Small Molecule Drug Discovery at the Glucagon-Like Peptide-1 Receptor

Discovery of cyclic guanidines as potent, orally active, human glucagon receptor antagonists

(2011) Christopher Sinz et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Structure-Based Discovery of Allosteric Modulators of Two Related Class B G-Protein-Coupled Receptors

(2011) Chris de Graaf et al.   ChemMedChem

Cyclobutane Derivatives As Novel Nonpeptidic Small Molecule Agonists of Glucagon-Like Peptide-1 Receptor

(2011) Qing Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Quantifying Ligand Bias at Seven-Transmembrane Receptors

(2011) S. Rajagopal et al.   MOLECULAR PHARMACOLOGY

Structure of the human histamine H1 receptor complex with doxepin

(2011) Tatsuro Shimamura et al.   NATURE

The structural basis for agonist and partial agonist action on a β1-adrenergic receptor

(2011) Tony Warne et al.   NATURE

Novel Small Molecule Glucagon-Like Peptide-1 Receptor Agonist Stimulates Insulin Secretion in Rodents and From Human Islets

(2010) K. W. Sloop et al.   DIABETES

Functional Selectivity and Biased Receptor Signaling

(2010) T. Kenakin   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Modulation of the Glucagon-Like Peptide-1 Receptor Signaling by Naturally Occurring and Synthetic Flavonoids

(2010) D. Wootten et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Allosteric Ligands of the Glucagon-Like Peptide 1 Receptor (GLP-1R) Differentially Modulate Endogenous and Exogenous Peptide Responses in a Pathway-Selective Manner: Implications for Drug Screening

(2010) C. Koole et al.   MOLECULAR PHARMACOLOGY

Allosteric modulation of G protein-coupled receptors: A pharmacological perspective

(2010) Peter Keov et al.   NEUROPHARMACOLOGY

Reversal of Obesity and Insulin Resistance by a Non-Peptidic Glucagon-Like Peptide-1 Receptor Agonist in Diet-Induced Obese Mice

(2010) Min He et al.   PLoS One

Structure of the Human Dopamine D3 Receptor in Complex with a D2/D3 Selective Antagonist

(2010) E. Y. T. Chien et al.   SCIENCE

Insulin-releasing and metabolic effects of small molecule GLP-1 receptor agonist 6,7-dichloro-2-methylsulfonyl-3-N-tert-butylaminoquinoxaline

(2009) Nigel Irwin et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Crystal Structure of Glucagon-like Peptide-1 in Complex with the Extracellular Domain of the Glucagon-like Peptide-1 Receptor

(2009) Christina Rye Underwood et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Incretin-based therapies for type 2 diabetes mellitus

(2009) Julie A. Lovshin et al.   Nature Reviews Endocrinology

Crystal Structure of the Ligand-bound Glucagon-like Peptide-1 Receptor Extracellular Domain

(2008) Steffen Runge et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Structure of a β1-adrenergic G-protein-coupled receptor

(2008) Tony Warne et al.   NATURE

Drugability of Extracellular Targets: Discovery of Small Molecule Drugs Targeting Allosteric, Functional and Subunit-Selective Sites on GPCRs and Ion Channels

(2008) Dimitri E Grigoriadis et al.   NEUROPSYCHOPHARMACOLOGY

The 2.6 Angstrom Crystal Structure of a Human A2A Adenosine Receptor Bound to an Antagonist

(2008) V.-P. Jaakola et al.   SCIENCE