Structure of the human dopamine D3 receptor in complex with a D2/D3 selective antagonist.

PubWeight™: 5.86‹?› | Rank: Top 1%

🔗 View Article (PMC 3058422)

Published in Science on November 19, 2010

Authors

Ellen Y T Chien1, Wei Liu, Qiang Zhao, Vsevolod Katritch, Gye Won Han, Michael A Hanson, Lei Shi, Amy Hauck Newman, Jonathan A Javitch, Vadim Cherezov, Raymond C Stevens

Author Affiliations

1: Department of Molecular Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA.

Articles citing this

(truncated to the top 100)

Structure of an agonist-bound human A2A adenosine receptor. Science (2011) 6.21

Molecular signatures of G-protein-coupled receptors. Nature (2013) 5.19

Structure of the human κ-opioid receptor in complex with JDTic. Nature (2012) 5.18

Agonist-bound adenosine A2A receptor structures reveal common features of GPCR activation. Nature (2011) 4.60

Structure-function of the G protein-coupled receptor superfamily. Annu Rev Pharmacol Toxicol (2012) 3.83

Structure of the human M2 muscarinic acetylcholine receptor bound to an antagonist. Nature (2012) 3.83

Crystal structure of a lipid G protein-coupled receptor. Science (2012) 3.78

Structure of the human histamine H1 receptor complex with doxepin. Nature (2011) 3.48

Structure of the CCR5 chemokine receptor-HIV entry inhibitor maraviroc complex. Science (2013) 3.17

Diversity and modularity of G protein-coupled receptor structures. Trends Pharmacol Sci (2011) 2.89

Structure of class B GPCR corticotropin-releasing factor receptor 1. Nature (2013) 2.87

Structure of the adenosine A(2A) receptor in complex with ZM241385 and the xanthines XAC and caffeine. Structure (2011) 2.84

Overcoming barriers to membrane protein structure determination. Nat Biotechnol (2011) 2.49

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

Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery. J Med Chem (2012) 2.10

Fusion partner toolchest for the stabilization and crystallization of G protein-coupled receptors. Structure (2012) 2.08

Crystal structure of oligomeric β1-adrenergic G protein-coupled receptors in ligand-free basal state. Nat Struct Mol Biol (2013) 2.06

Molecular determinants of selectivity and efficacy at the dopamine D3 receptor. J Med Chem (2012) 1.87

G-protein-coupled receptor inactivation by an allosteric inverse-agonist antibody. Nature (2012) 1.82

Progress in structure based drug design for G protein-coupled receptors. J Med Chem (2011) 1.82

Nanobody stabilization of G protein-coupled receptor conformational states. Curr Opin Struct Biol (2011) 1.75

Structure-based drug screening for G-protein-coupled receptors. Trends Pharmacol Sci (2012) 1.72

Lipidic cubic phase technologies for membrane protein structural studies. Curr Opin Struct Biol (2011) 1.67

Two distinct conformations of helix 6 observed in antagonist-bound structures of a beta1-adrenergic receptor. Proc Natl Acad Sci U S A (2011) 1.59

Membrane protein structure determination using crystallography and lipidic mesophases: recent advances and successes. Biochemistry (2012) 1.57

Ligand-dependent perturbation of the conformational ensemble for the GPCR β2 adrenergic receptor revealed by HDX. Structure (2011) 1.54

Thermostabilisation of an agonist-bound conformation of the human adenosine A(2A) receptor. J Mol Biol (2011) 1.54

The GPCR Network: a large-scale collaboration to determine human GPCR structure and function. Nat Rev Drug Discov (2012) 1.50

Lifting the lid on GPCRs: the role of extracellular loops. Br J Pharmacol (2012) 1.50

Automated sample-scanning methods for radiation damage mitigation and diffraction-based centering of macromolecular crystals. J Synchrotron Radiat (2011) 1.44

Structural insights into adrenergic receptor function and pharmacology. Trends Pharmacol Sci (2011) 1.42

Pharmacological modulation of chemokine receptor function. Br J Pharmacol (2012) 1.41

Action of molecular switches in GPCRs--theoretical and experimental studies. Curr Med Chem (2012) 1.40

The significance of G protein-coupled receptor crystallography for drug discovery. Pharmacol Rev (2011) 1.39

The Protein Structure Initiative: achievements and visions for the future. F1000 Biol Rep (2012) 1.38

Medication discovery for addiction: translating the dopamine D3 receptor hypothesis. Biochem Pharmacol (2012) 1.24

High resolution structure of the ba3 cytochrome c oxidase from Thermus thermophilus in a lipidic environment. PLoS One (2011) 1.23

Tools for GPCR drug discovery. Acta Pharmacol Sin (2012) 1.22

N-(3-fluoro-4-(4-(2-methoxy or 2,3-dichlorophenyl)piperazine-1-yl)butyl)arylcarboxamides as selective dopamine D3 receptor ligands: critical role of the carboxamide linker for D3 receptor selectivity. J Med Chem (2011) 1.20

Second extracellular loop of human glucagon-like peptide-1 receptor (GLP-1R) has a critical role in GLP-1 peptide binding and receptor activation. J Biol Chem (2011) 1.19

N-terminal T4 lysozyme fusion facilitates crystallization of a G protein coupled receptor. PLoS One (2012) 1.17

Toward structure determination using membrane-protein nanocrystals and microcrystals. Methods (2011) 1.16

Harvesting and cryo-cooling crystals of membrane proteins grown in lipidic mesophases for structure determination by macromolecular crystallography. J Vis Exp (2012) 1.13

Domain coupling in GPCRs: the engine for induced conformational changes. Trends Pharmacol Sci (2011) 1.12

Turning receptors on and off with intracellular pepducins: new insights into G-protein-coupled receptor drug development. J Biol Chem (2012) 1.10

GPCR stabilization using the bicelle-like architecture of mixed sterol-detergent micelles. Methods (2011) 1.09

Critical features for biosynthesis, stability, and functionality of a G protein-coupled receptor uncovered by all-versus-all mutations. Proc Natl Acad Sci U S A (2012) 1.09

Biophysical mapping of the adenosine A2A receptor. J Med Chem (2011) 1.08

Crystallizing membrane proteins using lipidic bicelles. Methods (2011) 1.08

Recognition in the face of diversity: interactions of heterotrimeric G proteins and G protein-coupled receptor (GPCR) kinases with activated GPCRs. J Biol Chem (2011) 1.07

Molecular basis of ligand dissociation in β-adrenergic receptors. PLoS One (2011) 1.06

Conformational dynamics of single G protein-coupled receptors in solution. J Phys Chem B (2011) 1.06

Molecular basis of secretin docking to its intact receptor using multiple photolabile probes distributed throughout the pharmacophore. J Biol Chem (2011) 1.06

New amphiphiles for membrane protein structural biology. Methods (2011) 1.03

Structural determinants of arrestin functions. Prog Mol Biol Transl Sci (2013) 1.01

The extracellular loops of Smoothened play a regulatory role in control of Hedgehog pathway activation. Development (2012) 1.01

Characterization of extrastriatal D2 in vivo specific binding of [¹⁸F](N-methyl)benperidol using PET. Synapse (2012) 1.01

Small molecule drug discovery at the glucagon-like peptide-1 receptor. Exp Diabetes Res (2012) 1.01

Lipid cubic phase as a membrane mimetic for integral membrane protein enzymes. Proc Natl Acad Sci U S A (2011) 1.00

Identification of the GPR55 agonist binding site using a novel set of high-potency GPR55 selective ligands. Biochemistry (2011) 1.00

Biophysical fragment screening of the β1-adrenergic receptor: identification of high affinity arylpiperazine leads using structure-based drug design. J Med Chem (2013) 0.99

Engineering an ultra-thermostable β(1)-adrenoceptor. J Mol Biol (2011) 0.99

Predicted structure of agonist-bound glucagon-like peptide 1 receptor, a class B G protein-coupled receptor. Proc Natl Acad Sci U S A (2012) 0.98

Current trends in α-helical membrane protein crystallization: an update. Protein Sci (2012) 0.98

Fragment screening at adenosine-A(3) receptors in living cells using a fluorescence-based binding assay. Chem Biol (2012) 0.98

New insights for drug design from the X-ray crystallographic structures of G-protein-coupled receptors. Mol Pharmacol (2012) 0.98

Characterization of lipid matrices for membrane protein crystallization by high-throughput small angle X-ray scattering. Methods (2011) 0.98

Allosteric and orthosteric sites in CC chemokine receptor (CCR5), a chimeric receptor approach. J Biol Chem (2011) 0.98

Ice breaking in GPCR structural biology. Acta Pharmacol Sin (2012) 0.97

Crystallizing membrane proteins for structure-function studies using lipidic mesophases. Biochem Soc Trans (2011) 0.97

Comprehensive analysis of host gene expression in Autographa californica nucleopolyhedrovirus-infected Spodoptera frugiperda cells. Virology (2011) 0.96

Discovery and characterization of a G protein-biased agonist that inhibits β-arrestin recruitment to the D2 dopamine receptor. Mol Pharmacol (2014) 0.96

GOMoDo: A GPCRs online modeling and docking webserver. PLoS One (2013) 0.96

Evaluation of the Pichia pastoris expression system for the production of GPCRs for structural analysis. Microb Cell Fact (2011) 0.95

Chemotype-selective modes of action of κ-opioid receptor agonists. J Biol Chem (2013) 0.95

Molecular dynamics simulations reveal specific interactions of post-translational palmitoyl modifications with rhodopsin in membranes. J Am Chem Soc (2012) 0.95

Beyond small-molecule SAR: using the dopamine D3 receptor crystal structure to guide drug design. Adv Pharmacol (2014) 0.95

Computational design of membrane proteins. Structure (2012) 0.95

Comparison of three GPCR structural templates for modeling of the P2Y12 nucleotide receptor. J Comput Aided Mol Des (2011) 0.95

In silico analysis of the binding of agonists and blockers to the β2-adrenergic receptor. J Mol Graph Model (2011) 0.94

Free energy landscape of G-protein coupled receptors, explored by accelerated molecular dynamics. Phys Chem Chem Phys (2014) 0.94

Bihelix: Towards de novo structure prediction of an ensemble of G-protein coupled receptor conformations. Proteins (2011) 0.94

Structure and function of serotonin G protein-coupled receptors. Pharmacol Ther (2015) 0.94

Engineering a prokaryotic Cys-loop receptor with a third functional domain. J Biol Chem (2011) 0.94

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

Structure-based ligand discovery targeting orthosteric and allosteric pockets of dopamine receptors. Mol Pharmacol (2013) 0.93

Structural model of ligand-G protein-coupled receptor (GPCR) complex based on experimental double mutant cycle data: MT7 snake toxin bound to dimeric hM1 muscarinic receptor. J Biol Chem (2011) 0.93

GPCR agonist binding revealed by modeling and crystallography. Trends Pharmacol Sci (2011) 0.93

Naturally evolved G protein-coupled receptors adopt metastable conformations. Proc Natl Acad Sci U S A (2012) 0.92

A single glycine in extracellular loop 1 is the critical determinant for pharmacological specificity of dopamine D2 and D3 receptors. Mol Pharmacol (2013) 0.92

Membrane-sensitive conformational states of helix 8 in the metabotropic Glu2 receptor, a class C GPCR. PLoS One (2012) 0.91

GPCR-SSFE: a comprehensive database of G-protein-coupled receptor template predictions and homology models. BMC Bioinformatics (2011) 0.91

A novel G protein-coupled receptor of Schistosoma mansoni (SmGPR-3) is activated by dopamine and is widely expressed in the nervous system. PLoS Negl Trop Dis (2012) 0.91

Allosteric modulation of metabotropic glutamate receptors. Adv Pharmacol (2011) 0.91

The N-terminal region of the dopamine D2 receptor, a rhodopsin-like GPCR, regulates correct integration into the plasma membrane and endocytic routes. Br J Pharmacol (2012) 0.90

G protein-coupled receptors--recent advances. Acta Biochim Pol (2012) 0.90

Elucidation of G-protein and β-arrestin functional selectivity at the dopamine D2 receptor. Proc Natl Acad Sci U S A (2015) 0.90

Structural probing of off-target G protein-coupled receptor activities within a series of adenosine/adenine congeners. PLoS One (2014) 0.90

Differential contribution of TM6 and TM12 to the pore of CFTR identified by three sulfonylurea-based blockers. Pflugers Arch (2011) 0.90

Articles cited by this

Crystal structure of rhodopsin: A G protein-coupled receptor. Science (2000) 28.60

High-resolution crystal structure of an engineered human beta2-adrenergic G protein-coupled receptor. Science (2007) 20.32

Structure of a beta1-adrenergic G-protein-coupled receptor. Nature (2008) 11.97

GPCR engineering yields high-resolution structural insights into beta2-adrenergic receptor function. Science (2007) 11.74

The 2.6 angstrom crystal structure of a human A2A adenosine receptor bound to an antagonist. Science (2008) 11.74

The retinal conformation and its environment in rhodopsin in light of a new 2.2 A crystal structure. J Mol Biol (2004) 7.38

Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics. Nature (1990) 6.18

A specific cholesterol binding site is established by the 2.8 A structure of the human beta2-adrenergic receptor. Structure (2008) 6.01

The probable arrangement of the helices in G protein-coupled receptors. EMBO J (1993) 3.57

Activation of the beta 2-adrenergic receptor involves disruption of an ionic lock between the cytoplasmic ends of transmembrane segments 3 and 6. J Biol Chem (2001) 3.49

Dopamine D2 receptors form higher order oligomers at physiological expression levels. EMBO J (2008) 2.99

Selective inhibition of cocaine-seeking behaviour by a partial dopamine D3 receptor agonist. Nature (1999) 2.89

Identification of two distinct inactive conformations of the beta2-adrenergic receptor reconciles structural and biochemical observations. Proc Natl Acad Sci U S A (2009) 2.77

G protein-coupled receptors. I. Diversity of receptor-ligand interactions. J Biol Chem (1998) 2.64

Functional role of the "ionic lock"--an interhelical hydrogen-bond network in family A heptahelical receptors. J Mol Biol (2008) 2.47

Current perspectives on selective dopamine D(3) receptor antagonists as pharmacotherapeutics for addictions and related disorders. Ann N Y Acad Sci (2010) 2.36

The binding site of aminergic G protein-coupled receptors: the transmembrane segments and second extracellular loop. Annu Rev Pharmacol Toxicol (2002) 2.27

The second extracellular loop of the dopamine D2 receptor lines the binding-site crevice. Proc Natl Acad Sci U S A (2004) 2.10

The D3 dopamine receptor: neurobiology and potential clinical relevance. Pharmacol Rev (1997) 2.09

Dopamine D3 receptor antagonism inhibits cocaine-seeking and cocaine-enhanced brain reward in rats. J Neurosci (2002) 1.84

Allele-specific activation of genetically engineered receptors. J Biol Chem (1991) 1.72

The novel dopamine D3 receptor antagonist NGB 2904 inhibits cocaine's rewarding effects and cocaine-induced reinstatement of drug-seeking behavior in rats. Neuropsychopharmacology (2005) 1.69

Stabilization of the human beta2-adrenergic receptor TM4-TM3-TM5 helix interface by mutagenesis of Glu122(3.41), a critical residue in GPCR structure. J Mol Biol (2007) 1.63

Pharmacology of human dopamine D3 receptor expressed in a mammalian cell line: comparison with D2 receptor. Eur J Pharmacol (1992) 1.57

N-(4-(4-(2,3-dichloro- or 2-methoxyphenyl)piperazin-1-yl)butyl)heterobiarylcarboxamides with functionalized linking chains as high affinity and enantioselective D3 receptor antagonists. J Med Chem (2009) 1.52

Acute administration of SB-277011A, NGB 2904, or BP 897 inhibits cocaine cue-induced reinstatement of drug-seeking behavior in rats: role of dopamine D3 receptors. Synapse (2005) 1.43

Phenotypic analysis of dopamine receptor knockout mice; recent insights into the functional specificity of dopamine receptor subtypes. Neuropharmacology (2004) 1.37

The structural evolution of dopamine D3 receptor ligands: structure-activity relationships and selected neuropharmacological aspects. Pharmacol Ther (2006) 1.33

The selective dopamine D3 receptor antagonists SB-277011A and NGB 2904 and the putative partial D3 receptor agonist BP-897 attenuate methamphetamine-enhanced brain stimulation reward in rats. Psychopharmacology (Berl) (2007) 1.30

Dopamine D4/D2 receptor selectivity is determined by A divergent aromatic microdomain contained within the second, third, and seventh membrane-spanning segments. Mol Pharmacol (1999) 1.29

The first transmembrane segment of the dopamine D2 receptor: accessibility in the binding-site crevice and position in the transmembrane bundle. Biochemistry (2001) 1.20

Identification and characterization of novel properties of the human D3 dopamine receptor. Mol Cell Neurosci (2004) 1.09

Antipsychotics with inverse agonist activity at the dopamine D3 receptor. J Neural Transm (Vienna) (1996) 0.95

Identification of transmembrane regions critical for ligand binding to the human D3 dopamine receptor using various D3/D1 transmembrane chimeras. Mol Pharmacol (1998) 0.93

Articles by these authors

Disability-adjusted life years (DALYs) for 291 diseases and injuries in 21 regions, 1990-2010: a systematic analysis for the Global Burden of Disease Study 2010. Lancet (2012) 41.47

Years lived with disability (YLDs) for 1160 sequelae of 289 diseases and injuries 1990-2010: a systematic analysis for the Global Burden of Disease Study 2010. Lancet (2012) 26.95

High-resolution crystal structure of an engineered human beta2-adrenergic G protein-coupled receptor. Science (2007) 20.32

Guidelines for the use and interpretation of assays for monitoring autophagy. Autophagy (2012) 20.08

Leukemic IDH1 and IDH2 mutations result in a hypermethylation phenotype, disrupt TET2 function, and impair hematopoietic differentiation. Cancer Cell (2010) 15.20

GPCR engineering yields high-resolution structural insights into beta2-adrenergic receptor function. Science (2007) 11.74

The 2.6 angstrom crystal structure of a human A2A adenosine receptor bound to an antagonist. Science (2008) 11.74

Deletion of IKZF1 and prognosis in acute lymphoblastic leukemia. N Engl J Med (2009) 10.54

Structures of the CXCR4 chemokine GPCR with small-molecule and cyclic peptide antagonists. Science (2010) 10.30

Genome-wide association studies of 14 agronomic traits in rice landraces. Nat Genet (2010) 8.75

Functional selectivity and classical concepts of quantitative pharmacology. J Pharmacol Exp Ther (2006) 7.03

The role of Tet3 DNA dioxygenase in epigenetic reprogramming by oocytes. Nature (2011) 6.73

Association of FKBP5 polymorphisms and childhood abuse with risk of posttraumatic stress disorder symptoms in adults. JAMA (2008) 6.60

Crystallizing membrane proteins using lipidic mesophases. Nat Protoc (2009) 6.36

Structure of an agonist-bound human A2A adenosine receptor. Science (2011) 6.21

A specific cholesterol binding site is established by the 2.8 A structure of the human beta2-adrenergic receptor. Structure (2008) 6.01

Structural genomics of the Thermotoga maritima proteome implemented in a high-throughput structure determination pipeline. Proc Natl Acad Sci U S A (2002) 6.00

High-throughput genotyping by whole-genome resequencing. Genome Res (2009) 5.74

Structure of the human κ-opioid receptor in complex with JDTic. Nature (2012) 5.18

An inhibitor of mutant IDH1 delays growth and promotes differentiation of glioma cells. Science (2013) 5.10

JAK mutations in high-risk childhood acute lymphoblastic leukemia. Proc Natl Acad Sci U S A (2009) 4.98

A map of rice genome variation reveals the origin of cultivated rice. Nature (2012) 4.92

Influence of child abuse on adult depression: moderation by the corticotropin-releasing hormone receptor gene. Arch Gen Psychiatry (2008) 4.65

Sequence and analysis of rice chromosome 4. Nature (2002) 4.39

Rearrangement of CRLF2 in B-progenitor- and Down syndrome-associated acute lymphoblastic leukemia. Nat Genet (2009) 4.35

The mechanism of a neurotransmitter:sodium symporter--inward release of Na+ and substrate is triggered by substrate in a second binding site. Mol Cell (2008) 4.29

The Rice Annotation Project Database (RAP-DB): 2008 update. Nucleic Acids Res (2007) 4.23

Genome-wide association study of flowering time and grain yield traits in a worldwide collection of rice germplasm. Nat Genet (2011) 4.19

Structure-function of the G protein-coupled receptor superfamily. Annu Rev Pharmacol Toxicol (2012) 3.83

Crystal structure of a lipid G protein-coupled receptor. Science (2012) 3.78

Targeted inhibition of mutant IDH2 in leukemia cells induces cellular differentiation. Science (2013) 3.72

Rearrangement of CRLF2 is associated with mutation of JAK kinases, alteration of IKZF1, Hispanic/Latino ethnicity, and a poor outcome in pediatric B-progenitor acute lymphoblastic leukemia. Blood (2010) 3.66

Serial femtosecond crystallography of G protein-coupled receptors. Science (2013) 3.58

Structure of the human histamine H1 receptor complex with doxepin. Nature (2011) 3.48

Acquired resistance to crizotinib from a mutation in CD74-ROS1. N Engl J Med (2013) 3.42

Structural basis for allosteric regulation of GPCRs by sodium ions. Science (2012) 3.40

Adenosine A1 receptors mediate local anti-nociceptive effects of acupuncture. Nat Neurosci (2010) 3.38

Mutations in SLC20A2 link familial idiopathic basal ganglia calcification with phosphate homeostasis. Nat Genet (2012) 3.34

LSD1 is a subunit of the NuRD complex and targets the metastasis programs in breast cancer. Cell (2009) 3.34

A comprehensive structure-based alignment of prokaryotic and eukaryotic neurotransmitter/Na+ symporters (NSS) aids in the use of the LeuT structure to probe NSS structure and function. Mol Pharmacol (2006) 3.23

Structure of the CCR5 chemokine receptor-HIV entry inhibitor maraviroc complex. Science (2013) 3.17

Curated genome annotation of Oryza sativa ssp. japonica and comparative genome analysis with Arabidopsis thaliana. Genome Res (2007) 3.13

Structure of the human smoothened receptor bound to an antitumour agent. Nature (2013) 3.08

Biased signaling pathways in β2-adrenergic receptor characterized by 19F-NMR. Science (2012) 3.07

A novel microRNA targeting HDAC5 regulates osteoblast differentiation in mice and contributes to primary osteoporosis in humans. J Clin Invest (2009) 3.03

The molecular mechanism governing the oncogenic potential of SOX2 in breast cancer. J Biol Chem (2008) 3.01

Dopamine D2 receptors form higher order oligomers at physiological expression levels. EMBO J (2008) 2.99

Allosteric communication between protomers of dopamine class A GPCR dimers modulates activation. Nat Chem Biol (2009) 2.98

Structure of the nociceptin/orphanin FQ receptor in complex with a peptide mimetic. Nature (2012) 2.96

Microscale fluorescent thermal stability assay for membrane proteins. Structure (2008) 2.95

Diversity and modularity of G protein-coupled receptor structures. Trends Pharmacol Sci (2011) 2.89

SNOSID, a proteomic method for identification of cysteine S-nitrosylation sites in complex protein mixtures. Proc Natl Acad Sci U S A (2006) 2.89

Beta2 adrenergic receptor activation. Modulation of the proline kink in transmembrane 6 by a rotamer toggle switch. J Biol Chem (2002) 2.87

Structure of the human glucagon class B G-protein-coupled receptor. Nature (2013) 2.86