Generating thermostabilized agonist-bound GPR40/FFAR1 using virus-like particles and a label-free binding assay

Loss of constitutive activity is correlated with increased thermostability of the human adenosine A2Areceptor

(2013) Nicolas Bertheleme et al.   BRITISH JOURNAL OF PHARMACOLOGY

Molecular signatures of G-protein-coupled receptors

(2013) A. J. Venkatakrishnan et al.   NATURE

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

(2013) Chiori Yabuki et al.   PLoS One

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

Discovery of 1,2,4-Triazine Derivatives as Adenosine A2A Antagonists using Structure Based Drug Design

(2012) Miles Congreve 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

Fusion Partner Toolchest for the Stabilization and Crystallization of G Protein-Coupled Receptors

(2012) Eugene Chun et al.   STRUCTURE

A crystal clear solution for determining G-protein-coupled receptor structures

(2012) Christopher G. Tate   TRENDS IN BIOCHEMICAL SCIENCES

GPR40-induced insulin secretion by the novel agonist TAK-875: first clinical findings in patients with type 2 diabetes

(2011) T. Araki et al.   DIABETES OBESITY & METABOLISM

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

Engineering an Ultra-Thermostable β1-Adrenoceptor

(2011) Jennifer L. Miller et al.   JOURNAL OF MOLECULAR BIOLOGY

Thermostabilisation of an Agonist-Bound Conformation of the Human Adenosine A2A Receptor

(2011) Guillaume Lebon et al.   JOURNAL OF MOLECULAR BIOLOGY

Structure of the Adenosine A2A Receptor in Complex with ZM241385 and the Xanthines XAC and Caffeine

(2011) Andrew S. Doré et al.   STRUCTURE

The properties of thermostabilised G protein-coupled receptors (StaRs) and their use in drug discovery

(2010) Nathan Robertson et al.   NEUROPHARMACOLOGY

Thermostabilization of the Neurotensin Receptor NTS1

(2009) Yoko Shibata et al.   JOURNAL OF MOLECULAR BIOLOGY

Structure-based discovery of  2-adrenergic receptor ligands

(2009) P. Kolb et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structural diversity of G protein-coupled receptors and significance for drug discovery

(2008) Malin C. Lagerström et al.   NATURE REVIEWS DRUG DISCOVERY

Co-evolving stability and conformational homogeneity of the human adenosine A2a receptor

(2008) F. Magnani et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Conformational thermostabilization of the  1-adrenergic receptor in a detergent-resistant form

(2008) M. J. Serrano-Vega et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA