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

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Selective orthosteric free fatty acid receptor 2 (FFA2) agonists: identification of the structural and chemical requirements for selective activation of FFA2 versus FFA3 is …
instance of (P31):
scholarly articleQ13442814

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P356DOI10.1074/JBC.M110.210872
P932PMC publication ID3060514
P698PubMed publication ID21220428

P50authorGraeme MilliganQ28468987
Brian D HudsonQ40356293
Trond UlvenQ40356350
Nicola J SmithQ57199403
P2093author name stringEvi Kostenis
Richard J Ward
Irina G Tikhonova
Christel Drewke
Manuel Grundmann
Johannes Schmidt
Elisabeth Christiansen
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Functional characterization of human receptors for short chain fatty acids and their role in polymorphonuclear cell activationQ28200878
Molecular identification of high and low affinity receptors for nicotinic acidQ28202556
PUMA-G and HM74 are receptors for nicotinic acid and mediate its anti-lipolytic effectQ28206812
Citric acid cycle intermediates as ligands for orphan G-protein-coupled receptorsQ28261556
Regulation of inflammatory responses by gut microbiota and chemoattractant receptor GPR43Q28509150
Ligand efficiency: a useful metric for lead selectionQ29617403
Drugging challenging targets using fragment-based approachesQ30979472
Short-chain fatty acids and human colonic function: roles of resistant starch and nonstarch polysaccharidesQ34294058
Transforming fragments into candidates: small becomes big in medicinal chemistryQ34981076
GPR109A, GPR109B and GPR81, a family of hydroxy-carboxylic acid receptorsQ35008381
The nicotinic acid receptor GPR109A (HM74A or PUMA-G) as a new therapeutic targetQ36502679
Collateral efficacy in drug discovery: taking advantage of the good (allosteric) nature of 7TM receptorsQ36880900
The evasive nature of drug efficacy: implications for drug discoveryQ36894549
Two arginine-glutamate ionic locks near the extracellular surface of FFAR1 gate receptor activation.Q37081904
Functional selectivity in GPCR modulator screeningQ37184786
International Union of Pharmacology. LXXI. Free fatty acid receptors FFA1, -2, and -3: pharmacology and pathophysiological functionsQ37338747
Molecular pharmacology of promiscuous seven transmembrane receptors sensing organic nutrients.Q37504335
Cellular assays as portals to seven-transmembrane receptor-based drug discoveryQ37553926
7TM pharmacology measured by label-free: a holistic approach to cell signallingQ37578079
Agonism and allosterism: the pharmacology of the free fatty acid receptors FFA2 and FFA3.Q37589701
Free fatty acid receptor 2 and nutrient sensing: a proposed role for fibre, fermentable carbohydrates and short-chain fatty acids in appetite regulationQ37756247
When simple agonism is not enough: emerging modalities of GPCR ligands.Q37775132
Deorphanization of GPR109B as a receptor for the beta-oxidation intermediate 3-OH-octanoic acid and its role in the regulation of lipolysisQ39832093
Locating ligand-binding sites in 7TM receptors by protein engineering.Q40535098
The probable arrangement of the helices in G protein-coupled receptors.Q40872681
Identification and functional characterization of allosteric agonists for the G protein-coupled receptor FFA2.Q42808008
The minor binding pocket: a major player in 7TM receptor activationQ42876628
Deconvolution of complex G protein-coupled receptor signaling in live cells using dynamic mass redistribution measurements.Q42937057
Roles of GPR41 and GPR43 in leptin secretory responses of murine adipocytes to short chain fatty acidsQ43095402
G protein-coupled receptor 43 is essential for neutrophil recruitment during intestinal inflammationQ43241053
Molecular mechanism of AMD3100 antagonism in the CXCR4 receptor: transfer of binding site to the CXCR3 receptorQ44636885
Ligand efficiency indices as guideposts for drug discovery.Q55040766
The first synthetic agonists of FFA2: Discovery and SAR of phenylacetamides as allosteric modulatorsQ82219704
A holistic view of GPCR signalingQ85008509
P433issue12
P407language of work or nameEnglishQ1860
P921main subjectfatty acidQ61476
P304page(s)10628-10640
P577publication date2011-01-10
P1433published inJournal of Biological ChemistryQ867727
P1476titleSelective orthosteric free fatty acid receptor 2 (FFA2) agonists: identification of the structural and chemical requirements for selective activation of FFA2 versus FFA3
P478volume286

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