Probing the existence of G protein-coupled receptor dimers by positive and negative ligand-dependent cooperative binding.

PubWeight™: 1.20‹?› | Rank: Top 10%

🔗 View Article (PMID 16926282)

Published in Mol Pharmacol on August 22, 2006

Authors

Laura Albizu1, Marie-Noëlle Balestre, Christophe Breton, Jean-Philippe Pin, Maurice Manning, Bernard Mouillac, Claude Barberis, Thierry Durroux

Author Affiliations

1: Institut de Génomique Fonctionnelle, Centre National de la Recherche Scientifique Unité Mixte Recherche 5203, 141 rue de la Cardonille, 34094 Montpellier CEDEX 5, France.

Articles citing this

Seven transmembrane receptors as shapeshifting proteins: the impact of allosteric modulation and functional selectivity on new drug discovery. Pharmacol Rev (2010) 3.27

Function, structure and therapeutic potential of complement C5a receptors. Br J Pharmacol (2007) 2.25

Time-resolved FRET between GPCR ligands reveals oligomers in native tissues. Nat Chem Biol (2010) 2.15

Allostery at G protein-coupled receptor homo- and heteromers: uncharted pharmacological landscapes. Pharmacol Rev (2010) 1.89

G protein-coupled receptor oligomerization revisited: functional and pharmacological perspectives. Pharmacol Rev (2014) 1.82

Oxytocin and vasopressin agonists and antagonists as research tools and potential therapeutics. J Neuroendocrinol (2012) 1.63

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

HTRF: A technology tailored for drug discovery - a review of theoretical aspects and recent applications. Curr Chem Genomics (2009) 1.39

Metabotropic glutamate mGlu2 receptor is necessary for the pharmacological and behavioral effects induced by hallucinogenic 5-HT2A receptor agonists. Neurosci Lett (2011) 1.21

Functional importance of a structurally distinct homodimeric complex of the family B G protein-coupled secretin receptor. Mol Pharmacol (2009) 1.12

G-protein-coupled receptor heteromers: function and ligand pharmacology. Br J Pharmacol (2007) 1.07

G protein activation by the leukotriene B4 receptor dimer. Evidence for an absence of trans-activation. J Biol Chem (2008) 1.04

Functional crosstalk and heteromerization of serotonin 5-HT2A and dopamine D2 receptors. Neuropharmacology (2011) 0.99

Trans-activation between 7TM domains: implication in heterodimeric GABAB receptor activation. EMBO J (2010) 0.96

A new mechanism of allostery in a G protein-coupled receptor dimer. Nat Chem Biol (2014) 0.93

On the fitting of binding data when receptor dimerization is suspected. Br J Pharmacol (2008) 0.92

BRET and Time-resolved FRET strategy to study GPCR oligomerization: from cell lines toward native tissues. Front Endocrinol (Lausanne) (2012) 0.92

Direct measurement of thermal stability of expressed CCR5 and stabilization by small molecule ligands. Biochemistry (2010) 0.89

G protein-coupled receptors: walking hand-in-hand, talking hand-in-hand? Br J Pharmacol (2011) 0.86

Heteromerization of G protein-coupled receptors: relevance to neurological disorders and neurotherapeutics. CNS Neurol Disord Drug Targets (2010) 0.84

Caged naloxone reveals opioid signaling deactivation kinetics. Mol Pharmacol (2013) 0.80

G-protein-coupled receptor heteromers or how neurons can display differently flavoured patterns in response to the same neurotransmitter. Br J Pharmacol (2009) 0.80

Microscopy: GPCR dimers moving closer. Nat Chem Biol (2010) 0.78

Neurotransmitter receptor heteromers in neurodegenerative diseases and neural plasticity. J Neural Transm (Vienna) (2008) 0.78

Receptor oligomerization: from early evidence to current understanding in class B GPCRs. Front Endocrinol (Lausanne) (2013) 0.77

Dual allosteric modulation of opioid antinociceptive potency by α2A-adrenoceptors. Neuropharmacology (2015) 0.76

'Partial' competition of heterobivalent ligand binding may be mistaken for allosteric interactions: a comparison of different target interaction models. Br J Pharmacol (2015) 0.76

Contributions of fluorescence techniques to understanding G protein-coupled receptor dimerisation. Biophys Rev (2012) 0.75

Articles by these authors

IUPHAR-DB: the IUPHAR database of G protein-coupled receptors and ion channels. Nucleic Acids Res (2008) 3.76

Cell-surface protein-protein interaction analysis with time-resolved FRET and snap-tag technologies: application to GPCR oligomerization. Nat Methods (2008) 2.88

Closed state of both binding domains of homodimeric mGlu receptors is required for full activity. Nat Struct Mol Biol (2004) 2.58

Building a new conceptual framework for receptor heteromers. Nat Chem Biol (2009) 2.41

Time-resolved FRET between GPCR ligands reveals oligomers in native tissues. Nat Chem Biol (2010) 2.15

Virtual screening workflow development guided by the "receiver operating characteristic" curve approach. Application to high-throughput docking on metabotropic glutamate receptor subtype 4. J Med Chem (2005) 2.06

Positioning trocars for performing sleeve gastrectomy. Points of controversy. Obes Surg (2015) 1.90

G protein-coupled receptor oligomerization revisited: functional and pharmacological perspectives. Pharmacol Rev (2014) 1.82

Oxytocin and vasopressin V1a and V2 receptors form constitutive homo- and heterodimers during biosynthesis. Mol Endocrinol (2002) 1.76

Evidence for a single heptahelical domain being turned on upon activation of a dimeric GPCR. EMBO J (2005) 1.72

Asymmetric conformational changes in a GPCR dimer controlled by G-proteins. EMBO J (2006) 1.66

Maternal perinatal undernutrition drastically reduces postnatal leptin surge and affects the development of arcuate nucleus proopiomelanocortin neurons in neonatal male rat pups. Endocrinology (2007) 1.59

Allosteric modulators of group I metabotropic glutamate receptors: novel subtype-selective ligands and therapeutic perspectives. Curr Opin Pharmacol (2002) 1.58

Structural insights into biased G protein-coupled receptor signaling revealed by fluorescence spectroscopy. Proc Natl Acad Sci U S A (2012) 1.57

Activation of a dimeric metabotropic glutamate receptor by intersubunit rearrangement. J Biol Chem (2007) 1.57

N-{4-Chloro-2-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]phenyl}-2-hydroxybenzamide (CPPHA) acts through a novel site as a positive allosteric modulator of group 1 metabotropic glutamate receptors. Mol Pharmacol (2007) 1.56

Asymmetric functioning of dimeric metabotropic glutamate receptors disclosed by positive allosteric modulators. J Biol Chem (2005) 1.55

A single subunit (GB2) is required for G-protein activation by the heterodimeric GABA(B) receptor. J Biol Chem (2001) 1.49

Dimers and beyond: The functional puzzles of class C GPCRs. Pharmacol Ther (2011) 1.48

Interaction of novel positive allosteric modulators of metabotropic glutamate receptor 5 with the negative allosteric antagonist site is required for potentiation of receptor responses. Mol Pharmacol (2007) 1.46

The heptahelical domain of GABA(B2) is activated directly by CGP7930, a positive allosteric modulator of the GABA(B) receptor. J Biol Chem (2004) 1.45

Peptide and non-peptide agonists and antagonists for the vasopressin and oxytocin V1a, V1b, V2 and OT receptors: research tools and potential therapeutic agents. Prog Brain Res (2008) 1.43

Sex- and diet-specific changes of imprinted gene expression and DNA methylation in mouse placenta under a high-fat diet. PLoS One (2010) 1.41

Cell surface detection of membrane protein interaction with homogeneous time-resolved fluorescence resonance energy transfer technology. Anal Biochem (2004) 1.40

CRF receptor 1 regulates anxiety behavior via sensitization of 5-HT2 receptor signaling. Nat Neurosci (2010) 1.38

Heterodimerization of V1a and V2 vasopressin receptors determines the interaction with beta-arrestin and their trafficking patterns. Proc Natl Acad Sci U S A (2004) 1.38

No ligand binding in the GB2 subunit of the GABA(B) receptor is required for activation and allosteric interaction between the subunits. J Neurosci (2002) 1.36

International Union of Pharmacology. LVI. Ghrelin receptor nomenclature, distribution, and function. Pharmacol Rev (2005) 1.35

Crosstalk between GABAB and mGlu1a receptors reveals new insight into GPCR signal integration. EMBO J (2009) 1.32

Discovery of thieno[2,3-c]pyridines as potent COT inhibitors. Bioorg Med Chem Lett (2008) 1.30

PROKR2 missense mutations associated with Kallmann syndrome impair receptor signalling activity. Hum Mol Genet (2008) 1.30

Maternal stress alters endocrine function of the feto-placental unit in rats. Am J Physiol Endocrinol Metab (2007) 1.27

A new approach to analyze cell surface protein complexes reveals specific heterodimeric metabotropic glutamate receptors. FASEB J (2010) 1.27

Locking the dimeric GABA(B) G-protein-coupled receptor in its active state. J Neurosci (2004) 1.25

A single olfactory receptor specifically binds a set of odorant molecules. Eur J Neurosci (2002) 1.25

The metabotropic glutamate receptor mGluR5 is endocytosed by a clathrin-independent pathway. J Biol Chem (2003) 1.23

G protein activation by serotonin type 4 receptor dimers: evidence that turning on two protomers is more efficient. J Biol Chem (2011) 1.21

Closure of the Venus flytrap module of mGlu8 receptor and the activation process: Insights from mutations converting antagonists into agonists. Proc Natl Acad Sci U S A (2002) 1.21

Metabotropic receptors for glutamate and GABA in pain. Brain Res Rev (2008) 1.20

Real-time analysis of agonist-induced activation of protease-activated receptor 1/Galphai1 protein complex measured by bioluminescence resonance energy transfer in living cells. Mol Pharmacol (2007) 1.17

Characterization of (2S,4R)-1-[5-chloro-1-[(2,4-dimethoxyphenyl)sulfonyl]-3-(2-methoxy-phenyl)-2-oxo-2,3-dihydro-1H-indol-3-yl]-4-hydroxy-N,N-dimethyl-2-pyrrolidine carboxamide (SSR149415), a selective and orally active vasopressin V1b receptor antagonist. J Pharmacol Exp Ther (2002) 1.16

Homer-dependent cell surface expression of metabotropic glutamate receptor type 5 in neurons. Mol Cell Neurosci (2002) 1.15

Assembly-dependent surface targeting of the heterodimeric GABAB Receptor is controlled by COPI but not 14-3-3. Mol Biol Cell (2005) 1.15

Coupling of agonist binding to effector domain activation in metabotropic glutamate-like receptors. J Biol Chem (2006) 1.14

Functioning of the dimeric GABA(B) receptor extracellular domain revealed by glycan wedge scanning. EMBO J (2008) 1.14

A fluorescent ligand-binding alternative using Tag-lite® technology. J Biomol Screen (2010) 1.13

Common structural requirements for heptahelical domain function in class A and class C G protein-coupled receptors. J Biol Chem (2007) 1.13

Distinct roles of metabotropic glutamate receptor dimerization in agonist activation and G-protein coupling. Proc Natl Acad Sci U S A (2012) 1.12

Electrophysiological and behavioral evidence that modulation of metabotropic glutamate receptor 4 with a new agonist reverses experimental parkinsonism. FASEB J (2009) 1.12

Functional crosstalk between GPCRs: with or without oligomerization. Curr Opin Pharmacol (2009) 1.12

D-myo-inositol 1-phosphate as a surrogate of D-myo-inositol 1,4,5-tris phosphate to monitor G protein-coupled receptor activation. Anal Biochem (2006) 1.11

GPCR-OKB: the G Protein Coupled Receptor Oligomer Knowledge Base. Bioinformatics (2010) 1.09

The asymmetric/symmetric activation of GPCR dimers as a possible mechanistic rationale for multiple signalling pathways. Trends Pharmacol Sci (2009) 1.09

The intracellular loops of the GB2 subunit are crucial for G-protein coupling of the heteromeric gamma-aminobutyrate B receptor. Mol Pharmacol (2002) 1.08

Angiotensin-converting enzyme 2 (ACE2) and ACE activities display tissue-specific sensitivity to undernutrition-programmed hypertension in the adult rat. Hypertension (2005) 1.08

Interdomain movements in metabotropic glutamate receptor activation. Proc Natl Acad Sci U S A (2011) 1.07

A new family of receptor tyrosine kinases with a venus flytrap binding domain in insects and other invertebrates activated by aminoacids. PLoS One (2009) 1.07

Molecular determinants involved in the allosteric control of agonist affinity in the GABAB receptor by the GABAB2 subunit. J Biol Chem (2004) 1.05

The oligomeric state sets GABA(B) receptor signalling efficacy. EMBO J (2011) 1.05

G protein activation by the leukotriene B4 receptor dimer. Evidence for an absence of trans-activation. J Biol Chem (2008) 1.04

Illuminating the activation mechanisms and allosteric properties of metabotropic glutamate receptors. Proc Natl Acad Sci U S A (2013) 1.04

Requirements and ontology for a G protein-coupled receptor oligomerization knowledge base. BMC Bioinformatics (2007) 1.04

GABAB receptor activation protects neurons from apoptosis via IGF-1 receptor transactivation. J Neurosci (2010) 1.03

Nutritional manipulations in the perinatal period program adipose tissue in offspring. Am J Physiol Endocrinol Metab (2013) 1.03

HPA axis programming by maternal undernutrition in the male rat offspring. Psychoneuroendocrinology (2007) 1.02

Differential association modes of the thrombin receptor PAR1 with Galphai1, Galpha12, and beta-arrestin 1. FASEB J (2010) 1.02

Toward efficient drug screening by homogeneous assays based on the development of new fluorescent vasopressin and oxytocin receptor ligands. J Med Chem (2007) 1.02

Sequential inter- and intrasubunit rearrangements during activation of dimeric metabotropic glutamate receptor 1. Sci Signal (2012) 1.01

Synthesis and biological evaluation of 1-amino-2-phosphonomethylcyclopropanecarboxylic acids, new group III metabotropic glutamate receptor agonists. J Med Chem (2007) 1.00

Dominant role of GABAB2 and Gbetagamma for GABAB receptor-mediated-ERK1/2/CREB pathway in cerebellar neurons. Cell Signal (2007) 1.00

A model for the functioning of family 3 GPCRs. Trends Pharmacol Sci (2002) 0.99

Biased agonist pharmacochaperones of the AVP V2 receptor may treat congenital nephrogenic diabetes insipidus. J Am Soc Nephrol (2009) 0.99

Functional selective oxytocin-derived agonists discriminate between individual G protein family subtypes. J Biol Chem (2011) 0.98

The complexity of their activation mechanism opens new possibilities for the modulation of mGlu and GABAB class C G protein-coupled receptors. Neuropharmacology (2010) 0.96

A novel selective metabotropic glutamate receptor 4 agonist reveals new possibilities for developing subtype selective ligands with therapeutic potential. FASEB J (2012) 0.96

Common and selective molecular determinants involved in metabotopic glutamate receptor agonist activity. J Med Chem (2002) 0.96

Maternal prenatal undernutrition programs adipose tissue gene expression in adult male rat offspring under high-fat diet. Am J Physiol Endocrinol Metab (2011) 0.96

Trans-activation between 7TM domains: implication in heterodimeric GABAB receptor activation. EMBO J (2010) 0.96

Insider access: pepducin symposium explores a new approach to GPCR modulation. Ann N Y Acad Sci (2009) 0.96

Inhibition of heterotrimeric G protein signaling by a small molecule acting on Galpha subunit. J Biol Chem (2009) 0.95

The metabotropic glutamate receptor mGlu7 activates phospholipase C, translocates munc-13-1 protein, and potentiates glutamate release at cerebrocortical nerve terminals. J Biol Chem (2010) 0.95

Laparoscopic Roux-en-Y gastric bypass with the absorbable bidirectional monofilament barbed suture Stratafix®: the hand-sewn technique. Obes Surg (2015) 0.94

The constitutively active V2 receptor mutants conferring NSIAD are weakly sensitive to agonist and antagonist regulation. PLoS One (2009) 0.94