Glepaglutide, a novel glucagon-like peptide-2 agonist, has anti-inflammatory and mucosal regenerative effects in an experimental model of inflammatory bowel disease in rats

Autor: Jolanta Skarbaliene, Jesper Mosolff Mathiesen, Bjarne Due Larsen, Christian Thorkildsen, Yvette Miata Petersen

Publikováno v: BMC Gastroenterology, Vol 23, Iss 1, Pp 1-9 (2023)

Abstract Background Glucagon-like peptide-2 (GLP-2) enhances intestinal repair and attenuates inflammation in preclinical inflammatory bowel disease (IBD) models, making GLP-2 analogues attractive candidates for IBD therapy. Glepaglutide is a long-ac

Externí odkaz: https://doaj.org/article/914d3c0bb5004d14a880381ddc36d5ff

Asymmetric activation of the calcium-sensing receptor homodimer

Autor: Sabrina N. Rahman, Michael J. Robertson, Alpay B. Seven, Fadil M. Hannan, Jesper Mosolff Mathiesen, Ouliana Panova, Rajesh V. Thakker, Yang Gao, Georgios Skiniotis, Chensong Zhang, Hans Bräuner-Osborne, Justin G. Meyerowitz

Publikováno v: Nature
Gao, Y, Robertson, M J, Rahman, S N, Seven, A B, Zhang, C, Meyerowitz, J G, Panova, O, Hannan, F M, Thakker, R V, Bräuner-Osborne, H, Mathiesen, J M & Skiniotis, G 2021, ' Asymmetric activation of the calcium-sensing receptor homodimer ', Nature, vol. 595, pp. 455-459 . https://doi.org/10.1038/s41586-021-03691-0

The calcium-sensing receptor (CaSR), a cell-surface sensor for Ca2+, is the master regulator of calcium homeostasis in humans and is the target of calcimimetic drugs for the treatment of parathyroid disorders1. CaSR is a family C G-protein-coupled re

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::693269c2b2519871c36c0a6e7ce0ec82
https://ora.ox.ac.uk/objects/uuid:6e7ae25a-1ba1-481e-9597-baf8358fcfc7

Probing the Existence of a Metastable Binding Site at the β2-Adrenergic Receptor with Homobivalent Bitopic Ligands

Autor: Kira Røpke Jørgensen, David E. Gloriam, Jesper Mosolff Mathiesen, Mikael Frykman, Daniel Sejer Pedersen, Emil Märcher-Rørsted, Henrik Johansson, Tomasz M. Wróbel, Mia Danielsen, Hans Bräuner-Osborne, Birgit I. Gaiser

Publikováno v: Journal of Medicinal Chemistry. 62:7806-7839

Herein, we report the development of bitopic ligands aimed at targeting the orthosteric binding site (OBS) and a metastable binding site (MBS) within the same receptor unit. Previous molecular dynamics studies on ligand binding to the β2-adrenergic

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::2f266c9b44be06ae8c41471ac2e4cba3
https://doi.org/10.1021/acs.jmedchem.9b00595

Structural insights into differences in G protein activation by family A and family B GPCRs

Autor: Lise Giehm, Asuka Inoue, Michael T. Lerch, Hongli Hu, Evan S. O'Brien, Mie Fabricius Pedersen, Kaavya Krishna Kumar, Gozde Eskici, Brian K. Kobilka, Georgios Skiniotis, Christine Jennings, Daniel Hilger, Jesper Mosolff Mathiesen

Publikováno v: Hilger, D, Kumar, K K, Hu, H, Pedersen, M F, O'Brien, E S, Giehm, L, Jennings, C, Eskici, G, Inoue, A, Lerch, M, Mathiesen, J M, Skiniotis, G & Kobilka, B K 2020, ' Structural insights into differences in G protein activation by family A and family B GPCRs ', Science, vol. 369, no. 6503 . https://doi.org/10.1126/science.aba3373

INTRODUCTIONTransmembrane signaling of heterotrimeric guanine nucleotide–binding protein (G protein)–coupled receptors (GPCRs) is mediated by ligand-dependent conformational changes that are transmitted from the extracellular ligand binding site

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::18b6bb82af914b1a42575b0409d28eeb
https://doi.org/10.1126/science.aba3373

Dissecting the roles of GRK2 and GRK3 in μ-opioid receptor internalization and β-arrestin2 recruitment using CRISPR/Cas9-edited HEK293 cells

Autor: Jesper Mosolff Mathiesen, Sofie D. Seiersen, Jeffrey R. van Senten, Mie Fabricius Pedersen, Hans Bräuner-Osborne, Michel Bouvier, Thor C. Møller

Publikováno v: Møller, T C, Pedersen, M F, van Senten, J R, Seiersen, S D, Mathiesen, J M, Bouvier, M & Bräuner-Osborne, H 2020, ' Dissecting the roles of GRK2 and GRK3 in μ-opioid receptor internalization and β-arrestin2 recruitment using CRISPR/Cas9-edited HEK293 cells ', Scientific Reports, vol. 10, no. 1, 17395 . https://doi.org/10.1038/s41598-020-73674-0
Scientific Reports
Scientific Reports, Vol 10, Iss 1, Pp 1-13 (2020)

Most G protein-coupled receptors (GPCRs) recruit β-arrestins and internalize upon agonist stimulation. For the μ-opioid receptor (μ-OR), this process has been linked to development of opioid tolerance. GPCR kinases (GRKs), particularly GRK2 and GR

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e97ca6d627bac5187dc196269597fae4
https://curis.ku.dk/ws/files/251408173/OA_Dissecting_the_roles_ofGRK2.pdf