Published in Br J Pharmacol on March 05, 2016
In silico design of novel probes for the atypical opioid receptor MRGPRX2. Nat Chem Biol (2017) 1.45
Orphan receptor ligand discovery by pickpocketing pharmacological neighbors. Nat Chem Biol (2016) 1.41
Molecular pharmacology of G protein-coupled receptors. Br J Pharmacol (2016) 0.75
A general method applicable to the search for similarities in the amino acid sequence of two proteins. J Mol Biol (1970) 155.96
Crystal structure of the β2 adrenergic receptor-Gs protein complex. Nature (2011) 13.92
The G-protein-coupled receptors in the human genome form five main families. Phylogenetic analysis, paralogon groups, and fingerprints. Mol Pharmacol (2003) 9.99
Transduction of receptor signals by beta-arrestins. Science (2005) 9.87
The IUPHAR/BPS Guide to PHARMACOLOGY: an expert-driven knowledgebase of drug targets and their ligands. Nucleic Acids Res (2013) 9.61
Structure of a nanobody-stabilized active state of the β(2) adrenoceptor. Nature (2011) 9.61
Free fatty acids regulate insulin secretion from pancreatic beta cells through GPR40. Nature (2003) 6.87
Crystallizing membrane proteins using lipidic mesophases. Nat Protoc (2009) 6.36
The Concise Guide to PHARMACOLOGY 2015/16: Enzymes. Br J Pharmacol (2015) 5.96
The Orphan G protein-coupled receptors GPR41 and GPR43 are activated by propionate and other short chain carboxylic acids. J Biol Chem (2002) 5.53
Molecular signatures of G-protein-coupled receptors. Nature (2013) 5.19
The role of beta-arrestins in the termination and transduction of G-protein-coupled receptor signals. J Cell Sci (2002) 5.04
Agonist-bound adenosine A2A receptor structures reveal common features of GPCR activation. Nature (2011) 4.60
The Concise Guide to PHARMACOLOGY 2015/16: G protein-coupled receptors. Br J Pharmacol (2015) 4.28
The orphan G protein-coupled receptor GPR40 is activated by medium and long chain fatty acids. J Biol Chem (2002) 4.11
TAK-875 versus placebo or glimepiride in type 2 diabetes mellitus: a phase 2, randomised, double-blind, placebo-controlled trial. Lancet (2012) 3.46
International Union of Pharmacology. XLVI. G protein-coupled receptor list. Pharmacol Rev (2005) 3.33
Molecular mechanism of β-arrestin-biased agonism at seven-transmembrane receptors. Annu Rev Pharmacol Toxicol (2011) 3.15
Structure of the human smoothened receptor bound to an antitumour agent. Nature (2013) 3.08
Structure of class B GPCR corticotropin-releasing factor receptor 1. Nature (2013) 2.87
Directory of useful decoys, enhanced (DUD-E): better ligands and decoys for better benchmarking. J Med Chem (2012) 2.86
Structure of the human glucagon class B G-protein-coupled receptor. Nature (2013) 2.86
Evaluating virtual screening methods: good and bad metrics for the "early recognition" problem. J Chem Inf Model (2007) 2.78
Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules. Br J Pharmacol (2006) 2.62
Structure-based discovery of beta2-adrenergic receptor ligands. Proc Natl Acad Sci U S A (2009) 2.48
Flexible ligand docking to multiple receptor conformations: a practical alternative. Curr Opin Struct Biol (2008) 2.38
The orphan G protein-coupled receptor 3 modulates amyloid-beta peptide generation in neurons. Science (2009) 2.35
Community-wide assessment of GPCR structure modelling and ligand docking: GPCR Dock 2008. Nat Rev Drug Discov (2009) 2.23
Status of GPCR modeling and docking as reflected by community-wide GPCR Dock 2010 assessment. Structure (2011) 2.11
Ligand discovery from a dopamine D3 receptor homology model and crystal structure. Nat Chem Biol (2011) 2.10
Fusion partner toolchest for the stabilization and crystallization of G protein-coupled receptors. Structure (2012) 2.08
Constitutive μ-opioid receptor activity leads to long-term endogenous analgesia and dependence. Science (2013) 1.91
Lipid G protein-coupled receptor ligand identification using beta-arrestin PathHunter assay. J Biol Chem (2009) 1.91
Allostery at G protein-coupled receptor homo- and heteromers: uncharted pharmacological landscapes. Pharmacol Rev (2010) 1.89
Structure-based discovery of novel chemotypes for adenosine A(2A) receptor antagonists. J Med Chem (2010) 1.88
Structure of a class C GPCR metabotropic glutamate receptor 1 bound to an allosteric modulator. Science (2014) 1.81
International Union of Pharmacology. LXXI. Free fatty acid receptors FFA1, -2, and -3: pharmacology and pathophysiological functions. Pharmacol Rev (2008) 1.80
Comprehensive repertoire and phylogenetic analysis of the G protein-coupled receptors in human and mouse. Genomics (2006) 1.80
Constitutive activity and inverse agonists of G protein-coupled receptors: a current perspective. Mol Pharmacol (2003) 1.72
Emerging paradigms in GPCR allostery: implications for drug discovery. Nat Rev Drug Discov (2013) 1.69
Allosteric ligands for the pharmacologically dark receptors GPR68 and GPR65. Nature (2015) 1.66
Structural biology. Crystal structure of the chemokine receptor CXCR4 in complex with a viral chemokine. Science (2015) 1.65
The orphan GPR50 receptor specifically inhibits MT1 melatonin receptor function through heterodimerization. EMBO J (2006) 1.64
International Union of Basic and Clinical Pharmacology. LXXXVIII. G protein-coupled receptor list: recommendations for new pairings with cognate ligands. Pharmacol Rev (2013) 1.60
GPCR 3D homology models for ligand screening: lessons learned from blind predictions of adenosine A2a receptor complex. Proteins (2010) 1.57
Expression Atlas update-an integrated database of gene and protein expression in humans, animals and plants. Nucleic Acids Res (2015) 1.53
A cluster of four novel human G protein-coupled receptor genes occurring in close proximity to CD22 gene on chromosome 19q13.1. Biochem Biophys Res Commun (1997) 1.50
Structure of class C GPCR metabotropic glutamate receptor 5 transmembrane domain. Nature (2014) 1.48
New concepts in pharmacological efficacy at 7TM receptors: IUPHAR review 2. Br J Pharmacol (2013) 1.43
Discovery of novel agonists and antagonists of the free fatty acid receptor 1 (FFAR1) using virtual screening. J Med Chem (2008) 1.38
G protein-coupled receptor deorphanizations. Annu Rev Pharmacol Toxicol (2012) 1.33
Crystal structure-based virtual screening for fragment-like ligands of the human histamine H(1) receptor. J Med Chem (2011) 1.30
Identification of residues important for agonist recognition and activation in GPR40. J Biol Chem (2007) 1.28
PRESTO-Tango as an open-source resource for interrogation of the druggable human GPCRome. Nat Struct Mol Biol (2015) 1.27
Bidirectional, iterative approach to the structural delineation of the functional "chemoprint" in GPR40 for agonist recognition. J Med Chem (2007) 1.26
Structure-based ligand discovery for the protein-protein interface of chemokine receptor CXCR4. Proc Natl Acad Sci U S A (2012) 1.25
Functional coupling of mammalian receptors to the yeast mating pathway using novel yeast/mammalian G protein alpha-subunit chimeras. Yeast (2000) 1.24
The identification of ligands at orphan G-protein coupled receptors. Annu Rev Pharmacol Toxicol (2004) 1.23
Tools for GPCR drug discovery. Acta Pharmacol Sin (2012) 1.22
Identification of novel species-selective agonists of the G-protein-coupled receptor GPR35 that promote recruitment of β-arrestin-2 and activate Gα13. Biochem J (2010) 1.22
High-resolution structure of the human GPR40 receptor bound to allosteric agonist TAK-875. Nature (2014) 1.19
Diversity screening versus focussed screening in drug discovery. Drug Discov Today (2000) 1.12
Synthesis and activity of small molecule GPR40 agonists. Bioorg Med Chem Lett (2006) 1.12
Advances in GPCR modeling evaluated by the GPCR Dock 2013 assessment: meeting new challenges. Structure (2014) 1.12
The flexible pocketome engine for structural chemogenomics. Methods Mol Biol (2009) 1.11
Identification of novel adenosine A(2A) receptor antagonists by virtual screening. J Med Chem (2012) 1.10
Randomized, double-blind, dose-ranging study of TAK-875, a novel GPR40 agonist, in Japanese patients with inadequately controlled type 2 diabetes. Diabetes Care (2012) 1.10
Design, synthesis, and biological activity of potent and orally available G protein-coupled receptor 40 agonists. J Med Chem (2011) 1.10
Selective orthosteric free fatty acid receptor 2 (FFA2) agonists: identification of the structural and chemical requirements for selective activation of FFA2 versus FFA3. J Biol Chem (2011) 1.09
Characterisation and differential expression of two very closely related G-protein-coupled receptors, GPR139 and GPR142, in mouse tissue and during mouse development. Neuropharmacology (2005) 1.08
Screening β-arrestin recruitment for the identification of natural ligands for orphan G-protein-coupled receptors. J Biomol Screen (2013) 1.08
Discovery of novel human histamine H4 receptor ligands by large-scale structure-based virtual screening. J Med Chem (2008) 1.07
Customizing G Protein-coupled receptor models for structure-based virtual screening. Curr Pharm Des (2009) 1.06
The fatty acid receptor FFA1/GPR40 a decade later: how much do we know? Trends Endocrinol Metab (2013) 1.06
Altered immune response in mice deficient for the G protein-coupled receptor GPR34. J Biol Chem (2010) 1.05
Luciferase Reporter Assay System for Deciphering GPCR Pathways. Curr Chem Genomics (2010) 1.05
Methodological advances: the unsung heroes of the GPCR structural revolution. Nat Rev Mol Cell Biol (2015) 1.03
Cellular and molecular biology of orphan G protein-coupled receptors. Int Rev Cytol (2006) 1.03
Cell adhesion receptor GPR133 couples to Gs protein. J Biol Chem (2011) 1.02
Femtosecond crystallography of membrane proteins in the lipidic cubic phase. Philos Trans R Soc Lond B Biol Sci (2014) 1.01
Conformation guides molecular efficacy in docking screens of activated β-2 adrenergic G protein coupled receptor. ACS Chem Biol (2013) 1.01
Computer-aided discovery of aromatic l-α-amino acids as agonists of the orphan G protein-coupled receptor GPR139. J Chem Inf Model (2014) 1.01
Structure-based identification of binding sites, native ligands and potential inhibitors for G-protein coupled receptors. Proteins (2003) 1.00
Are GPCRs still a source of new targets? J Biomol Screen (2013) 1.00
Identification of the GPR55 agonist binding site using a novel set of high-potency GPR55 selective ligands. Biochemistry (2011) 1.00
From G Protein-coupled Receptor Structure Resolution to Rational Drug Design. J Biol Chem (2015) 0.99
High constitutive activity is an intrinsic feature of ghrelin receptor protein: a study with a functional monomeric GHS-R1a receptor reconstituted in lipid discs. J Biol Chem (2011) 0.99
Identification of surrogate agonists and antagonists for orphan G-protein-coupled receptor GPR139. J Biomol Screen (2009) 0.97
Discovery of a novel selective kappa-opioid receptor agonist using crystal structure-based virtual screening. J Chem Inf Model (2013) 0.96
Discovery and SAR of a Series of Agonists at Orphan G Protein-Coupled Receptor 139. ACS Med Chem Lett (2011) 0.95
ALiBERO: evolving a team of complementary pocket conformations rather than a single leader. J Chem Inf Model (2012) 0.94
Elucidation of signaling and functional activities of an orphan GPCR, GPR81. J Lipid Res (2008) 0.93
Structure-based ligand discovery targeting orthosteric and allosteric pockets of dopamine receptors. Mol Pharmacol (2013) 0.93
Hot-spots-guided receptor-based pharmacophores (HS-Pharm): a knowledge-based approach to identify ligand-anchoring atoms in protein cavities and prioritize structure-based pharmacophores. J Chem Inf Model (2008) 0.92
Combination of ligand- and structure-based methods in virtual screening. Drug Discov Today Technol (2013) 0.92
Structure-based and fragment-based GPCR drug discovery. ChemMedChem (2013) 0.92
The natural inverse agonist agouti-related protein induces arrestin-mediated endocytosis of melanocortin-3 and -4 receptors. J Biol Chem (2006) 0.92
GPCR-SSFE: a comprehensive database of G-protein-coupled receptor template predictions and homology models. BMC Bioinformatics (2011) 0.91
GPR88 reveals a discrete function of primary cilia as selective insulators of GPCR cross-talk. PLoS One (2013) 0.91
Muscarinic receptors as model targets and antitargets for structure-based ligand discovery. Mol Pharmacol (2013) 0.87