Discovery of TAK-875: A Potent, Selective, and Orally Bioavailable GPR40 Agonist. - Wikidata - awgldk - TriplyDB

Discovery of TAK-875: A Potent, Selective, and Orally Bioavailable GPR40 Agonist.

Discovery of TAK-875: A Potent, Selective, and Orally Bioavailable GPR40 Agonist.

http://www.wikidata.org/entity/Q33558075

about

High-resolution structure of the human GPR40 receptor bound to allosteric agonist TAK-875 A novel antidiabetic drug, fasiglifam/TAK-875, acts as an ago-allosteric modulator of FFAR1 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 AMG 837: a novel GPR40/FFA1 agonist that enhances insulin secretion and lowers glucose levels in rodents A potent class of GPR40 full agonists engages the enteroinsular axis to promote glucose control in rodents.Discontinued in 2013: diabetic drugs.Evaluation of the pharmacokinetics and safety of a single oral dose of fasiglifam in subjects with normal or varying degrees of impaired renal function.GPR40 (FFAR1) - Combined Gs and Gq signaling in vitro is associated with robust incretin secretagogue action ex vivo and in vivo Discovery of DS-1558: A Potent and Orally Bioavailable GPR40 Agonist Differential intracellular calcium influx, nitric oxide production, ICAM-1 and IL8 expression in primary bovine endothelial cells exposed to nonesterified fatty acids Efficacy and safety of fasiglifam (TAK-875), a G protein-coupled receptor 40 agonist, in Japanese patients with type 2 diabetes inadequately controlled by diet and exercise: a randomized, double-blind, placebo-controlled, phase III trial.Randomized, double-blind, dose-ranging study of TAK-875, a novel GPR40 agonist, in Japanese patients with inadequately controlled type 2 diabetes.Pharmacometric Approaches to Guide Dose Selection of the Novel GPR40 Agonist TAK-875 in Subjects With Type 2 Diabetes Mellitus.An Amino-Benzosuberene Analogue That Inhibits Tubulin Assembly and Demonstrates Remarkable Cytotoxicity.Drugs or diet?--Developing novel therapeutic strategies targeting the free fatty acid family of GPCRs Synthesis of structurally diverse benzosuberene analogues and their biological evaluation as anti-cancer agents.Catalytic enantioselective cyclization/cross-coupling with alkyl electrophiles.Minireview: The effects of species ortholog and SNP variation on receptors for free fatty acids.The therapeutic potential of GPR120: a patent review.Fasiglifam as a new potential treatment option for patients with type 2 diabetes.The G-Protein-Coupled Long-Chain Fatty Acid Receptor GPR40 and Glucose Metabolism.Toward molecular imaging of the free fatty acid receptor 1.The 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.Fasiglifam (TAK-875): Mechanistic Investigation and Retrospective Identification of Hazards for Drug Induced Liver Injury.Key Questions for Translation of FFA Receptors: From Pharmacology to Medicines.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.Application of GPCR Structures for Modelling of Free Fatty Acid Receptors.GPR40-induced insulin secretion by the novel agonist TAK-875: first clinical findings in patients with type 2 diabetes.Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist.CoMSIA study on substituted aryl alkanoic acid analogs as GPR40 agonists.Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles.Improving the Pharmacokinetics of GPR40/FFA1 Full Agonists Optimization of GPR40 Agonists for Type 2 Diabetes.Discovery of TUG-770: A Highly Potent Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes.Fasiglifam (TAK-875) Alters Bile Acid Homeostasis in Rats and Dogs: A Potential Cause of Drug Induced Liver Injury Fasiglifam (TAK-875) has dual potentiating mechanisms via Gαq-GPR40/FFAR1 signaling branches on glucose-dependent insulin secretion.

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Discovery of TAK-875: A Potent, Selective, and Orally Bioavailable GPR40 Agonist.

http://www.wikidata.org/entity/Q33558075

description

2010 nî lūn-bûn

@nan

2010 թուականի Յունիսին հրատարակուած գիտական յօդուած

@hyw

2010 թվականի հունիսին հրատարակված գիտական հոդված

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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

@zh-hant

2010年論文

@zh-hk

2010年論文

@zh-mo

2010年論文

@zh-tw

2010年论文

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name

Discovery of TAK-875: A Potent, Selective, and Orally Bioavailable GPR40 Agonist.

@ast

Discovery of TAK-875: A Potent, Selective, and Orally Bioavailable GPR40 Agonist.

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Discovery of TAK-875: A Potent, Selective, and Orally Bioavailable GPR40 Agonist.

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type

label

Discovery of TAK-875: A Potent, Selective, and Orally Bioavailable GPR40 Agonist.

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Discovery of TAK-875: A Potent, Selective, and Orally Bioavailable GPR40 Agonist.

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Discovery of TAK-875: A Potent, Selective, and Orally Bioavailable GPR40 Agonist.

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prefLabel

Discovery of TAK-875: A Potent, Selective, and Orally Bioavailable GPR40 Agonist.

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Discovery of TAK-875: A Potent, Selective, and Orally Bioavailable GPR40 Agonist.

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Discovery of TAK-875: A Potent, Selective, and Orally Bioavailable GPR40 Agonist.

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ACS Medicinal Chemistry Letters

P1476

Discovery of TAK-875: A Potent, Selective, and Orally Bioavailable GPR40 Agonist.

@en

P2093

Akifumi Kogame

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

Ayako Harada

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

Junichi Miyazaki

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

Koji Takeuchi

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

Masahiro Ito

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

Masami Suzuki

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

Miyuki Funami

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

Naoyuki Kanzaki

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

Nobuhiro Suzuki

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

Nobuyuki Negoro

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

P2860

A cluster of four novel human G protein-coupled receptor genes occurring in close proximity to CD22 gene on chromosome 19q13.1

The Orphan G protein-coupled receptors GPR41 and GPR43 are activated by propionate and other short chain carboxylic acids

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.

Oleic acid interacts with GPR40 to induce Ca2+ signaling in rat islet beta-cells: mediation by PLC and L-type Ca2+ channel and link to insulin release.

Role of GPR40 in fatty acid action on the beta cell line INS-1E.

Identification of residues important for agonist recognition and activation in GPR40

The incretin system: glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors in type 2 diabetes

Free fatty acids regulate gut incretin glucagon-like peptide-1 secretion through GPR120

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290-294

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scholarly article

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10.1021/ML1000855

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6

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1

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2010-06-18T00:00:00Z

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24900210

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4007909

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