G protein-coupled receptor GPR35 suppresses lipid accumulation in hepatocytes

Autor: Susanna Engberg, Amanda E. Mackenzie, Li-Chiung Lin, Graeme Milligan, Andrew B. Tobin, Tezz Quon

Although prevalent, nonalcoholic fatty liver disease is not currently treated effectively with medicines. Initially, using wild-type and genome-edited clones of the human hepatocyte cell line HepG2, we show that activation of the orphan G protein-cou

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9e1fcdf62b9b331df14fdf6a87f0bf45
https://eprints.gla.ac.uk/258956/3/258956.pdf

Structure-Activity Relationship Studies of Tetrahydroquinolone Free Fatty Acid Receptor 3 Modulators

Autor: Anders Højgaard Hansen, Elisabeth Rexen Ulven, Natasja Barki, Graeme Milligan, Tezz Quon, Trond Ulven, Matjaz Brvar, Brian D. Hudson, Christine J. McKenzie, Palash Dutta, Andrew B. Tobin, Eugenia Sergeev, Line Ørsted Bielefeldt

Publikováno v: Journal of Medicinal Chemistry
Ulven, E R, Quon, T, Sergeev, E, Barki, N, Brvar, M, Hudson, B D, Dutta, P, Hansen, A H, Bielefeldt, L Ø, Tobin, A B, McKenzie, C J, Milligan, G & Ulven, T 2020, ' Structure-Activity Relationship Studies of Tetrahydroquinolone Free Fatty Acid Receptor 3 Modulators ', Journal of Medicinal Chemistry, vol. 63, no. 7, pp. 3577-3595 . https://doi.org/10.1021/acs.jmedchem.9b02036
Ulven, E R, Quon, T, Sergeev, E, Barki, N, Brvar, M, Hudson, B D, Dutta, P, Hansen, A H, Bielefeldt, L, Tobin, A B, McKenzie, C J, Milligan, G & Ulven, T 2020, ' Structure-Activity Relationship Studies of Tetrahydroquinolone Free Fatty Acid Receptor 3 Modulators ', Journal of Medicinal Chemistry, vol. 63, no. 7, pp. 3577-3595 . https://doi.org/10.1021/acs.jmedchem.9b02036

Free fatty acid receptor 3 (FFA3, previously GPR41) is activated by short-chain fatty acids, mediates health effects of the gut microbiota, and is a therapeutic target for metabolic and inflammatory diseases. The shortage of well-characterized tool c

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e97f1ad2105006673dcf1a65c7bdb907
https://pubmed.ncbi.nlm.nih.gov/32141297

Receptor selectivity between the G proteins Gα

Autor: Amanda E, Mackenzie, Tezz, Quon, Li-Chiung, Lin, Alexander S, Hauser, Laura, Jenkins, Asuka, Inoue, Andrew B, Tobin, David E, Gloriam, Brian D, Hudson, Graeme, Milligan

Publikováno v: The FASEB Journal

Despite recent advances in structural definition of GPCR–G protein complexes, the basis of receptor selectivity between G proteins remains unclear. The Gα12 and Gα13 subtypes together form the least studied group of heterotrimeric G proteins. G p

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::b1b2c8cbcd6d1879a5a6afd26c63fbe8
https://pubmed.ncbi.nlm.nih.gov/30601679

A Hydrogen-Bonded Polar Network in the Core of the Glucagon-Like Peptide-1 Receptor Is a Fulcrum for Biased Agonism: Lessons from Class B Crystal Structures

Autor: Cassandra Koole, John Simms, Arthur Christopoulos, Sebastian G.B. Furness, Laurence J. Miller, Tezz Quon, Denise Wootten, Christopher A. Reynolds, Juan Carlos Mobarec, Patrick M. Sexton, Thomas Coudrat, Kevin J. Smith

The glucagon-like peptide 1 (GLP-1) receptor is a class B G protein-coupled receptor (GPCR) that is a key target for treatments for type II diabetes and obesity. This receptor, like other class B GPCRs, displays biased agonism, though the physiologic

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::35780bef003e54095e99cd96e2dea217
https://europepmc.org/articles/PMC4767408/