Cellular Assay to Study β-Arrestin Recruitment by the Cannabinoid Receptors 1 and 2

Autor: Jara, Bouma, Marjolein, Soethoudt, Noortje, van Gils, Lizi, Xia, Mario, van der Stelt, Laura H, Heitman

Publikováno v: Methods in molecular biology (Clifton, N.J.). 2576:189-199

Cannabinoid receptor 1 (CB1R) and cannabinoid receptor 2 (CB2R) are G protein-coupled receptors (GPCRs) that activate a variety of pathways upon activation by (partial) agonists including the G protein pathway and the recruitment of β-arrestins. Dif

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid_dedup__::4dfdeb7859c910a4d16bcd2d5daf9df7
https://doi.org/10.1007/978-1-0716-2728-0_15

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

Autor: Stephen J. Hill, Lizi Xia, Monica Bouzo-Lorenzo, Adriaan P. IJzerman, Laura H. Heitman, Leigh A. Stoddart, Stephen J. Briddon

Publikováno v: Purinergic Signalling
Purinergic Signalling, 15(2), 139-153

There is a growing interest in understanding the binding kinetics of compounds that bind to G protein-coupled receptors prior to progressing a lead compound into clinical trials. The widely expressed adenosine A3 receptor (A3AR) has been implicated i

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::731cd68b611f897a31af58900a44ab61
https://doi.org/10.1007/s11302-019-09650-9

Sodium Ion Binding Pocket Mutations and Adenosine A2AReceptor Function

Autor: Natalia V. Ortiz Zacarías, Lizi Xia, Raymond C. Stevens, Eelke B. Lenselink, Adriaan P. IJzerman, Laura H. Heitman, Vsevolod Katritch, Hugo Gutiérrez-de-Terán, Arnault Massink

Publikováno v: Mol Pharmacol

Recently we identified a sodium ion binding pocket in a high-resolution structure of the human adenosine A2A receptor. In the present study we explored this binding site through site-directed mutagenesis and molecular dynamics simulations. Amino acid

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d8cc98860c91f30e850dfb065675ade7
https://doi.org/10.1124/mol.114.095737

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

Autor: Jordyn Stuart, Hui Deng, Vincenzo Di Marzo, Marjolein Soethoudt, Andrea Chicca, Jürg Gertsch, Mark Connor, Uwe Grether, Lizi Xia, Christa MacDonald, Elliot D. Mock, Georgios Alachouzos, Pal Pacher, Camille Perret, Henk de Vries, Benno Rothenhäusler, Travis W. Grim, Christoph Ullmer, Juergen Fingerle, Filomena Fezza, Michelle Glass, Mauro Maccarrone, Mario van der Stelt, Marc P. Baggelaar, David B. Finlay, Luciano De Petrocellis, Marianela Dalghi Gens, Laura H. Heitman, Andrea Martella, Aron H. Lichtman, Noortje van Gils, Nicolina Mastrangelo

Publikováno v: Nature Communications, 8, 13958
Nature communications 8 (2017). doi:10.1038/ncomms13958
info:cnr-pdr/source/autori:Soethoudt, Marjolein; Grether, Uwe; Fingerle, Juergen; Grim, Travis W.; Fezza, Filomena; de Petrocellis, Luciano; Ullmer, Christoph; Rothenhausler, Benno; Perret, Camille; van Gils, Noortje; Finlay, David; MacDonald, Christa; Chicca, Andrea; Gens, Marianela Dalghi; Stuart, Jordyn; de Vries, Henk; Mastrangelo, Nicolina; Xia, Lizi; Alachouzos, Georgios; Baggelaar, Marc P.; Martella, Andrea; Mock, Elliot D.; Deng, Hui; Heitman, Laura H.; Connor, Mark; Di Marzo, Vincenzo; Gertsch, Jurg; Lichtman, Aron H.; Maccarrone, Mauro; Pacher, Pal; Glass, Michelle; van der Stelt, Mario/titolo:Cannabinoid CB2 receptor ligand profiling reveals biased signalling and off-target activity/doi:10.1038%2Fncomms13958/rivista:Nature communications/anno:2017/pagina_da:/pagina_a:/intervallo_pagine:/volume:8
Nature Communications
Soethoudt, Marjolein; Grether, Uwe; Fingerle, Jürgen; Grim, Travis W; Fezza, Filomena; de Petrocellis, Luciano; Ullmer, Christoph; Rothenhäusler, Benno; Perret, Camille; van Gils, Noortje; Finlay, David; MacDonald, Christa; Chicca, Andrea; Gens, Marianela Dalghi; Stuart, Jordyn; de Vries, Henk; Mastrangelo, Nicolina; Xia, Lizi; Alachouzos, Georgios; Baggelaar, Marc P; ... (2017). Cannabinoid CB2 receptor ligand profiling reveals biased signalling and off-target activity. Nature communications, 8(13958), p. 13958. Nature Publishing Group 10.1038/ncomms13958
Nature Communications, Vol 8, Iss 1, Pp 1-14 (2017)

The cannabinoid CB2 receptor (CB2R) represents a promising therapeutic target for various forms of tissue injury and inflammatory diseases. Although numerous compounds have been developed and widely used to target CB2R, their selectivity, molecular m

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b75f8afe19194035304c041481432e51
https://hdl.handle.net/1887/48099

Binding kinetics of ZM241385 derivatives at the human adenosine A(2A) receptor

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

Publikováno v: ChemMedChem, 9(4), 752-761
ChemMedChem

Classical drug design and development rely mostly on affinity- or potency-driven structure-activity relationships (SAR). Thus far, a given compound's binding kinetics have been largely ignored, the importance of which is now being increasingly recogn

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::348d076deea1fea2155e27955b55f3f3
http://hdl.handle.net/1887/3209420