Published in Mol Pharmacol on May 08, 2009
Seven transmembrane receptors as shapeshifting proteins: the impact of allosteric modulation and functional selectivity on new drug discovery. Pharmacol Rev (2010) 3.27
Allostery at G protein-coupled receptor homo- and heteromers: uncharted pharmacological landscapes. Pharmacol Rev (2010) 1.89
Making structural sense of dimerization interfaces of delta opioid receptor homodimers. Biochemistry (2011) 1.13
Mapping spatial approximations between the amino terminus of secretin and each of the extracellular loops of its receptor using cysteine trapping. FASEB J (2012) 1.13
Structural basis of M3 muscarinic receptor dimer/oligomer formation. J Biol Chem (2011) 1.06
Secretin occupies a single protomer of the homodimeric secretin receptor complex: insights from photoaffinity labeling studies using dual sites of covalent attachment. J Biol Chem (2010) 1.01
Calcitonin and calcitonin receptor-like receptors: common themes with family B GPCRs? Br J Pharmacol (2012) 0.97
Molecular basis of association of receptor activity-modifying protein 3 with the family B G protein-coupled secretin receptor. Biochemistry (2009) 0.97
Lessons from free energy simulations of delta-opioid receptor homodimers involving the fourth transmembrane helix. Biochemistry (2010) 0.95
Occupancy of both sites on the thyrotropin (TSH) receptor dimer is necessary for phosphoinositide signaling. FASEB J (2011) 0.91
Glucagon-like peptide-1 receptor dimerization differentially regulates agonist signaling but does not affect small molecule allostery. Proc Natl Acad Sci U S A (2012) 0.89
Transmembrane peptides as unique tools to demonstrate the in vivo action of a cross-class GPCR heterocomplex. FASEB J (2014) 0.87
Importance of lipid-exposed residues in transmembrane segment four for family B calcitonin receptor homo-dimerization. Regul Pept (2010) 0.87
G protein-coupled receptors: walking hand-in-hand, talking hand-in-hand? Br J Pharmacol (2011) 0.86
Direct interactions between calcitonin-like receptor (CLR) and CGRP-receptor component protein (RCP) regulate CGRP receptor signaling. Endocrinology (2012) 0.85
Receptor oligomerization in family B1 of G-protein-coupled receptors: focus on BRET investigations and the link between GPCR oligomerization and binding cooperativity. Front Endocrinol (Lausanne) (2012) 0.84
A novel approach to quantify G-protein-coupled receptor dimerization equilibrium using bioluminescence resonance energy transfer. Methods Mol Biol (2013) 0.82
Consequences of splice variation on Secretin family G protein-coupled receptor function. Br J Pharmacol (2012) 0.81
The N-terminal HSDCIF motif is required for cell surface trafficking and dimerization of family B G protein coupled receptor PAC1. PLoS One (2012) 0.80
Role of CGRP-receptor component protein (RCP) in CLR/RAMP function. Curr Protein Pept Sci (2013) 0.79
Transmembrane signal transduction by peptide hormones via family B G protein-coupled receptors. Front Pharmacol (2015) 0.78
Glucagon-Like Peptide-1 and Its Class B G Protein-Coupled Receptors: A Long March to Therapeutic Successes. Pharmacol Rev (2016) 0.78
Ligand binding and activation of the secretin receptor, a prototypic family B G protein-coupled receptor. Br J Pharmacol (2012) 0.78
Receptor oligomerization: from early evidence to current understanding in class B GPCRs. Front Endocrinol (Lausanne) (2013) 0.77
Structure and Function of Cross-class Complexes of G Protein-coupled Secretin and Angiotensin 1a Receptors. J Biol Chem (2016) 0.77
The class B G-protein-coupled GLP-1 receptor: an important target for the treatment of type-2 diabetes mellitus. Int J Obes Suppl (2014) 0.75
Spatial Intensity Distribution Analysis Quantifies the Extent and Regulation of Homo-Dimerization of the Secretin Receptor. Biochem J (2017) 0.75
Ligand: a versatile computerized approach for characterization of ligand-binding systems. Anal Biochem (1980) 28.03
High-resolution crystal structure of an engineered human beta2-adrenergic G protein-coupled receptor. Science (2007) 20.32
Structural basis of glutamate recognition by a dimeric metabotropic glutamate receptor. Nature (2000) 6.58
Biased probability Monte Carlo conformational searches and electrostatic calculations for peptides and proteins. J Mol Biol (1994) 6.41
A monomeric G protein-coupled receptor isolated in a high-density lipoprotein particle efficiently activates its G protein. Proc Natl Acad Sci U S A (2007) 6.04
Heterodimerization is required for the formation of a functional GABA(B) receptor. Nature (1998) 5.59
A peptide derived from a beta2-adrenergic receptor transmembrane domain inhibits both receptor dimerization and activation. J Biol Chem (1996) 3.77
Efficient coupling of transducin to monomeric rhodopsin in a phospholipid bilayer. J Biol Chem (2007) 2.59
The evolution of transmembrane helix kinks and the structural diversity of G protein-coupled receptors. Proc Natl Acad Sci U S A (2004) 2.19
Helix-packing motifs in membrane proteins. Proc Natl Acad Sci U S A (2006) 2.13
Identification of amino acid residues crucial for chemokine receptor dimerization. Nat Immunol (2004) 2.09
Hinges, swivels and switches: the role of prolines in signalling via transmembrane alpha-helices. Trends Pharmacol Sci (2000) 2.08
Oligomerization of G protein-coupled receptors: past, present, and future. Biochemistry (2004) 2.03
Homodimerization of the beta2-adrenergic receptor as a prerequisite for cell surface targeting. J Biol Chem (2004) 2.03
Transmembrane segment IV contributes a functionally important interface for oligomerization of the Class II G protein-coupled secretin receptor. J Biol Chem (2007) 1.55
Oligomerization of the alpha 1a- and alpha 1b-adrenergic receptor subtypes. Potential implications in receptor internalization. J Biol Chem (2003) 1.49
A day in the life of a G protein-coupled receptor: the contribution to function of G protein-coupled receptor dimerization. Br J Pharmacol (2007) 1.47
Relationship between native and recombinant cholecystokinin receptors: role of differential glycosylation. Pancreas (1996) 1.46
Allosteric modulation of heterodimeric G-protein-coupled receptors. Trends Pharmacol Sci (2007) 1.42
Preferential formation of MT1/MT2 melatonin receptor heterodimers with distinct ligand interaction properties compared with MT2 homodimers. Mol Pharmacol (2004) 1.37
Agonist-dependent dissociation of oligomeric complexes of G protein-coupled cholecystokinin receptors demonstrated in living cells using bioluminescence resonance energy transfer. J Biol Chem (2001) 1.34
Synergistic interaction between adenosine A2A and glutamate mGlu5 receptors: implications for striatal neuronal function. Proc Natl Acad Sci U S A (2002) 1.30
The hunchback and its neighbours: proline as an environmental modulator. Trends Biochem Sci (2001) 1.28
Oligomerization, biogenesis, and signaling is promoted by a glycophorin A-like dimerization motif in transmembrane domain 1 of a yeast G protein-coupled receptor. J Biol Chem (2003) 1.25
Constitutive formation of oligomeric complexes between family B G protein-coupled vasoactive intestinal polypeptide and secretin receptors. Mol Pharmacol (2005) 1.23
Probing the existence of G protein-coupled receptor dimers by positive and negative ligand-dependent cooperative binding. Mol Pharmacol (2006) 1.20
Metabotropic glutamate 1alpha and adenosine A1 receptors assemble into functionally interacting complexes. J Biol Chem (2001) 1.17
Dimerization in the absence of higher-order oligomerization of the G protein-coupled secretin receptor. Biochim Biophys Acta (2008) 1.10
Dimers of class A G protein-coupled receptors function via agonist-mediated trans-activation of associated G proteins. J Biol Chem (2003) 1.07
G-protein-coupled receptor heteromers: function and ligand pharmacology. Br J Pharmacol (2007) 1.07
Spatial approximation between secretin residue five and the third extracellular loop of its receptor provides new insight into the molecular basis of natural agonist binding. Mol Pharmacol (2008) 1.06
Pattern of intra-family hetero-oligomerization involving the G-protein-coupled secretin receptor. J Mol Neurosci (2008) 1.05
Secretin receptor oligomers form intracellularly during maturation through receptor core domains. Biochemistry (2006) 1.05
Heterodimers of alpha1B- and alpha1D-adrenergic receptors form a single functional entity. Mol Pharmacol (2005) 1.04
The arrangement of the transmembrane helices in the secretin receptor family of G-protein-coupled receptors. FEBS Lett (1997) 1.03
Silencing of secretin receptor function by dimerization with a misspliced variant secretin receptor in ductal pancreatic adenocarcinoma. Cancer Res (2002) 1.03
Structural determinants for G-protein activation and specificity in the third intracellular loop of the thyroid-stimulating hormone receptor. J Mol Med (Berl) (2006) 0.98
Structure of the integral membrane domain of the GLP1 receptor. Proteins (1999) 0.97
Use of probes with fluorescence indicator distributed throughout the pharmacophore to examine the peptide agonist-binding environment of the family B G protein-coupled secretin receptor. J Biol Chem (2005) 0.96
Identification of a novel site within G protein alpha subunits important for specificity of receptor-G protein interaction. Mol Pharmacol (2004) 0.93
Identification of an interaction between residue 6 of the natural peptide ligand and a distinct residue within the amino-terminal tail of the secretin receptor. J Biol Chem (1999) 0.92
Genetic analysis of receptor-Galphaq coupling selectivity. J Biol Chem (1997) 0.83
XCMS: processing mass spectrometry data for metabolite profiling using nonlinear peak alignment, matching, and identification. Anal Chem (2006) 15.00
Structures of the CXCR4 chemokine GPCR with small-molecule and cyclic peptide antagonists. Science (2010) 10.30
METLIN: a metabolite mass spectral database. Ther Drug Monit (2005) 10.15
Functional selectivity and classical concepts of quantitative pharmacology. J Pharmacol Exp Ther (2006) 7.03
Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders. Nat Rev Drug Discov (2009) 6.69
Sirtuin 2 inhibitors rescue alpha-synuclein-mediated toxicity in models of Parkinson's disease. Science (2007) 5.49
Allosteric modulation of G protein-coupled receptors. Annu Rev Pharmacol Toxicol (2007) 4.02
Structure of the human histamine H1 receptor complex with doxepin. Nature (2011) 3.48
Virtual ligand screening of the p300/CBP histone acetyltransferase: identification of a selective small molecule inhibitor. Chem Biol (2010) 3.38
Signalling bias in new drug discovery: detection, quantification and therapeutic impact. Nat Rev Drug Discov (2012) 3.30
Comparative study of several algorithms for flexible ligand docking. J Comput Aided Mol Des (2003) 3.29
Seven transmembrane receptors as shapeshifting proteins: the impact of allosteric modulation and functional selectivity on new drug discovery. Pharmacol Rev (2010) 3.27
International Union of Pharmacology Committee on Receptor Nomenclature and Drug Classification. XXXVIII. Update on terms and symbols in quantitative pharmacology. Pharmacol Rev (2003) 2.93
International Union of Pharmacology. XXXII. The mammalian calcitonin gene-related peptides, adrenomedullin, amylin, and calcitonin receptors. Pharmacol Rev (2002) 2.86
Pocketome via comprehensive identification and classification of ligand binding envelopes. Mol Cell Proteomics (2005) 2.83
Study of recurrence after surgical resection of intraductal papillary mucinous neoplasm of the pancreas. Gastroenterology (2002) 2.76
Conserved binding mode of human beta2 adrenergic receptor inverse agonists and antagonist revealed by X-ray crystallography. J Am Chem Soc (2010) 2.62
Activation and allosteric modulation of a muscarinic acetylcholine receptor. Nature (2013) 2.49
Allosteric modulation of the cannabinoid CB1 receptor. Mol Pharmacol (2005) 2.42
Flexible ligand docking to multiple receptor conformations: a practical alternative. Curr Opin Struct Biol (2008) 2.38
International Union of Pharmacology. XXXV. The glucagon receptor family. Pharmacol Rev (2003) 2.25
Novel receptor partners and function of receptor activity-modifying proteins. J Biol Chem (2002) 2.14
Status of GPCR modeling and docking as reflected by community-wide GPCR Dock 2010 assessment. Structure (2011) 2.11
Allosteric GPCR modulators: taking advantage of permissive receptor pharmacology. Trends Pharmacol Sci (2007) 2.10
Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery. J Med Chem (2012) 2.10
Analysis of full and partial agonists binding to beta2-adrenergic receptor suggests a role of transmembrane helix V in agonist-specific conformational changes. J Mol Recognit (2009) 2.05
Nuclear hormone receptor targeted virtual screening. J Med Chem (2003) 2.05
Allosteric modulation of G protein-coupled receptors: a pharmacological perspective. Neuropharmacology (2010) 1.97
A simple method for quantifying functional selectivity and agonist bias. ACS Chem Neurosci (2011) 1.93
Structure-based discovery of novel chemotypes for adenosine A(2A) receptor antagonists. J Med Chem (2010) 1.88
GPCR modulation by RAMPs. Pharmacol Ther (2005) 1.85
Identification of protein-protein interaction sites from docking energy landscapes. J Mol Biol (2004) 1.79
Serine-arginine protein kinase 1 overexpression is associated with tumorigenic imbalance in mitogen-activated protein kinase pathways in breast, colonic, and pancreatic carcinomas. Cancer Res (2007) 1.73
Possible endogenous agonist mechanism for the activation of secretin family G protein-coupled receptors. Mol Pharmacol (2006) 1.72
Critical role for the second extracellular loop in the binding of both orthosteric and allosteric G protein-coupled receptor ligands. J Biol Chem (2007) 1.70
The liganding of glycolipid transfer protein is controlled by glycolipid acyl structure. PLoS Biol (2006) 1.70
Emerging paradigms in GPCR allostery: implications for drug discovery. Nat Rev Drug Discov (2013) 1.69
Positive and negative allosteric modulators promote biased signaling at the calcium-sensing receptor. Endocrinology (2011) 1.69
Optimal docking area: a new method for predicting protein-protein interaction sites. Proteins (2005) 1.69
ADP_EM: fast exhaustive multi-resolution docking for high-throughput coverage. Bioinformatics (2006) 1.68
Procalcitonin has bioactivity at calcitonin receptor family complexes: potential mediator implications in sepsis. Crit Care Med (2008) 1.67
A novel mechanism of G protein-coupled receptor functional selectivity. Muscarinic partial agonist McN-A-343 as a bitopic orthosteric/allosteric ligand. J Biol Chem (2008) 1.66
Statistical analysis and prediction of protein-protein interfaces. Proteins (2005) 1.65
ICM-DISCO docking by global energy optimization with fully flexible side-chains. Proteins (2003) 1.63
Soft protein-protein docking in internal coordinates. Protein Sci (2002) 1.60
Structural basis for modulation of a G-protein-coupled receptor by allosteric drugs. Nature (2013) 1.59
Structural basis of receptor sulfotyrosine recognition by a CC chemokine: the N-terminal region of CCR3 bound to CCL11/eotaxin-1. Structure (2014) 1.58
GPCR 3D homology models for ligand screening: lessons learned from blind predictions of adenosine A2a receptor complex. Proteins (2010) 1.57
G-protein-coupled receptor Mas is a physiological antagonist of the angiotensin II type 1 receptor. Circulation (2005) 1.57
New insights into the function of M4 muscarinic acetylcholine receptors gained using a novel allosteric modulator and a DREADD (designer receptor exclusively activated by a designer drug). Mol Pharmacol (2008) 1.57
Match-only integral distribution (MOID) algorithm for high-density oligonucleotide array analysis. BMC Bioinformatics (2002) 1.56
Transmembrane segment IV contributes a functionally important interface for oligomerization of the Class II G protein-coupled secretin receptor. J Biol Chem (2007) 1.55
Disseminating structural genomics data to the public: from a data dump to an animated story. Trends Biochem Sci (2006) 1.55
Four-dimensional docking: a fast and accurate account of discrete receptor flexibility in ligand docking. J Med Chem (2009) 1.54
Discovery of diverse thyroid hormone receptor antagonists by high-throughput docking. Proc Natl Acad Sci U S A (2003) 1.53
Excess polymorphisms in genes for membrane proteins in Plasmodium falciparum. Science (2002) 1.52
Structure-function studies of allosteric agonism at M2 muscarinic acetylcholine receptors. Mol Pharmacol (2007) 1.51
The GPCR Network: a large-scale collaboration to determine human GPCR structure and function. Nat Rev Drug Discov (2012) 1.50
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. Mol Pharmacol (2010) 1.49
Identifying conformational changes of the beta(2) adrenoceptor that enable accurate prediction of ligand/receptor interactions and screening for GPCR modulators. J Comput Aided Mol Des (2009) 1.48
Polar transmembrane interactions drive formation of ligand-specific and signal pathway-biased family B G protein-coupled receptor conformations. Proc Natl Acad Sci U S A (2013) 1.46
Identification of orthosteric and allosteric site mutations in M2 muscarinic acetylcholine receptors that contribute to ligand-selective signaling bias. J Biol Chem (2010) 1.46
Molecular mechanisms of action and in vivo validation of an M4 muscarinic acetylcholine receptor allosteric modulator with potential antipsychotic properties. Neuropsychopharmacology (2009) 1.45
Comprehensive identification of "druggable" protein ligand binding sites. Genome Inform (2004) 1.42
Type-II kinase inhibitor docking, screening, and profiling using modified structures of active kinase states. J Med Chem (2008) 1.38
RNA editing of the serotonin 5HT2C receptor and its effects on cell signalling, pharmacology and brain function. Pharmacol Ther (2008) 1.36
Docking and scoring with ICM: the benchmarking results and strategies for improvement. J Comput Aided Mol Des (2012) 1.34
Allosteric agonists of 7TM receptors: expanding the pharmacological toolbox. Trends Pharmacol Sci (2006) 1.32
Pharmacological discrimination of calcitonin receptor: receptor activity-modifying protein complexes. Mol Pharmacol (2005) 1.31
Structure based prediction of subtype-selectivity for adenosine receptor antagonists. Neuropharmacology (2010) 1.31
Targeting the RNA splicing machinery as a novel treatment strategy for pancreatic carcinoma. Cancer Res (2006) 1.29
Probing the molecular mechanism of interaction between 4-n-butyl-1-[4-(2-methylphenyl)-4-oxo-1-butyl]-piperidine (AC-42) and the muscarinic M(1) receptor: direct pharmacological evidence that AC-42 is an allosteric agonist. Mol Pharmacol (2005) 1.29
Relative affinity of angiotensin peptides and novel ligands at AT1 and AT2 receptors. Clin Sci (Lond) (2011) 1.29
Ab initio prediction of peptide-MHC binding geometry for diverse class I MHC allotypes. Proteins (2006) 1.29
Modeling of the aryl hydrocarbon receptor (AhR) ligand binding domain and its utility in virtual ligand screening to predict new AhR ligands. J Med Chem (2009) 1.28
Reversible and specific extracellular antagonism of receptor-histidine kinase signaling. J Biol Chem (2001) 1.28
The best of both worlds? Bitopic orthosteric/allosteric ligands of g protein-coupled receptors. Annu Rev Pharmacol Toxicol (2011) 1.26
Spatial approximation between the amino terminus of a peptide agonist and the top of the sixth transmembrane segment of the secretin receptor. J Biol Chem (2003) 1.26