time adenosine A1 receptor agonists produce sustained wash-resistant antilipolytic effect in rat adipocytes, Biochemical Pharmacology 164: 45-52.
- Soethoudt M., Alachouzos G., Rooden E.J. van, Moya Garzón M.D., Berg R.J.B.H.N. van den, Heitman L.H. & Stelt M. van der (2018), Development of a Cannabinoid-Based Photoaffinity Probe to Determine the D8/9- Tetrahydrocannabinol Protein Interaction Landscape in Neuroblastoma Cells, Cannabis and Cannabinoid Research 3(1): 136-151.
- Yang X., Michiels T.J.M., Jong C. de, Soethoudt M., Dekker N., Gordon E., Stelt M. van der, Heitman L.H., Es D. van der & IJzerman A.P. (2018), An Affinity-Based Probe for the Human Adenosine A(2A) Receptor, Journal of Medicinal Chemistry 61(17): 7892-7901.
- Doornbos M.L.J., Vermond S.C., Lavreysen H., Tresadern G., IJzerman A.P. & Heitman L.H. (2018), Impact of allosteric modulation: exploring the binding kinetics of glutamate and other orthosteric ligands of the metabotropic glutamate receptor 2, Biochemical Pharmacology 155: 356-365.
- Doornbos M.L.J., Linden I. van der, Vereyken L., Tresadern G., IJzerman A.P., Lavreysen H. & Heitman L.H. (2018), Constitutive activity of the metabotropic glutamate receptor 2 explored with a whole-cell label-free biosensor, Biochemical Pharmacology 152: 201-210.
- Guo D., Peletier L.A., Bridge L., Keur W., Vries H. de, Zweemer J.M., Heitman L.H. & IJzerman A.P. (2018), A two-state model for the kinetics of competitive radioligand binding, British Journal of Pharmacology 175(10): 1719-1730.
- Xia L., Vries H. de, Yang X., Lenselink E.B., Kyrizaki A., Barth F., Louvel J., Dreyer M.K., Es D. van der, IJzerman A.P. & Heitman L.H. (2018), Kinetics of human cannabinoid 1 (CB1) receptor antagonists: Structure-kinetics relationships (SKR) and implications for insurmountable antagonism, Biochemical Pharmacology 151: 166-179.
- Ortiz Zacarías N.V., Lenselink E.B., IJzerman A.P., Handel T.M. & Heitman L.H. (2018), Intracellular Receptor Modulation: Novel Approach to Target GPCRs, Trends in Pharmacological Sciences 39(6): 547-559.
- Soethoudt M., Hoorens M.W.H., Doelman W., Martella A., Stelt M. van der & Heitman L.H. (2018), Structure-kinetic relationship studies of cannabinoid CB2 receptor agonists reveal substituent-specific lipophilic effects on residence time, Biochemical Pharmacology 152: 129-142.
- Doornbos M.L.J., Wang X., Vermond S.C., Peeters L., Pérez-Benito L., Trabanco A.A., Lavreysen H., Cid J.M., Heitman L.H., Tresadern G. & IJzerman A.P. (2019), Covalent Allosteric Probe for the Metabotropic Glutamate Receptor 2: Design, Synthesis, and Pharmacological Characterization, Journal of Medicinal Chemistry 62(1): 223-233.
- Soethoudt M., Stolze S.C., Westphal M.V., Stralen L. van, Martella A., Rooden E.J. van, Guba W., Varga Z.V., Deng H., Kasteren S.I. van, Grether U., IJzerman A.P., Pacher P., Carreira E.M., Overkleeft H.S., Heitman L.H., Ioan-Facsinay A. & Stelt M. van der (2018), A selective photoaffinity probe that enables assessment of cannabinoid CB2 receptor expression and ligand engagement in human cells, Journal of the American Chemical Society 140(19): 6067-6075.
- Heimann D., Börgel F., Vries H. de, Patberg M., Jan-Smith E., Frehland B., Schepmann D., Heitman L.H. & Wunsch B. (2018), Optimization of the metabolic stability of a fluorinated cannabinoid receptor subtype 2 (CB2) ligand designed for PET studies, European Journal of Medicinal Chemistry 146: 409-422.
- Xia L.Z., Kyrizaki A., Tosh D.K., Duijl T.T. van, Roorda J.C., Jacobson K.A., IJzerman A.P. & Heitman L.H. (2018), A binding kinetics study of human adenosine A(3) receptor agonists, Biochemical Pharmacology 153: 248-259.
- Hilger J.M., Lieuw W.L., Heitman L.H. & IJzerman A.P. (2017), Label-free technology and patient cells: from early drug development to precision medicine, Drug Discovery Today 22(12): 1808-1815.
- Xia L., Vries H. de, Lenselink E.B., Louvel J.A., Waring M.J., Cheng L., Pahlen S., Petersson M.J., Schell P., Olsson R.I., Heitman L.H., Sheppard R.J. & IJzerman A.P. (2017), Structure-Affinity Relationships and Structure-Kinetic Relationships of 1,2-Diarylimidazol-4-carboxamide Derivatives as Human Cannabinoid 1 Receptor Antagonists, Journal of Medicinal Chemistry 60(23): 9545-9564.
- Jespers W., Schiedel A.C., Heitman L.H., Cooke R.M., Kleene L., Westen G.J.P. van, Gloriam D.E., Müller C.E., Sotelo E. & Gutiérrez-de-Terán H. (2018), Structural Mapping of Adenosine Receptor Mutations: Ligand Binding and Signaling Mechanisms, Trends in Pharmacological Sciences 39(1): 75-89.
- Nederpelt I., Kuzikov M., Witte W.E.A. de, Schnider P., Tuijt B., Gul S., IJzerman A.P., Lange E.C.M. de & Heitman L.H. (2017), From receptor binding kinetics to signal transduction; a missing link in predicting in vivo drug-action, Scientific Reports 7: 14169.
- Heimann D., Börgel F., Vries H. de, Bachmann K., Rose V.E., Frehland B., Schepmann D., Heitman L.H. & Wünsch B. (2018), Optimization of pharmacokinetic properties by modification of a carbazole-based cannabinoid receptor subtype 2 (CB2) ligand, European Journal of Medicinal Chemistry 143: 1436-1447.
- Martella A., Sijben H.J., Rufer A.C., Grether U., Fingerle J., Ullmer C., Hartung T., IJzerman A.P., Stelt M. van der & Heitman L.H. (2017), A novel selective inverse agonist of the CB2 receptor as a radiolabeled tool compound for kinetic binding studies, Molecular Pharmacology 92(4): 389-400.
- Xia L., Burger W.A.C., Veldhoven J.P.D. van, Kuiper B.J., Duijl T.T. van, Lenselink E.B., Paasman E., Heitman L.H. & IJzerman A.P. (2017), Structure-Affinity Relationships and Structure-Kinetics Relationships of Pyrido[2,1-f]purine-2,4-dione Derivatives as Human Adenosine A(3) Receptor Antagonists, Journal of Medicinal Chemistry 60(17): 7555-7568.
- Doornbos M.L.J., Cid J.M., Haubrich J., Nunes A.G., Sande J.W. van de, Vermond S.C., Mulder T., Trabanco A.A., Ahnaou A., Drinkenburg W.H., Lavreysen H., Heitman L.H., IJzerman A.P. & Tresadern G. (2017), Discovery and Kinetic Profiling of 7‑Aryl-1,2,4-triazolo[4,3‑a]pyridines: Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 2, Journal of Medicinal Chemistry 60(15): 6704–6720.
- Heimann D., Lueg C., Vries H. de, Frehland B., Schepmann D., Heitman L.H. & Wunsch B. (2017), Bioisosteric replacement of central 1,2,4-oxadiazole ring of high affinity CB2 ligands by regioisomeric 1,3,4-oxadiazole ring, MedChemComm 8: 1697-1705.
- Thum S., Kokornaczyk A.K., Seki T., De Maria M., Ortiz Zacarias N.V., Vries H. de, Weiss C., Koch M.l., Schepmann D., Kitamura M., Tschammer N., Heitman L.H., Junker A. & Wuensch B. (2017), Synthesis and biological evaluation of chemokine receptor ligands with 2-benzazepine scaffold, European Journal of Medicinal Chemistry 135: 401-413.
- Yang X., Dong G., Michiels T.J.M., Lenselink E.B., Heitman L.H., Louvel J.A. & IJzerman A.P. (2017), A covalent antagonist for the human adenosine A_2A receptor, Purinergic Signalling 13(2): 191-201.
- Hillger J.M., Roy B. le, Wang Z., Mulder-Krieger T., Boomsma D.I., Slagboom P.E., Danen E.H.J., IJzerman A.P. & Heitman L.H. (2017), Phenotypic screening of cannabinoid receptor 2 ligands shows different sensitivity to genotype, Biochemical Pharmacology 130: 60-70.
- Schuetz D.A., Witte W.E.A. de, Wong Y.C, Knasmueller B., Richter L., Kokh D.B., Sadiq S.K., Bosma R., Nederpelt I., Heitman L.H., Segala E., Amaral M., Guo D., Andres D., Georgi V., Stoddart L.A., Hill S., Cooke R.M., Graaf C. de, Leurs R., Frech M., Wade R.C., Lange E.C.M. de, IJzerman A.P., Mueller-Fahrnow A. & Ecker G.F. (2017), Kinetics for Drug Discovery: an industry-driven effort to target drug residence time, Drug Discovery Today 22(6): 896-911.
- Bot I., Ortiz Zacarias N.V., Witte W.E. de, Vries H. de, Santbrink P.J. van, Velden D. van der, Kroener M.J., Berg D.J. van den, Stamos D., Lange E.C.M. de, Kuiper J., IJzerman A.P. & Heitman L.H. (2017), A novel CCR2 antagonist inhibits atherogenesis in apoE deficient mice by achieving high receptor occupancy, Scientific Reports 2017(7): 52.
- Soethoudt M., Grether U., Fingerle J., Grim T.W., Fezza F., Petrocellis L. de, Ullmer C., Rothenhäusler B., Perret C., Gils N. van, Finlay D., MacDonald C., Chicca A., Gens M.D., Stuart J., Vries H. de, Mastrangelo N., Xia L., Alachouzos G., Baggelaar M.P., Martella A., Mock E.D., Deng H., Heitman L.H., Connor M., Di Marzo V., Gertsch J., Lichtman A.H., Maccarrone M., Pacher P., Glass M. & Stelt M. van der (2017), Cannabinoid CB2 receptor ligand profiling reveals biased signalling and off-target activity, Nature Communications 8: 13958.
- Soethoudt M., Van Gils N., Stelt M. van der & Heitman L.H. (2016), Protocol to Study β-Arrestin Recruitment by CB1 and CB2 Cannabinoid Receptors. In: Maccarrone M. (Ed.), Endocannabinoid Signaling: Methods and Protocols. Methods in Molecular Biology no. 1412. New York: Springer . 103-111.
- Zheng Y., Qin L., Ortiz Zacarias N.V., Vries H. de, Han G.W., Gustavsson M., Dabros M., Zhao C., Cherney R.J., Carter P., Stamos D., Abagyan R., Cherezov V., Stevens R.C., IJzerman A.P., Heitman L.H., Tebben A., Kufareva I. & Handel T.M. (2016), Structure of CC chemokine receptor 2 with orthosteric and allosteric antagonists, Nature 540(7633): 458-461.
- Nederpelt I., Bleeker D., Tuijt B., IJzerman A.P. & Heitman L.H. (2016), Kinetic binding and activation profiles of endogenous tachykinins targeting the NK1 receptor, Biochemical Pharmacology 118: 88-95.
- Guo D., Heitman L.H. & IJzerman A.P. (2016), The Added Value of Assessing Ligand-Receptor Binding Kinetics in Drug Discovery, Acs Medicinal Chemistry Letters 7(9): 819-821.
- Hillger J.M., Diehl C., Spronsen E. van, Boomsma D.I., Slagboom P.E., Heitman L.H. & Ijzerman A.P. (2016), Getting personal: Endogenous adenosine receptor signaling in lymphoblastoid cell lines, Biochemical Pharmacology 115: 114-122.
- Segala E., Guo D., Cheng R.K.Y., Bortolato A., Deflorian F., Dore A.S., Errey J.C., Heitman L.H., IJzerman A.P., Marshall F.H. & Cooke R.M. (2016), Controlling the dissociation of ligands from the adenosine A(2A) receptor through modulation of salt bridge strength, Journal of Medicinal Chemistry 59(13): 6470-6479.
- Guo D., Pan A.C., Dror R.O., Mocking T., Liu R., Heitman L.H., Shaw D.E. & IJzerman A.P. (2016), Molecular Basis of Ligand Dissociation from the Adenosine A(2A) Receptor, Molecular Pharmacology 89(5): 485-491.
- Nederpelt I., Vergroesen R.D., IJzerman A.P. & Heitman L.H. (2016), Persistent GnRH receptor activation in pituitary αT3-1 cells analyzed with a label-free technology, Biosensors and Bioelectronics 79: 721-727.
- Yu Z., Liu J., Veldhoven J.P.D. van, IJzerman A.P., Schalij M.J., Pijnappels D.A., Heitman L.H. & Vries A.A.F. de (2016), Allosteric modulation of K(v)11.1 (hERG) channels protects against drug-induced ventricular arrhythmias, Circulation: Arrhythmia and Electrophysiology 9(4): e003439.
- Guo D., Heitman L.H. & IJzerman A.P. (2017), Kinetic Aspects of the Interaction between Ligand and G Protein-Coupled Receptor: The Case of the Adenosine Receptors, Chemical Reviews 117(1): 38-66.
- Guo D., Dijksteel G.S., Duijl T. van, Heezen M., Heitman L.H. & IJzerman A.P. (2016), Equilibrium and kinetic selectivity profiling on the human adenosine receptors, Biochemical Pharmacology 105: 34-41.
- Doornbos M.L.J., Perez-Benito L., Tresadern G., Mulder T., Biesmans I., Trabanco A.A., Cid M.J., Lavreysen H., IJzerman A.P. & Heitman L.H. (2016), Molecular mechanism of positive allosteric modulation of the metabotropic glutamate receptor 2 by JNJ-46281222, British Journal of Pharmacology 173(3): 588-600.
- Mukhopadhyay P., Baggelaar M., Erdelyi K., Cao Z., Cinar R., Fezza F., Ignatowska-Jankowska B., Wilkerson J., Gils N. van, Hansen T., Ruben M., Soethoudt M., Heitman L., Kunos G., Maccarrone M., Lichtman A., Pacher P. & Stelt M. van der (2016), The novel, orally available and peripherally restricted selective cannabinoid CB2 receptor agonist LEI-101 prevents cisplatin-induced nephrotoxicity, British Journal of Pharmacology 173(3): 446–458.
- Nederpelt I., Georgi V., Schiele F., Nowak-Reppel K., Fernández-Montalván A.E., IJzerman A.P. & Heitman L.H. (2016), Characterization of 12 GnRH peptide agonists : a kinetic perspective, British Journal of Pharmacology 173(1): 128-141.
- Witte W.E., Wong Y.C., Nederpelt I., Heitman L.H., Danhof M., Graaf P.H. van der, Gilissen R.A. & De Lange E.C. (2016), Mechanistic models enable the rational use of in vitro drug-target binding kinetics for better drug effects in patients, Expert Opinion on Drug Discovery 11(1): 45-63.
- Nederpelt I., Bunnik J., IJzerman A.P. & Heitman L.H. (2016), Kinetic profile of neuro-peptide-receptor interactions, Trends in Neurosciences 39: 830.
- Junker A., Kokornaczyk A.K., Zweemer A.J., Frehland B., Schepmann D., Yamaguchi J., Itami K., Faust A., Hermann S., Wagner S., Schaefers M., Koch M., Weiss C., Heitman L.H., Kopka K. & Wuensch B. (2015), Synthesis, binding affinity and structure-activity relationships of novel, selective and dual targeting CCR2 and CCR5 receptor antagonists, ORGANIC & BIOMOLECULAR CHEMISTRY 13(8): 2407-2422.
- Hillger J.M., Schoop J., Boomsma D.I., Slagboom P.E., IJzerman A.P. & Heitman L.H. (2015), Whole-cell biosensor for label-free detection of GPCR-mediated drug responses in personal cell lines, Biosensors and Bioelectronics 74: 233-42.
- Xia L., Vries H. de, IJzerman A.P. & Heitman L.H. (2016), Scintillation proximity assay (SPA) as a new approach to determine a ligand's kinetic profile. A case in point for the adenosine A1 receptor, Purinergic Signalling 12(1): 115-126.
- Yu Z., Veldhoven J.P.D. van, Hart I.M. 't, Kopf A.H., Heitman L.H. & IJzerman A.P. (2015), Synthesis and biological evaluation of negative allosteric modulators of the Kv11.1(hERG) channel, European Journal of Medicinal Chemistry 106: 50-9.
- Vilums M., Heuberger J., Heitman L.H. & IJzerman A.P. (2015), Indanes--Properties, Preparation, and Presence in Ligands for G Protein Coupled Receptors, Medicinal Research Reviews 35(6): 1097-1126.
- Guo D., Heitman L.H. & IJzerman A.P. (2015), The Role of Target Binding Kinetics in Drug Discovery, ChemMedChem 10(11): 1793-6.
- Louvel J., Guo D., Soethoudt M., Mocking T.A.M., Lenselink E.B., Mulder-Krieger T., Heitman L.H. & Ijzerman A.P. (2015), Structure-kinetics relationships of Capadenoson derivatives as adenosine A(1) receptor agonists, European Journal of Medicinal Chemistry 101: 681-691.
- Vilums M., Zweemer A.J.M., Dilanchian A., Veldhoven J.P.D., Vries H. de, Brussee J., Saunders J., Stamos D., Heitman L.H. & IJzerman A.P. (2015), Evaluation of (4-Arylpiperidin-1-yl)cyclopentanecarboxamides As High-Affinity and Long-Residence-Time Antagonists for the CCR2 Receptor, ChemMedChem 10(7): 1249-1258.
- Strunz A.K., Zweemer J.M., Weiss C., Schepmann D., Junker A., Heitman L.H., Koch M. & Wünsch B. (2015), Synthesis and biological evaluation of spirocyclic antagonists of CCR2 (chemokine CC receptor subtype 2), Bioorganic & Medicinal Chemistry 23(14): 4034-4049.
- Zhiyi Y., Veldhoven J.P.D. van, Louvel J.A., Hart I.M.E. 't, Rook M.B., Heyden M.A.G. van der, Heitman L.H. & IJzerman A.P. (2015), Structure-affinity relationships (SARs) and structure-kinetics relationships (SKRs) of Kv11.1 blockers, Journal of Medicinal Chemistry 58(15): 5916-5929.
- Guo D., IJzerman A.P. & Heitman L.H. (2015), Importance of drug-target residence time at G protein-coupled receptors - a case for the adenosine receptors. In: Keseru G., Swinney D.C., Mannhold R., Kubinyi H. & Folkers G. (Eds.), Thermodynamics and Kinetics of Drug Binding. Methods and Principles in Medicinal Chemistry. Dusseldorf: Wiley. 360.
- Vilums M., Zweemer A.J., Barmare F., Gracht A.M. van der, Bleeker D.C.T., Yu Z., Vries H. de, Gross R., Clemens J., Krenitsky P., Brussee H., Stamos D., Saunders J., Heitman L.H. & IJzerman A.P. (2015), When structure-affinity relationships meet structure-kinetics relationships: 3-((Inden-1-yl)amino)-1-isopropyl-cyclopentane-1-carboxamides as CCR2 antagonists, European Journal of Medicinal Chemistry 93: 121-34.
- Yu Z., IJzerman A.P. & Heitman L.H. (2015), Kv11.1 (hERG)-induced cardiotoxicity: a molecular insight from a binding kinetics study of prototypical Kv11.1 (hERG) inhibitors, British Journal of Pharmacology 172(3): 940-955.
- Massink A., Gutiérrez-de-Terán H., Lenselink E.B., Ortiz Zacarías N.V., Xia L., Heitman L.H., Katritch V., Stevens R.C. & IJzerman A.P. (2015), Sodium Ion Binding Pocket Mutations and Adenosine A2A Receptor Function, Molecular Pharmacology 87(2): 305-13.
- Guo D., Xia L., Veldhoven J.P.D. van, Hazeu M.D., Mocking T., Brussee J.M., IJzerman A.P. & Heitman L.H. (2014), Binding kinetics of ZM241385 derivatives at the human adenosine A(2A) receptor, ChemMedChem 9(4): 752-761.
- Vilums M., Zweemer A.J.M., Dekkers S., Askar Y., Vries H. de, Saunders J., Stamos D., Brussee J., Heitman L.H. & IJzerman A.P. (2014), Design and synthesis of novel small molecule CCR2 antagonists: evaluation of 4-aminopiperidine derivatives, Bioorganic and Medicinal Chemistry Letters 24(23): 5377-5380.
- Guo D., Hillger J.M., IJzerman A.P. & Heitman L.H. (2014), Drug-Target Residence Time-A Case for G Protein-Coupled Receptors, Medicinal Research Reviews 34(4): 856-892.
- Zweemer A.J.M., Toraskar J., Heitman L.H. & IJzerman A.P. (2014), Bias in chemokine receptor signalling, Trends in Immunology 35(6): 243-252.
- Louvel J.A., Guo D., Agliardi M., Mocking T.A.M., Kars R., Xia L., Vries H. de, Brussee J., Heitman L.H. & IJzerman A.P. (2014), Agonists for the adenosine A(1) receptor with tunable residence time: a case for nonribose 4-Amino-6-aryl-5-cyano-2-thiopyrimidines, Journal of Medicinal Chemistry 57(8): 3213-3222.
- Yu Z., Klaasse E., Heitman L.H. & IJzerman A.P. (2014), Allosteric modulators of the hERG K+ channel Radioligand binding assays reveal allosteric characteristics of dofetilide analogs, Toxicology and Applied Pharmacology 274(1): 78-86.
- Gutlerrez-de-Teran Hugo, Massink Arnault, Rodriguez David, Liu Wei, Han Gye Won, Joseph Jeremiah S., Katritch Ilia, Heitman Laura H., Xia Lizi, IJzerman Adriaan P., Cherezov Vadim, Katritch Vsevolod & Stevens Raymond C. (2013), The Role of a Sodium Ion Binding Site in the Allosteric Modulation of the A(2A) Adenosine G Protein-Coupled Receptor, Structure Fold Design 21(12): 2175-2185.
- Zweemer Annelien J.M., Nederpelt Indira, Vrieling Hilde, Hafith Sarah, Doornbos Maarten L.J., De Vries Henk, Abt Jeffrey, Gross Raymond, Stamos Dean, Saunders John, Smit Martine J., IJzerman Adriaan P. & Heitman Laura H. (2013), Multiple Binding Sites for Small-Molecule Antagonists at the CC Chemokine Receptor 2, Molecular Pharmacology 84(4): 551-561.
- Vilums Maris, Zweemer Annelien J.M., Yu Zhiyi, De Vries Henk, Hillger Julia M., Wapenaar Hannah, Bollen Ilse A.E., Barmare Farhana, Gross Raymond, Clemens Jeremy, Krenitsky Paul, Brussee Johannes, Stamos Dean, Saunders John, Heitman Laura H. & IJzerman Adriaan P. (2013), Structure-Kinetic Relationships-An Overlooked Parameter in Hit-to-Lead Optimization: A Case of Cyclopentylamines as Chemokine Receptor 2 Antagonists, Journal of Medicinal Chemistry 56(19): 7706-7714.
- Guo Dong, Van Dorp Erika J.H., Mulder-Krieger Thea, Van Veldhoven Jacobus P.D., Brussee Johannes, IJzerman Adriaan P. & Heitman Laura H. (2013), Dual-Point Competition Association Assay: A Fast and High-Throughput Kinetic Screening Method for Assessing Ligand-Receptor Binding Kinetics, Journal of Biomolecular Screening 18(3): 309-320.
- Guo Dong, Mulder-Krieger Thea, IJzerman Adriaan P. & Heitman Laura H. (2012), Functional efficacy of adenosine A2A receptor agonists is positively correlated to their receptor residence time, British Journal of Pharmacology 166(6): 1846-1859.
- Liu Wei, Chun Eugene, Thompson Aaron A., Chubukov Pavel, Xu Fei, Katritch Vsevolod, Han Gye Won, Roth Christopher B., Heitman Laura H., IJzerman Adriaan P., Cherezov Vadim & Stevens Raymond C. (2012), Structural Basis for Allosteric Regulation of GPCRs by Sodium Ions, Science 337(6091): 232-236.
- Heitman Laura H., Kleinau Gunnar, Brussee Johannes, Krause Gerd & Ijzerman Adriaan P. (2012), Determination of different putative allosteric binding pockets at the lutropin receptor by using diverse drug-like low molecular weight ligands, Molecular and Cellular Endocrinology 351(2): 326-336.
- Watts A.O., Scholten D.J., Heitman L.H., Vischer H.F. & Leurs R. (2012), Label-free impedance responses of endogenous and synthetic chemokine receptor CXCR3 agonists correlate with G(i)-protein pathway activation, Biochemical and Biophysical Research Communications 419(2): 412-418.
- Chen D., Errey J.C., Heitman L.H., Marshall F.H., IJzerman A.P. & Siegal G.D. (2012), Fragment screening of GPCRs using biophysical methods: identification of ligands of the adenosine A(2A) receptor with novel biological activity, ACS Chemical Biology 7(12): 2064-2073.
- Heitman Laura H., Narlawar Rajeshwar, De Vries Henk, Willemsen Milou N., Wolfram Dieter, Brussee Johannes & IJzerman Adriaan P. (2010), Corrections to Substituted Terphenyl Compounds as the First Class of Low Molecular Weight Allosteric Inhibitors of the Luteinizing Hormone Receptor, Journal of Medicinal Chemistry 53(1): 520-520.
- Heitman L.H. (22 April 2009), Allosteric Modulation of 'Reproductive' GPCRs : a case for the GnRH and LH receptors (Dissertatie, Faculty of Science, Leiden University). Supervisor(s): IJzerman A.P.
- Heitman L.H., Göblyös A., Zweemer A.M., Bakker R., Mulder-Krieger T., Veldhoven J.P.D. van, Vries H. de, Brussee J. & IJzerman A.P. (2009), A series of 2,4-disubstituted quinolines as a new class of allosteric enhancers of the adenosine A(3) receptor, Journal of Medicinal Chemistry 52(4): 926-931.
- Bonger K.M., Van den Berg R., Knijnenburg A.D., Heitman L.H., Van Koppen C.J., Timmers C., Overkleeft H.S. & Marel G.A. van der (2009), Discovery of Selective Luteinizing Hormone Receptor Agonists Using the Bivalent Ligand Method, ChemMedChem 4(7): 1189-1195.
- Heitman Laura H., Narlawar Rajeshwar, De Vries Henk, Willemsen Milou N., Wolfram Dieter, Brussee Johannes & IJzerman Adriaan P. (2009), Substituted Terphenyl Compounds as the First Class of Low Molecular Weight Allosteric Inhibitors of the Luteinizing Hormone Receptor, Journal of Medicinal Chemistry 52(7): 2036-2042.
- Heitman L.H., Oosterom J., Bonger K.M., Timmers C., Wiegerinck P. & IJzerman A.P. (2008), [3H]Org 43553, the first low molecular weight agonistic and allosteric radioligand for the human luteinizing hormone receptor, Molecular Pharmacology 73(2): 518-524.
- Heitman L.H., Ye K., Oosterom J. & IJzerman A.P. (2008), Amiloride derivatives and a nonpeptidic antagonist bind at two distinct allosteric sites in the human gonadotropin-releasing hormone receptor, Molecular Pharmacology 73(6): 1808-1815.
- Heitman L.H., Veldhoven J.P.D. van, Zweemer A.M., Ye K., Brussee J. & IJzerman A.P. (2008), False Positives in a Reporter Gene Assay: Identification and Synthesis of Substituted N-Pyridin-2-yl-benzamides as Competitive Inhibitors of Firefly Luciferase, Journal of Medicinal Chemistry 51(15): 4724-4729.
- Heitman L.H. & IJzerman A.P. (2008), G Protein-Coupled Receptors of the Hypothalamic-Pituitary-Gonadal Axis: A Case for GnRH, LH, FSH, and GPR54 Receptor Ligands, Medical Research Reviews 28(6): 975-1011.
- Bonger K.M., Berg R.J.B.H.N. van den, Knijnenburg A.D., Heitman L.H., IJzerman A.P., Oosterom J., Timmers C.M., Overkleeft H.S. & Marel G.A. van der (2008), Synthesis and evaluation of homodimeric GnRHR antagonists having a rigid bis-propargylated benzene core, Bioorganic & Medicinal Chemistry 16(7): 3744-3758.
- Bonger K.M., Berg R.J.B.H.N. van den, Heitman L.H., IJzerman A.P., Oosterom J., Timmers C.M., Overkleeft H.S. & Marel G.A. van der (2007), Synthesis and evaluation of homo-bivalent GnRHR ligands, Bioorganic & Medicinal Chemistry 15(14): 4841-4856.
- Heitman L.H., Mulder-Krieger T., Spanjersberg R.F., Frijtag Drabbe Künzel J.K. von, Dalpiaz A. & IJzerman A.P. (2006), Allosteric modulation, thermodynamics and binding to wild-type and mutant (T277A) adenosine A1 receptors of LUF5831, a novel nonadenosine-like agonist, British Journal of Pharmacology 147(5): 533-541.
- Nieuwendijk A.M.C.H. van den, Pietra D., Heitman L.H., Göblyös A. & IJzerman A.P. (2004), Synthesis and biological evaluation of 2,3,5-substituted [1,2,4]thiadiazoles as allosteric modulators of adenosine receptors, Journal of Medicinal Chemistry 47(3): 663-672.
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