Discovery and Characterization of Novel Antagonists of the Proinflammatory Orphan Receptor GPR84

Autor: Irina G. Tikhonova, Graeme Milligan, Andrew B. Tobin, Stuart P. McElroy, Laura Jenkins, Zobaer Al Mahmud, Matt Barnes, Angus Morrison, K.A. Bennett, Sara Marsango, Sarah J. Mancini

Publikováno v: Jenkins, L, Marsango, S, Mancini, S, Mahmud, Z A, Morrison, A, McElroy, S P, Bennett, K A, Barnes, M, Tobin, A B, Tikhonova, I G & Milligan, G 2021, ' Discovery and Characterization of Novel Antagonists of the Proinflammatory Orphan Receptor GPR84 ', ACS Pharmacology & Translational Science . https://doi.org/10.1021/acsptsci.1c00151

GPR84 is a poorly characterized, nominally orphan, proinflammatory G protein-coupled receptor that can be activated by medium chain length fatty acids. It is attracting considerable interest as a potential therapeutic target for antagonist ligands in

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f08cd354d4193cec58f79a1f81831392
https://pubmed.ncbi.nlm.nih.gov/34661077

The Na+/Glucose Cotransporter Inhibitor Canagliflozin Activates AMPK by Inhibiting Mitochondrial Function and Increasing Cellular AMP Levels

Autor: Rebecca J. Ford, Brennan K. Smith, Ian P. Salt, Ryan D. Pitt, Graeme J. Gowans, Gregory R. Steinberg, Sarah J. Mancini, Emily A. Day, D. Grahame Hardie, Simon A. Hawley

Publikováno v: Diabetes. 65:2784-2794

Canagliflozin, dapagliflozin, and empagliflozin, all recently approved for treatment of type 2 diabetes, were derived from the natural product phlorizin. They reduce hyperglycemia by inhibiting glucose reuptake by sodium/glucose cotransporter (SGLT)

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bdb4a02c902e4f2b42acbbc5c3305421
https://doi.org/10.2337/db16-0058

Investigating the Role of AMPK in Inflammation

Autor: Sarah J, Mancini, Ian P, Salt

Publikováno v: Methods in molecular biology (Clifton, N.J.). 1732

In addition to the well-characterized role of AMPK in the regulation of nutrient metabolism, it is increasingly clear that AMPK activation has multiple actions on inflammatory signalling. Here we describe methods to identify effects of AMPK activity

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::97ad9d6a0f1df95e59a9513d31b8b70d
https://pubmed.ncbi.nlm.nih.gov/29480484

Role of AMP-activated protein kinase in adipose tissue metabolism and inflammation

Autor: Sarah J. Mancini, Ian P. Salt, Silvia Bijland

Publikováno v: Clinical Science. 124:491-507

AMPK (AMP-activated protein kinase) is a key regulator of cellular and whole-body energy balance. AMPK phosphorylates and regulates many proteins concerned with nutrient metabolism, largely acting to suppress anabolic ATP-consuming pathways while sti

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ae5ad9370b6aade399bb7d968b378f62
https://doi.org/10.1042/cs20120536

Activation of AMP-activated protein kinase rapidly suppresses multiple pro-inflammatory pathways in adipocytes including IL-1 receptor-associated kinase-4 phosphorylation

Autor: Sarah J, Mancini, Anna D, White, Silvia, Bijland, Claire, Rutherford, Delyth, Graham, Erik A, Richter, Benoit, Viollet, Rhian M, Touyz, Timothy M, Palmer, Ian P, Salt

Publikováno v: Molecular and Cellular Endocrinology

Inflammation of adipose tissue in obesity is associated with increased IL-1β, IL-6 and TNF-α secretion and proposed to contribute to insulin resistance. AMP-activated protein kinase (AMPK) regulates nutrient metabolism and is reported to have anti-

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::e61d5308734c0ee871504343c6607eb6
https://pubmed.ncbi.nlm.nih.gov/27840174