Selective small-molecule agonists of G protein-coupled receptor 40 promote glucose-dependent insulin secretion and reduce blood glucose in mice
about
A novel antidiabetic drug, fasiglifam/TAK-875, acts as an ago-allosteric modulator of FFAR1Membrane Potential and Calcium Dynamics in Beta Cells from Mouse Pancreas Tissue Slices: Theory, Experimentation, and AnalysisThe action and mode of binding of thiazolidinedione ligands at free fatty acid receptor 1Overexpression of GPR40 in pancreatic beta-cells augments glucose-stimulated insulin secretion and improves glucose tolerance in normal and diabetic mice.DC260126: a small-molecule antagonist of GPR40 that protects against pancreatic β-Cells dysfunction in db/db miceA Single Amino Acid Mutation (R104P) in the E/DRY Motif of GPR40 Impairs Receptor FunctionAMG 837: a novel GPR40/FFA1 agonist that enhances insulin secretion and lowers glucose levels in rodentsInvestigational anti-hyperglycemic agents: the future of type 2 diabetes therapy?An islet in distress: β cell failure in type 2 diabetes.Glucolipotoxicity of the pancreatic beta cell.GPR40 partial agonist MK-2305 lower fasting glucose in the Goto Kakizaki rat via suppression of endogenous glucose production.Lipid receptors and islet function: therapeutic implications?Downregulation of carnitine acyl-carnitine translocase by miRNAs 132 and 212 amplifies glucose-stimulated insulin secretionA potent class of GPR40 full agonists engages the enteroinsular axis to promote glucose control in rodents.Incretin-like effects of small molecule trace amine-associated receptor 1 agonists.Treatment with CNX-011-67, a novel GPR40 agonist, delays onset and progression of diabetes and improves beta cell preservation and function in male ZDF ratsDiscovery of DS-1558: A Potent and Orally Bioavailable GPR40 AgonistGlucolipotoxicity in Pancreatic β-Cells.Exogenous insulin enhances glucose-stimulated insulin response in healthy humans independent of changes in free fatty acids.Identification and pharmacological characterization of multiple allosteric binding sites on the free fatty acid 1 receptorThe fatty acid receptor GPR40 plays a role in insulin secretion in vivo after high-fat feeding.Lack of FFAR1/GPR40 does not protect mice from high-fat diet-induced metabolic disease.Pancreatic β-cell response to increased metabolic demand and to pharmacologic secretagogues requires EPAC2ATwo arginine-glutamate ionic locks near the extracellular surface of FFAR1 gate receptor activation.GPR40: good cop, bad cop?Drugs or diet?--Developing novel therapeutic strategies targeting the free fatty acid family of GPCRsDeletion of GPR40 impairs glucose-induced insulin secretion in vivo in mice without affecting intracellular fuel metabolism in islets.Progress in the discovery and development of small-molecule modulators of G-protein-coupled receptor 40 (GPR40/FFA1/FFAR1): an emerging target for type 2 diabetes.Agonism and allosterism: the pharmacology of the free fatty acid receptors FFA2 and FFA3.Gastrointestinal targets to modulate satiety and food intake.Diabetes area participation analysis: a review of companies and targets described in the 2008 - 2010 patent literature.Minireview: The effects of species ortholog and SNP variation on receptors for free fatty acids.Activation of GPR40 as a therapeutic target for the treatment of type 2 diabetes.GPR40 agonists for the treatment of type 2 diabetes: life after 'TAKing' a hit.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.PPARγ signaling and emerging opportunities for improved therapeutics.For Better or Worse: FFAR1 and FFAR4 Signaling in Cancer and Diabetes.In vitro and mouse in vivo characterization of the potent free fatty acid 1 receptor agonist TUG-469.
P2860
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P2860
Selective small-molecule agonists of G protein-coupled receptor 40 promote glucose-dependent insulin secretion and reduce blood glucose in mice
description
2008 nî lūn-bûn
@nan
2008年の論文
@ja
2008年論文
@yue
2008年論文
@zh-hant
2008年論文
@zh-hk
2008年論文
@zh-mo
2008年論文
@zh-tw
2008年论文
@wuu
2008年论文
@zh
2008年论文
@zh-cn
name
Selective small-molecule agoni ...... d reduce blood glucose in mice
@ast
Selective small-molecule agoni ...... d reduce blood glucose in mice
@en
type
label
Selective small-molecule agoni ...... d reduce blood glucose in mice
@ast
Selective small-molecule agoni ...... d reduce blood glucose in mice
@en
prefLabel
Selective small-molecule agoni ...... d reduce blood glucose in mice
@ast
Selective small-molecule agoni ...... d reduce blood glucose in mice
@en
P2093
P2860
P356
P1433
P1476
Selective small-molecule agoni ...... d reduce blood glucose in mice
@en
P2093
Aleksandr Petrov
Andrew D Howard
Carina P Tan
Changyou Zhou
George J Eiermann
Gino Salituro
Joel P Berger
Monica Einstein
Nancy A Thornberry
P2860
P304
P356
10.2337/DB08-0130
P407
P577
2008-05-13T00:00:00Z