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

Autor: Maarten L J, Doornbos, Laura H, Heitman

Publikováno v: Methods in cell biology. 149

The superfamily of G protein-coupled receptors (GPCRs) represents the largest group of cell surface receptors in the human body. It is estimated that around 40% of the drugs currently on the market target GPCRs. As only a very small number of GPCRs i

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::2095c1610d99dfa43fbe6cd955ddf42c
https://pubmed.ncbi.nlm.nih.gov/30616818

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

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

Publikováno v: British Journal of Pharmacology. 173:588-600

Background and Purpose Allosteric modulation of the mGlu 2 receptor is a potential strategy for treatment of various neurological and psychiatric disorders. Here, we describe the in vitro characterization of the mGlu 2 positive allosteric modulator (

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::6d90570735e8c3a06e277e87721af12d
https://doi.org/10.1111/bph.13390

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

Autor: Maarten L. J. Doornbos, Hilde Lavreysen, Alexandro Nunes, Adriaan P. IJzerman, Jordi Haubrich, Gary Tresadern, Sophie C. Vermond, Wilhelmus Drinkenburg, Laura H. Heitman, Jasper W. van de Sande, A. Ahnaou, Andrés A. Trabanco, Thea Mulder-Krieger, José María Cid

Publikováno v: Journal of medicinal chemistry, 60(15), 6704–6720
Journal of Medicinal Chemistry, 60(15), 6704-6720. AMER CHEMICAL SOC
Journal of Medicinal Chemistry
Journal of Medicinal Chemistry, 60(15), 6704-6720

We report the synthesis and biological evaluation of a series of 7-aryl-1,2,4-triazolo[4,3-a]pyridines with mGlu2 positive allosteric modulator (PAM) activity and affinity. Besides traditional in vitro parameters of potency and affinity, kinetic para

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fbf3f2fdcd3f801936cef0c1df484262
http://hdl.handle.net/1887/55826

Multiple Binding Sites for Small Molecule Antagonists at the Chemokine Receptor CCR2

Autor: Maarten L. J. Doornbos, Annelien J.M. Zweemer, Dean Stamos, Hilde Vrieling, Jeffrey Abt, John Saunders, Indira Nederpelt, Sarah Hafith, Henk de Vries, Laura H. Heitman, Martine J. Smit, Raymond S. Gross, Adriaan P. IJzerman

Publikováno v: Molecular Pharmacology, 2013(84), 551-561. American Society for Pharmacology and Experimental Therapeutics
Zweemer, A J, Nederpelt, I, Vrieling, H, Hafith, S, Doornbos, M L, de Vries, H, Abt, J, Gross, R, Stamos, D, Saunders, J, Smit, M J, IJzerman, A P & Heitman, L H 2013, ' Multiple Binding Sites for Small Molecule Antagonists at the Chemokine Receptor CCR2 ', Molecular Pharmacology, vol. 2013, no. 84, pp. 551-561 . https://doi.org/10.1124/mol.113.086850

The chemokine receptor CCR2 is a G protein-coupled receptor that is activated primarily by the endogenous CC chemokine ligand 2 (CCL2). Many different small-molecule antagonists have been developed to inhibit this receptor, as it is involved in a var

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::876056dc6ab3615ab4c65f282a968413
https://doi.org/10.1124/mol.113.086850