Discovery of the First Highly Selective Antagonist of the GluK3 Kainate Receptor Subtype

Autor: Paulina Chałupnik, Alina Vialko, Darryl S. Pickering, Markus Hinkkanen, Stephanie Donbosco, Thor C. Møller, Anders A. Jensen, Birgitte Nielsen, Yasmin Bay, Anders S. Kristensen, Tommy N. Johansen, Kamil Łątka, Marek Bajda, Ewa Szymańska

Publikováno v: International Journal of Molecular Sciences, Vol 23, Iss 15, p 8797 (2022)

Kainate receptors belong to the family of glutamate receptors ion channels, which are responsible for the majority of rapid excitatory synaptic transmission in the central nervous system. The therapeutic potential of kainate receptors is still poorly

Externí odkaz: https://doaj.org/article/41bc4f7161f44d6e92ef3e5cfa67ab09

Pharmacological evidence for a metabotropic glutamate receptor heterodimer in neuronal cells

Autor: David Moreno Delgado, Thor C Møller, Jeanne Ster, Jesús Giraldo, Damien Maurel, Xavier Rovira, Pauline Scholler, Jurriaan M Zwier, Julie Perroy, Thierry Durroux, Eric Trinquet, Laurent Prezeau, Philippe Rondard, Jean-Philippe Pin

Publikováno v: eLife, Vol 6 (2017)

Metabotropic glutamate receptors (mGluRs) are mandatory dimers playing important roles in regulating CNS function. Although assumed to form exclusive homodimers, 16 possible heterodimeric mGluRs have been proposed but their existence in native cells

Externí odkaz: https://doaj.org/article/45f8031aa1ce42f587b4ebe1846baae1

GLP-1 Val8: A Biased GLP-1R Agonist with Altered Binding Kinetics and Impaired Release of Pancreatic Hormones in Rats

Autor: Sine P. Schiellerup, Gertrud Malene Hjortø, Mette M. Rosenkilde, Florent Xavier Smit, Olav Larsen, Bolette Hartmann, Thor C. Møller, C. Christiansen, Jens J. Holst, Wijnand J.C. van der Velden, Hans Bräuner-Osborne, Thomas M. Frimurer

Publikováno v: ACS Pharmacol Transl Sci

[Image: see text] Biased ligands that selectively confer activity in one pathway over another are pharmacologically important because biased signaling may reduce on-target side effects and improve drug efficacy. Here, we describe an N-terminal modifi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8c1b2b60a588622bae14728766e1f217
https://doi.org/10.1021/acsptsci.0c00193

Use of CRISPR/Cas9-edited HEK293 cells reveals that both conventional and novel protein kinase C isozymes are involved in mGlu

Autor: Jeffrey R, van Senten, Thor C, Møller, Ee Von, Moo, Sofie D, Seiersen, Hans, Bräuner-Osborne

Publikováno v: The Journal of biological chemistry. 298(10)

The internalization of G protein-coupled receptors (GPCRs) can be regulated by PKC. However, most tools available to study the contribution of PKC isozymes have considerable limitations, including a lack of selectivity. In this study, we generated an

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::37c6fabe3005ac52426425b58f23519a
https://pubmed.ncbi.nlm.nih.gov/36087841

GRK2 selectively attenuates the neutrophil NADPH-oxidase response triggered by β-arrestin recruiting GPR84 agonists

Autor: Johanna Fredriksson, André Holdfeldt, Jonas Mårtensson, Lena Björkman, Thor C. Møller, Erik Müllers, Claes Dahlgren, Martina Sundqvist, Huamei Forsman

Publikováno v: Fredriksson, J, Holdfeldt, A, Mårtensson, J, Björkman, L, Møller, T C, Müllers, E, Dahlgren, C, Sundqvist, M & Forsman, H 2022, ' GRK2 selectively attenuates the neutrophil NADPH-oxidase response triggered by β-arrestin recruiting GPR84 agonists ', Biochimica et Biophysica Acta-Molecular Cell Research, vol. 1869, no. 7, 119262 . https://doi.org/10.1016/j.bbamcr.2022.119262

In order to avoid a prolonged pro-inflammatory neutrophil response, signaling downstream of an agonist-activated G protein-coupled receptor (GPCR) has to be rapidly terminated. Among the family of GPCR kinases (GRKs) that regulate receptor phosphoryl

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9325d3857279f1049bf84ea0cf4bb7ed
https://pubmed.ncbi.nlm.nih.gov/35341806