Structure-Activity Study of Dihydrocinnamic Acids and Discovery of the Potent FFA1 (GPR40) Agonist TUG-469. - Test2 - elhamkhani - TriplyDB

Structure-Activity Study of Dihydrocinnamic Acids and Discovery of the Potent FFA1 (GPR40) Agonist TUG-469.

Structure-Activity Study of Dihydrocinnamic Acids and Discovery of the Potent FFA1 (GPR40) Agonist TUG-469.

http://www.wikidata.org/entity/Q39158059

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 Indomethacin treatment prevents high fat diet-induced obesity and insulin resistance but not glucose intolerance in C57BL/6J mice.Discovery of DS-1558: A Potent and Orally Bioavailable GPR40 Agonist Making Dimethylamino a Transformable Directing Group by Nickel-Catalyzed C-N Borylation.Reevaluation of fatty acid receptor 1 as a drug target for the stimulation of insulin secretion in humans.Characterizing 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.In vitro and mouse in vivo characterization of the potent free fatty acid 1 receptor agonist TUG-469.Free Fatty Acid Receptor 1 (FFAR1) as an Emerging Therapeutic Target for Type 2 Diabetes Mellitus: Recent Progress and Prevailing Challenges.Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist.Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles.Improving the Pharmacokinetics of GPR40/FFA1 Full Agonists Discovery of TUG-770: A Highly Potent Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes.Short-chain free fatty acid receptors FFA2/GPR43 and FFA3/GPR41 as new potential therapeutic targets.SAR Studies of Indole-5-propanoic Acid Derivatives To Develop Novel GPR40 Agonists.Structural basis for the agonist action at free fatty acid receptor 1 (FFA1R or GPR40).Design and Synthesis of Novel, Selective GPR40 AgoPAMs.Ligands at Free Fatty Acid Receptor 1 (GPR40).Palmitate and insulin counteract glucose-induced thioredoxin interacting protein (TXNIP) expression in insulin secreting cells via distinct mechanisms.

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Structure-Activity Study of Dihydrocinnamic Acids and Discovery of the Potent FFA1 (GPR40) Agonist TUG-469.

http://www.wikidata.org/entity/Q39158059

description

2010 nî lūn-bûn

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2010年の論文

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2010年論文

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2010年論文

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2010年論文

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2010年論文

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2010年論文

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2010年论文

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2010年论文

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2010年论文

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name

Structure-Activity Study of Di ...... FFA1 (GPR40) Agonist TUG-469.

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Structure-Activity Study of Dihydrocinnamic Acids and Discovery of the Potent FFA1

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type

label

Structure-Activity Study of Di ...... FFA1 (GPR40) Agonist TUG-469.

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Structure-Activity Study of Dihydrocinnamic Acids and Discovery of the Potent FFA1

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Structure-Activity Study of Di ...... FFA1 (GPR40) Agonist TUG-469.

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Structure-Activity Study of Dihydrocinnamic Acids and Discovery of the Potent FFA1

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P1433

ACS Medicinal Chemistry Letters

P1476

Structure-Activity Study of Di ...... t FFA1 (GPR40) Agonist TUG-469

@en

P2093

Alexandra Hamacher

http://www.w3.org/2001/XMLSchema#string

Christel Drewke

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Christian Urban

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Evi Kostenis

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Johannes Schmidt

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Karsten Kristiansen

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Kasper K Karlsen

http://www.w3.org/2001/XMLSchema#string

Maria E Due-Hansen

http://www.w3.org/2001/XMLSchema#string

Matthias U Kassack

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Mette Steensgaard

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P2860

The orphan G protein-coupled receptor GPR40 is activated by medium and long chain fatty acids.

A human cell surface receptor activated by free fatty acids and thiazolidinedione drugs.

Free fatty acids regulate insulin secretion from pancreatic beta cells through GPR40.

GPR40 is necessary but not sufficient for fatty acid stimulation of insulin secretion in vivo.

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

Overexpression of GPR40 in pancreatic beta-cells augments glucose-stimulated insulin secretion and improves glucose tolerance in normal and diabetic mice.

Ligand efficiency: a useful metric for lead selection

Synthesis and biological evaluation of 3-aryl-3-(4-phenoxy)-propionic acid as a novel series of G protein-coupled receptor 40 agonists.

Selective small-molecule agonists of G protein-coupled receptor 40 promote glucose-dependent insulin secretion and reduce blood glucose in mice

The fatty acid receptor GPR40 plays a role in insulin secretion in vivo after high-fat feeding.

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345-349

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scholarly article

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10.1021/ML100106C

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7

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1

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Elisabeth Rexen Ulven

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2010-07-02T00:00:00Z

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24900217

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4007913

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