Two arginine-glutamate ionic locks near the extracellular surface of FFAR1 gate receptor activation.
about
High-resolution structure of the human GPR40 receptor bound to allosteric agonist TAK-875A novel antidiabetic drug, fasiglifam/TAK-875, acts as an ago-allosteric modulator of FFAR1Defining the molecular basis for the first potent and selective orthosteric agonists of the FFA2 free fatty acid receptorThe action and mode of binding of thiazolidinedione ligands at free fatty acid receptor 1Comparison of dynamics of extracellular accesses to the β(1) and β(2) adrenoceptors binding sites uncovers the potential of kinetic basis of antagonist selectivity.Rhodopsin and the others: a historical perspective on structural studies of G protein-coupled receptors.Selective orthosteric free fatty acid receptor 2 (FFA2) agonists: identification of the structural and chemical requirements for selective activation of FFA2 versus FFA3Third extracellular loop (EC3)-N terminus interaction is important for seven-transmembrane domain receptor function: implications for an activation microswitch region.Docking-based virtual screening for ligands of G protein-coupled receptors: not only crystal structures but also in silico models.Extracellular loop 2 of the free fatty acid receptor 2 mediates allosterism of a phenylacetamide ago-allosteric modulator.The extracellular loop 2 (ECL2) of the human histamine H4 receptor substantially contributes to ligand binding and constitutive activity.Signaling-sensitive amino acids surround the allosteric ligand binding site of the thyrotropin receptor.Free fatty acid receptors: structural models and elucidation of ligand binding interactions.Free fatty acid receptors: emerging targets for treatment of diabetes and its complications.Identification and pharmacological characterization of multiple allosteric binding sites on the free fatty acid 1 receptorNovel insights on thyroid-stimulating hormone receptor signal transduction.Agonism and allosterism: the pharmacology of the free fatty acid receptors FFA2 and FFA3.Lifting the lid on GPCRs: the role of extracellular loops.Molecular mechanisms of target recognition by lipid GPCRs: relevance for cancer.Free Fatty Acid Receptor 1 (FFAR1) as an Emerging Therapeutic Target for Type 2 Diabetes Mellitus: Recent Progress and Prevailing Challenges.From molecular details of the interplay between transmembrane helices of the thyrotropin receptor to general aspects of signal transduction in family a G-protein-coupled receptors (GPCRs).Extracellular ionic locks determine variation in constitutive activity and ligand potency between species orthologs of the free fatty acid receptors FFA2 and FFA3.Model structures of inactive and peptide agonist bound C5aR: Insights into agonist binding, selectivity and activation.Ligands at Free Fatty Acid Receptor 1 (GPR40).
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P2860
Two arginine-glutamate ionic locks near the extracellular surface of FFAR1 gate receptor activation.
description
article científic
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article scientifique
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articolo scientifico
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artigo científico
@pt
bilimsel makale
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scientific article published on 08 December 2008
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vedecký článok
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vetenskaplig artikel
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videnskabelig artikel
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vědecký článek
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name
Two arginine-glutamate ionic l ...... FAR1 gate receptor activation.
@en
Two arginine-glutamate ionic l ...... FAR1 gate receptor activation.
@nl
type
label
Two arginine-glutamate ionic l ...... FAR1 gate receptor activation.
@en
Two arginine-glutamate ionic l ...... FAR1 gate receptor activation.
@nl
prefLabel
Two arginine-glutamate ionic l ...... FAR1 gate receptor activation.
@en
Two arginine-glutamate ionic l ...... FAR1 gate receptor activation.
@nl
P2093
P2860
P356
P1476
Two arginine-glutamate ionic l ...... FFAR1 gate receptor activation
@en
P2093
Chi Shing Sum
Irina G Tikhonova
Marvin C Gershengorn
P2860
P304
P356
10.1074/JBC.M806987200
P407
P577
2008-12-08T00:00:00Z