Cargando…

Discovery of TUG-770: A Highly Potent Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes

[Image: see text] Free fatty acid receptor 1 (FFA1 or GPR40) enhances glucose-stimulated insulin secretion from pancreatic β-cells and currently attracts high interest as a new target for the treatment of type 2 diabetes. We here report the discovery of a highly potent FFA1 agonist with favorable ph...

Descripción completa

Detalles Bibliográficos
Autores principales:	Christiansen, Elisabeth, Hansen, Steffen V. F., Urban, Christian, Hudson, Brian D., Wargent, Edward T., Grundmann, Manuel, Jenkins, Laura, Zaibi, Mohamed, Stocker, Claire J., Ullrich, Susanne, Kostenis, Evi, Kassack, Matthias U., Milligan, Graeme, Cawthorne, Michael A., Ulven, Trond
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	American Chemical Society 2013
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3654565/ https://www.ncbi.nlm.nih.gov/pubmed/23687558 http://dx.doi.org/10.1021/ml4000673

Ejemplares similares

Selective Orthosteric Free Fatty Acid Receptor 2 (FFA2) Agonists: IDENTIFICATION OF THE STRUCTURAL AND CHEMICAL REQUIREMENTS FOR SELECTIVE ACTIVATION OF FFA2 VERSUS FFA3
por: Schmidt, Johannes, et al.
Publicado: (2011)

The Molecular Basis of Ligand Interaction at Free Fatty Acid Receptor 4 (FFA4/GPR120)
por: Hudson, Brian D., et al.
Publicado: (2014)

Short-chain free fatty acid receptors FFA2/GPR43 and FFA3/GPR41 as new potential therapeutic targets
por: Ulven, Trond
Publicado: (2012)

FFA2-, but not FFA3-agonists inhibit GSIS of human pseudoislets: a comparative study with mouse islets and rat INS-1E cells
por: Lorza-Gil, Estela, et al.
Publicado: (2020)

Extracellular Ionic Locks Determine Variation in Constitutive Activity and Ligand Potency between Species Orthologs of the Free Fatty Acid Receptors FFA2 and FFA3
por: Hudson, Brian D., et al.
Publicado: (2012)

FFA4/GPR120: Pharmacology and Therapeutic Opportunities
por: Milligan, Graeme, et al.
Publicado: (2017)

Chemically engineering ligand selectivity at the free fatty acid receptor 2 based on pharmacological variation between species orthologs
por: Hudson, Brian D., et al.
Publicado: (2012)

Glucose-stimulated insulin secretion depends on FFA1 and Gq in neonatal mouse islets
por: Lorza-Gil, Estela, et al.
Publicado: (2023)

Concomitant Action of Structural Elements and Receptor Phosphorylation Determines Arrestin-3 Interaction with the Free Fatty Acid Receptor FFA4
por: Butcher, Adrian J., et al.
Publicado: (2014)

Leanness and Low Plasma Leptin in GPR17 Knockout Mice Are Dependent on Strain and Associated With Increased Energy Intake That Is Not Suppressed by Exogenous Leptin
por: Wargent, Edward T., et al.
Publicado: (2021)

Defining the Molecular Basis for the First Potent and Selective Orthosteric Agonists of the FFA2 Free Fatty Acid Receptor
por: Hudson, Brian D., et al.
Publicado: (2013)

Probe-Dependent Negative Allosteric Modulators of the Long-Chain Free Fatty Acid Receptor FFA4
por: Watterson, Kenneth R., et al.
Publicado: (2017)

Three classes of ligands each bind to distinct sites on the orphan G protein-coupled receptor GPR84
por: Mahmud, Zobaer Al, et al.
Publicado: (2017)

Allosteric targeting of the FFA2 receptor (GPR43) restores responsiveness of desensitized human neutrophils
por: Frei, Robert, et al.
Publicado: (2020)

Reevaluation of Fatty Acid Receptor 1 as a Drug Target for the Stimulation of Insulin Secretion in Humans
por: Wagner, Robert, et al.
Publicado: (2013)

High fat-fed GPR55 null mice display impaired glucose tolerance without concomitant changes in energy balance or insulin sensitivity but are less responsive to the effects of the cannabinoids rimonabant or Δ(9)-tetrahydrocannabivarin on weight gain
por: Wargent, Edward T., et al.
Publicado: (2020)

The Specificity and Broad Multitarget Properties of Ligands for the Free Fatty Acid Receptors FFA3/GPR41 and FFA2/GPR43 and the Related Hydroxycarboxylic Acid Receptor HCA2/GPR109A
por: Bisenieks, Egils, et al.
Publicado: (2021)

The GPR120 agonist TUG‐891 promotes metabolic health by stimulating mitochondrial respiration in brown fat
por: Schilperoort, Maaike, et al.
Publicado: (2018)

Treatment of Type 2 Diabetes by Free Fatty Acid Receptor Agonists
por: Watterson, Kenneth R., et al.
Publicado: (2014)

Evidence from studies in rodents and in isolated adipocytes that agonists of the chemerin receptor CMKLR1 may be beneficial in the treatment of type 2 diabetes
por: Wargent, Edward T., et al.
Publicado: (2015)

GPR55: signaling pathways and functions
por: Balenga, Nariman, et al.
Publicado: (2009)

Polyunsaturated fatty acid receptors, GPR40 and GPR120, are expressed in the hypothalamus and control energy homeostasis and inflammation
por: Dragano, Nathalia R. V., et al.
Publicado: (2017)

Development of Free Fatty Acid Receptor 4 (FFA4/GPR120) Agonists in Health Science
por: Son, So-Eun, et al.
Publicado: (2021)

The cannabinoid Δ(9)-tetrahydrocannabivarin (THCV) ameliorates insulin sensitivity in two mouse models of obesity
por: Wargent, E T, et al.
Publicado: (2013)

Label-free cell phenotypic study of FFA4 and FFA1 and discovery of novel agonists of FFA4 from natural products
por: Xu, Fangfang, et al.
Publicado: (2019)

Novel FFA1 (GPR40) agonists containing spirocyclic periphery: polar azine periphery as a driver of potency
por: Krasavin, Mikhail, et al.
Publicado: (2016)

Therapeutic validation of an orphan G protein‐coupled receptor: The case of GPR84
por: Marsango, Sara, et al.
Publicado: (2020)

Chemogenetics defines a short-chain fatty acid receptor gut–brain axis
por: Barki, Natasja, et al.
Publicado: (2022)

The GPR120 Agonist TUG-891 Inhibits the Motility and Phagocytosis of Mouse Alveolar Macrophages
por: Su, Xing-Li, et al.
Publicado: (2020)

Agonist-induced phosphorylation of orthologues of the orphan receptor GPR35 functions as an activation sensor
por: Divorty, Nina, et al.
Publicado: (2022)

Antagonism of the prostaglandin D(2 )receptor CRTH2 attenuates asthma pathology in mouse eosinophilic airway inflammation
por: Uller, Lena, et al.
Publicado: (2007)

AMG 837: A Novel GPR40/FFA1 Agonist that Enhances Insulin Secretion and Lowers Glucose Levels in Rodents
por: Lin, Daniel C.-H., et al.
Publicado: (2011)

Increased whole blood FFA2/GPR43 receptor expression is associated with increased 30-day survival in patients with sepsis
por: Carr, Zyad J., et al.
Publicado: (2018)

Delphinidin Reduces Glucose Uptake in Mice Jejunal Tissue and Human Intestinal Cells Lines through FFA1/GPR40
por: Hidalgo, Jorge, et al.
Publicado: (2017)

Discovery of GPR183 Agonists Based on an Antagonist Scaffold
por: Kjær, Viktoria M. S., et al.
Publicado: (2021)

PGH(1), the Precursor for the Anti-Inflammatory Prostaglandins of the 1-series, Is a Potent Activator of the Pro-Inflammatory Receptor CRTH2/DP2
por: Schröder, Ralf, et al.
Publicado: (2012)

Non-equivalence of Key Positively Charged Residues of the Free Fatty Acid 2 Receptor in the Recognition and Function of Agonist Versus Antagonist Ligands
por: Sergeev, Eugenia, et al.
Publicado: (2016)

Discovery of Potent Tetrazole Free Fatty Acid Receptor 2 Antagonists
por: Valentini, Alice, et al.
Publicado: (2023)

G protein‐coupled receptors not currently in the spotlight: free fatty acid receptor 2 and GPR35
por: Milligan, Graeme
Publicado: (2017)

Long Chain Fatty Acids as Modulators of Immune Cells Function: Contribution of FFA1 and FFA4 Receptors
por: Hidalgo, Maria A., et al.
Publicado: (2021)

Cannot write session to /tmp/vufind_sessions/sess_5rjka9lggs8op0kcm689v54s9t