Activation of GPR40 as a Therapeutic Target for the Treatment of Type 2 Diabetes

Pancreatic β Cell Dedifferentiation as a Mechanism of Diabetic β Cell Failure

(2012) Chutima Talchai et al.   CELL

A Multiple-Ascending-Dose Study to Evaluate Safety, Pharmacokinetics, and Pharmacodynamics of a Novel GPR40 Agonist, TAK-875, in Subjects With Type 2 Diabetes

(2012) E Leifke et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

G protein-coupled receptor (GPR)40-dependent potentiation of insulin secretion in mouse islets is mediated by protein kinase D1

(2012) M. Ferdaoussi et al.   DIABETOLOGIA

Discovery of Phenylpropanoic Acid Derivatives Containing Polar Functionalities as Potent and Orally Bioavailable G Protein-Coupled Receptor 40 Agonists for the Treatment of Type 2 Diabetes

(2012) Satoshi Mikami et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identification of Fused-Ring Alkanoic Acids with Improved Pharmacokinetic Profiles that Act as G Protein-Coupled Receptor 40/Free Fatty Acid Receptor 1 Agonists

(2012) Nobuyuki Negoro et al.   JOURNAL OF MEDICINAL CHEMISTRY

Optimization of (2,3-Dihydro-1-benzofuran-3-yl)acetic Acids: Discovery of a Non-Free Fatty Acid-Like, Highly Bioavailable G Protein-Coupled Receptor 40/Free Fatty Acid Receptor 1 Agonist as a Glucose-Dependent Insulinotropic Agent

(2012) Nobuyuki Negoro et al.   JOURNAL OF MEDICINAL CHEMISTRY

TAK-875 versus placebo or glimepiride in type 2 diabetes mellitus: a phase 2, randomised, double-blind, placebo-controlled trial

(2012) Charles F Burant et al.   LANCET

3-Substituted 3-(4-aryloxyaryl)-propanoic acids as GPR40 agonists

(2011) Shawn P. Walsh et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

AMG 837: A potent, orally bioavailable GPR40 agonist

(2011) Jonathan B. Houze et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Cooperative Activation of Alkyne and Thioamide Functionalities; Direct Catalytic Asymmetric Conjugate Addition of Terminal Alkynes to α,β-Unsaturated Thioamides

(2011) Ryo Yazaki et al.   Chemistry-An Asian Journal

Feasible Synthesis of the GPR40 Antagonist by Constructing 2-Thiouracil Ring via Acid Mediated Cyclization

(2011) Jiayu Liao et al.   HETEROCYCLES

Safety, Tolerability, Pharmacokinetics, and Pharmacodynamic Properties of the GPR40 Agonist TAK-875: Results From a Double-Blind, Placebo-Controlled Single Oral Dose Rising Study in Healthy Volunteers

(2011) Himanshu Naik et al.   JOURNAL OF CLINICAL PHARMACOLOGY

Identification of a Potent and Selective Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist with Favorable Physicochemical and in Vitro ADME Properties

(2011) Elisabeth Christiansen et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design, Synthesis, and Biological Activity of Potent and Orally Available G Protein-Coupled Receptor 40 Agonists

(2011) Shinobu Sasaki et al.   JOURNAL OF MEDICINAL CHEMISTRY

Enantioselective Synthesis of a GPR40 Agonist AMG 837 via Catalytic Asymmetric Conjugate Addition of Terminal Alkyne to α,β-Unsaturated Thioamide

(2011) Ryo Yazaki et al.   ORGANIC LETTERS

DC260126, a small-molecule antagonist of GPR40, improves insulin tolerance but not glucose tolerance in obese Zucker rats

(2010) Xiaodong Zhang et al.   BIOMEDICINE & PHARMACOTHERAPY

G-protein coupled receptors mediating long chain fatty acid signalling in the pancreatic beta-cell

(2009) Noel G. Morgan et al.   BIOCHEMICAL PHARMACOLOGY

Synthesis and SAR of 1,2,3,4-tetrahydroisoquinolin-1-ones as novel G-protein-coupled receptor 40 (GPR40) antagonists

(2009) Paul S. Humphries et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Deletion of GPR40 Impairs Glucose-Induced Insulin Secretion In Vivo in Mice Without Affecting Intracellular Fuel Metabolism in Islets

(2009) T. Alquier et al.   DIABETES

GPR40: Good Cop, Bad Cop?

(2009) T. Alquier et al.   DIABETES

Overexpression of GPR40 in Pancreatic  -Cells Augments Glucose-Stimulated Insulin Secretion and Improves Glucose Tolerance in Normal and Diabetic Mice

(2009) K. Nagasumi et al.   DIABETES

Novel selective ligands for free fatty acid receptors GPR120 and GPR40

(2009) Takafumi Hara et al.   NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY

Metabolic cycling in control of glucose-stimulated insulin secretion

(2008) Mette V. Jensen et al.   AMERICAN JOURNAL OF PHYSIOLOGY-ENDOCRINOLOGY AND METABOLISM

Discovery of diacylphloroglucinols as a new class of GPR40 (FFAR1) agonists

(2008) Sandip B. Bharate et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Selective Small-Molecule Agonists of G Protein-Coupled Receptor 40 Promote Glucose-Dependent Insulin Secretion and Reduce Blood Glucose in Mice

(2008) C. P. Tan et al.   DIABETES

The Fatty Acid Receptor GPR40 Plays a Role in Insulin Secretion In Vivo After High-Fat Feeding

(2008) M. Kebede et al.   DIABETES

Lack of FFAR1/GPR40 Does Not Protect Mice From High-Fat Diet-Induced Metabolic Disease

(2008) H. Lan et al.   DIABETES

Discovery of Potent and Selective Agonists for the Free Fatty Acid Receptor 1 (FFA1/GPR40), a Potential Target for the Treatment of Type II Diabetes

(2008) Elisabeth Christiansen et al.   JOURNAL OF MEDICINAL CHEMISTRY

β-cell failure as a complication of diabetes

(2008) K. J. Chang-Chen et al.   REVIEWS IN ENDOCRINE & METABOLIC DISORDERS