Identification and pharmacological characterization of multiple allosteric binding sites on the free fatty acid 1 receptor
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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 FFAR1Lipotoxicity in the pancreatic beta cell: not just survival and function, but proliferation as well?The Concise Guide to PHARMACOLOGY 2013/14: G protein-coupled receptorsGPR40 partial agonist MK-2305 lower fasting glucose in the Goto Kakizaki rat via suppression of endogenous glucose production.A potent class of GPR40 full agonists engages the enteroinsular axis to promote glucose control in rodents.GPR40 (FFAR1) - Combined Gs and Gq signaling in vitro is associated with robust incretin secretagogue action ex vivo and in vivoFree fatty acid receptors: structural models and elucidation of ligand binding interactions.Drugs or diet?--Developing novel therapeutic strategies targeting the free fatty acid family of GPCRsCharacterizing pharmacological ligands to study the long-chain fatty acid receptors GPR40/FFA1 and GPR120/FFA4.Treatment of type 2 diabetes by free Fatty Acid receptor agonists.GPR40 agonists for the treatment of type 2 diabetes: life after 'TAKing' a hit.Molecular mechanisms of target recognition by lipid GPCRs: relevance for cancer.Basal hypersecretion of glucagon and insulin from palmitate-exposed human islets depends on FFAR1 but not decreased somatostatin secretionThe Role and Future of FFA1 as a Therapeutic Target.Free fatty acid receptor agonists for the treatment of type 2 diabetes: drugs in preclinical to phase II clinical development.β-Arrestin Recruitment and Biased Agonism at Free Fatty Acid Receptor 1.GPR40 reduces food intake and body weight through GLP-1.Allosteric communication pipelines in G-protein-coupled receptors.Key Questions for Translation of FFA Receptors: From Pharmacology to Medicines.Gut Hormone Regulation and Secretion via FFA1 and FFA4.Free Fatty Acid Receptor 1 (FFAR1) as an Emerging Therapeutic Target for Type 2 Diabetes Mellitus: Recent Progress and Prevailing Challenges.Application of GPCR Structures for Modelling of Free Fatty Acid Receptors.Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles.Pharmacological properties of acid N-thiazolylamide FFA2 agonists.Vascular, but not luminal, activation of FFAR1 (GPR40) stimulates GLP-1 secretion from isolated perfused rat small intestine.GPR40 partial agonists and AgoPAMs: Differentiating effects on glucose and hormonal secretions in the rodent.Quercetin/oleic acid-based G-protein-coupled receptor 40 ligands as new insulin secretion modulators.Identification of Two Distinct Sites for Antagonist and Biased Agonist Binding to the Human Chemokine Receptor CXCR3.Structural basis for the cooperative allosteric activation of the free fatty acid receptor GPR40.Design and Synthesis of Novel, Selective GPR40 AgoPAMs.Using Biosensors to Study Free Fatty Acid Receptor Pharmacology and Function.Ligands at Free Fatty Acid Receptor 1 (GPR40).G-protein-coupled receptors for free fatty acids: nutritional and therapeutic targets.Structural basis for GPR40 allosteric agonism and incretin stimulation.Dissecting the Physiology and Pathophysiology of Glucagon-Like Peptide-1
P2860
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P2860
Identification and pharmacological characterization of multiple allosteric binding sites on the free fatty acid 1 receptor
description
2012 nî lūn-bûn
@nan
2012年の論文
@ja
2012年学术文章
@wuu
2012年学术文章
@zh-cn
2012年学术文章
@zh-hans
2012年学术文章
@zh-my
2012年学术文章
@zh-sg
2012年學術文章
@yue
2012年學術文章
@zh
2012年學術文章
@zh-hant
name
Identification and pharmacolog ...... the free fatty acid 1 receptor
@ast
Identification and pharmacolog ...... the free fatty acid 1 receptor
@en
type
label
Identification and pharmacolog ...... the free fatty acid 1 receptor
@ast
Identification and pharmacolog ...... the free fatty acid 1 receptor
@en
prefLabel
Identification and pharmacolog ...... the free fatty acid 1 receptor
@ast
Identification and pharmacolog ...... the free fatty acid 1 receptor
@en
P2093
P2860
P356
P1476
Identification and pharmacolog ...... the free fatty acid 1 receptor
@en
P2093
Daniel C-H Lin
Gayathri Swaminath
Jane Zhang
Jonathan Houze
Kathy Nguyen
Marc Vimolratana
Michael Chen
Nigel J M Birdsall
Paul J Dransfield
P2860
P304
P356
10.1124/MOL.112.079640
P577
2012-08-02T00:00:00Z