Selective orthosteric free fatty acid receptor 2 (FFA2) agonists: identification of the structural and chemical requirements for selective activation of FFA2 versus FFA3 - Wikidata - awgldk - TriplyDB

Selective orthosteric free fatty acid receptor 2 (FFA2) agonists: identification of the structural and chemical requirements for selective activation of FFA2 versus FFA3

Selective orthosteric free fatty acid receptor 2 (FFA2) agonists: identification of the structural and chemical requirements for selective activation of FFA2 versus FFA3

http://www.wikidata.org/entity/Q33789758

about

Defining the molecular basis for the first potent and selective orthosteric agonists of the FFA2 free fatty acid receptor Pharmacology and physiology of gastrointestinal enteroendocrine cells An Acetate-Specific GPCR, FFAR2, Regulates Insulin Secretion The Concise Guide to PHARMACOLOGY 2013/14: G protein-coupled receptors Free fatty acid receptors: structural models and elucidation of ligand binding interactions.A Novel Allosteric Activator of Free Fatty Acid 2 Receptor Displays Unique Gi-functional Bias Drugs or diet?--Developing novel therapeutic strategies targeting the free fatty acid family of GPCRs The Influence of the Microbiome on Early-Life Severe Viral Lower Respiratory Infections and Asthma-Food for Thought?Low affinity GPCRs for metabolic intermediates: challenges for pharmacologists.Minireview: The effects of species ortholog and SNP variation on receptors for free fatty acids.The therapeutic potential of GPR43: a novel role in modulating metabolic health.Treatment of type 2 diabetes by free Fatty Acid receptor agonists.Free fatty acid receptors as therapeutic targets for the treatment of diabetes.Homology modeling of FFA2 identifies novel agonists that potentiate insulin secretion.The Pharmacology and Function of Receptors for Short-Chain Fatty Acids.Identifying ligands at orphan GPCRs: current status using structure-based approaches.Fatty acid and mineral receptors as drug targets for gastrointestinal disorders.SCFA Receptors in Pancreatic β Cells: Novel Diabetes Targets?A cell-permeable inhibitor to trap Gαq proteins in the empty pocket conformation.Application of GPCR Structures for Modelling of Free Fatty Acid Receptors.A biased ligand for OXE-R uncouples Gα and Gβγ signaling within a heterotrimer.Chemically engineering ligand selectivity at the free fatty acid receptor 2 based on pharmacological variation between species orthologs.Metalloprotease cleavage of the N terminus of the orphan G protein-coupled receptor GPR37L1 reduces its constitutive activity.Non-equivalence of Key Positively Charged Residues of the Free Fatty Acid 2 Receptor in the Recognition and Function of Agonist Versus Antagonist Ligands.Short-chain free fatty acid receptors FFA2/GPR43 and FFA3/GPR41 as new potential therapeutic targets.Extracellular ionic locks determine variation in constitutive activity and ligand potency between species orthologs of the free fatty acid receptors FFA2 and FFA3.Mutation analysis and molecular modeling for the investigation of ligand-binding modes of GPR84.Distinctive microbiomes and metabolites linked with weight loss after gastric bypass, but not gastric banding.Synthesis, Activity, and Docking Study of Novel Phenylthiazole-Carboxamido Acid Derivatives as FFA2 Agonists.SCFAs strongly stimulate PYY production in human enteroendocrine cells.Using Biosensors to Study Free Fatty Acid Receptor Pharmacology and Function.Ligands at the Free Fatty Acid Receptors 2/3 (GPR43/GPR41).Applying label-free dynamic mass redistribution technology to frame signaling of G protein-coupled receptors noninvasively in living cells.G-protein-coupled receptors for free fatty acids: nutritional and therapeutic targets.Microbiome-host systems interactions: protective effects of propionate upon the blood-brain barrier.Label-Free Biosensors for Cell Biology

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P2860

Selective orthosteric free fatty acid receptor 2 (FFA2) agonists: identification of the structural and chemical requirements for selective activation of FFA2 versus FFA3

http://www.wikidata.org/entity/Q33789758

description

2011 nî lūn-bûn

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2011 թուականի Յունուարին հրատարակուած գիտական յօդուած

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2011 թվականի հունվարին հրատարակված գիտական հոդված

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2011年の論文

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2011年論文

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2011年論文

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Selective orthosteric free fat ...... activation of FFA2 versus FFA3

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Selective orthosteric free fat ...... activation of FFA2 versus FFA3

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Selective orthosteric free fat ...... activation of FFA2 versus FFA3

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Selective orthosteric free fat ...... activation of FFA2 versus FFA3

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Selective orthosteric free fat ...... activation of FFA2 versus FFA3

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JBC.M110.210872

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Journal of Biological Chemistry

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Selective orthosteric free fat ...... activation of FFA2 versus FFA3

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Christel Drewke

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Elisabeth Christiansen

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Evi Kostenis

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Graeme Milligan

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Irina G Tikhonova

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Johannes Schmidt

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Manuel Grundmann

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Richard J Ward

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P2860

Conserved polar residues in transmembrane domains V, VI, and VII of free fatty acid receptor 2 and free fatty acid receptor 3 are required for the binding and function of short chain fatty acids

The Orphan G protein-coupled receptors GPR41 and GPR43 are activated by propionate and other short chain carboxylic acids

The maximal affinity of ligands

The action and mode of binding of thiazolidinedione ligands at free fatty acid receptor 1

Identification of a free fatty acid receptor, FFA2R, expressed on leukocytes and activated by short-chain fatty acids

Functional characterization of human receptors for short chain fatty acids and their role in polymorphonuclear cell activation

Molecular identification of high and low affinity receptors for nicotinic acid

PUMA-G and HM74 are receptors for nicotinic acid and mediate its anti-lipolytic effect

Citric acid cycle intermediates as ligands for orphan G-protein-coupled receptors

Regulation of inflammatory responses by gut microbiota and chemoattractant receptor GPR43

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10628-10640

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10.1074/JBC.M110.210872

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