β-Arrestin Recruitment and Biased Agonism at Free Fatty Acid Receptor 1

GPR40 agonists for the treatment of type 2 diabetes: life after ‘TAKing’ a hit

(2015) A. D. Mancini et al.   DIABETES OBESITY & METABOLISM

GPR40 (FFAR1) – Combined Gs and Gq signaling in vitro is associated with robust incretin secretagogue action ex vivo and in vivo

(2015) Maria Hauge et al.   Molecular Metabolism

Differential requirements of arrestin-3 and clathrin for ligand-dependent and -independent internalization of human G protein-coupled receptor 40

(2014) Jing Qian et al.   CELLULAR SIGNALLING

Allosteric Modulation of M1Muscarinic Acetylcholine Receptor Internalization and Subcellular Trafficking

(2014) Holly R. Yeatman et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

High-resolution structure of the human GPR40 receptor bound to allosteric agonist TAK-875

(2014) Ankita Srivastava et al.   NATURE

CNX-011-67, a novel GPR40 agonist, enhances glucose responsiveness, insulin secretion and islet insulin content in n-STZ rats and in islets from type 2 diabetic patients

(2014) Venkategowda Sunil et al.   BMC Pharmacology & Toxicology

Recent developments in biased agonism

(2013) James W Wisler et al.   CURRENT OPINION IN CELL BIOLOGY

Reevaluation of Fatty Acid Receptor 1 as a Drug Target for the Stimulation of Insulin Secretion in Humans

(2013) R. Wagner et al.   DIABETES

β-Arrestin2 plays a key role in the modulation of the pancreatic beta cell mass in mice

(2013) Magalie A. Ravier et al.   DIABETOLOGIA

Signalling bias in new drug discovery: detection, quantification and therapeutic impact

(2013) Terry Kenakin et al.   NATURE REVIEWS DRUG DISCOVERY

A Novel Antidiabetic Drug, Fasiglifam/TAK-875, Acts as an Ago-Allosteric Modulator of FFAR1

(2013) Chiori Yabuki et al.   PLoS One

The fatty acid receptor FFA1/GPR40 a decade later: how much do we know?

(2013) Arturo D. Mancini et al.   TRENDS IN ENDOCRINOLOGY AND METABOLISM

Restructuring G-Protein- Coupled Receptor Activation

(2012) Martin Audet 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

Probing Heterotrimeric G Protein Activation: Applications to Biased Ligands

(2012) Colette Denis et al.   CURRENT PHARMACEUTICAL DESIGN

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

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

AMG 837: A potent, orally bioavailable GPR40 agonist

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

Expression of G protein-coupled receptors and related proteins in HEK293, AtT20, BV2, and N18 cell lines as revealed by microarray analysis

(2011) Brady K Atwood et al.   BMC GENOMICS

Emerging paradigms of β-arrestin-dependent seven transmembrane receptor signaling

(2011) Arun K. Shukla et al.   TRENDS IN BIOCHEMICAL SCIENCES

M3-muscarinic receptor promotes insulin release via receptor phosphorylation/arrestin-dependent activation of protein kinase D1

(2010) K. C. Kong et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

(2010) Nobuyuki Negoro et al.   ACS Medicinal Chemistry Letters

GLP-1 Mediates Antiapoptotic Effect by Phosphorylating Bad through a β-Arrestin 1-mediated ERK1/2 Activation in Pancreatic β-Cells

(2009) Julie Quoyer et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

(2008) M. Kebede et al.   DIABETES

 -Arrestin-1 mediates glucagon-like peptide-1 signaling to insulin secretion in cultured pancreatic   cells

(2008) N. Sonoda et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA