GPCR engineering yields high-resolution structural insights into beta2-adrenergic receptor function

scientific article

GPCR engineering yields high-resolution structural insights into beta2-adrenergic receptor function is …
instance of (P31):
scholarly articleQ13442814

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P356DOI10.1126/SCIENCE.1150609
P3181OpenCitations bibliographic resource ID630752
P698PubMed publication ID17962519
P5875ResearchGate publication ID5882507

P50authorBrian KobilkaQ80907
Raymond C. StevensQ7298638
Vadim CherezovQ28320126
William I WeisQ42325569
Søren G. F. RasmussenQ56896313
Tong Sun KobilkaQ69506919
Michael A HansonQ91742960
P2093author name stringHee-Jung Choi
Daniel M Rosenbaum
Foon Sun Thian
Søren G F Rasmussen
Xiao-Jie Yao
P2860cites workHigh-resolution crystal structure of an engineered human beta2-adrenergic G protein-coupled receptorQ24657484
GPCRDB information system for G protein-coupled receptorsQ24681765
Crystal structure of the human beta2 adrenergic G-protein-coupled receptorQ27648868
Structure of bacteriophage T4 lysozyme refined at 1.7 A resolutionQ27728620
Protein flexibility and adaptability seen in 25 crystal forms of T4 lysozymeQ27729775
PRODRG: a tool for high-throughput crystallography of protein-ligand complexesQ27860633
Structural basis of beta-adrenergic receptor subtype specificity studied with chimeric beta 1/beta 2-adrenergic receptorsQ28359891
Agonist-induced conformational changes at the cytoplasmic side of transmembrane segment 6 in the beta 2 adrenergic receptor mapped by site-selective fluorescent labeling.Q31705336
Agonists induce conformational changes in transmembrane domains III and VI of the beta2 adrenoceptorQ33887729
Stabilization of phage T4 lysozyme by engineered disulfide bondsQ34300374
Identification of residues required for ligand binding to the beta-adrenergic receptorQ34633995
Chimeric alpha 2-,beta 2-adrenergic receptors: delineation of domains involved in effector coupling and ligand binding specificityQ34681325
Crystal structures of fusion proteins with large-affinity tagsQ35161672
Role of group-conserved residues in the helical core of beta2-adrenergic receptorQ35758611
Agonist-induced conformational changes in the G-protein-coupling domain of the beta 2 adrenergic receptorQ35925395
The role of internal water molecules in the structure and function of the rhodopsin family of G protein-coupled receptorsQ36685974
A dileucine motif in the C terminus of the beta2-adrenergic receptor is involved in receptor internalizationQ36799040
Conformational complexity of G-protein-coupled receptorsQ36880905
Kinetic analysis of G protein-coupled receptor signaling using fluorescence resonance energy transfer in living cellsQ36940133
Involvement of Asn-293 in stereospecific agonist recognition and in activation of the beta 2-adrenergic receptorQ37392202
Beta2 adrenergic receptor activation. Modulation of the proline kink in transmembrane 6 by a rotamer toggle switchQ40712100
Activation of the beta 2-adrenergic receptor involves disruption of an ionic lock between the cytoplasmic ends of transmembrane segments 3 and 6.Q40803165
The forgotten serine. A critical role for Ser-2035.42 in ligand binding to and activation of the beta 2-adrenergic receptor.Q40858064
Constitutive activation of G protein-coupled receptors as a result of selective substitution of a conserved leucine residue in transmembrane helix III.Q40862862
Structural instability of a constitutively active G protein-coupled receptor. Agonist-independent activation due to conformational flexibilityQ41132503
Sequential binding of agonists to the beta2 adrenoceptor. Kinetic evidence for intermediate conformational statesQ42046378
Identification of a conserved switch residue responsible for selective constitutive activation of the beta2-adrenergic receptorQ42450308
Functionally different agonists induce distinct conformations in the G protein coupling domain of the beta 2 adrenergic receptorQ43586918
Beta(1)-selective agonist (-)-1-(3,4-dimethoxyphenetylamino)-3-(3,4-dihydroxy)-2-propanol [(-)-RO363] differentially interacts with key amino acids responsible for beta(1)-selective binding in resting and active statesQ43926085
The retinal conformation and its environment in rhodopsin in light of a new 2.2 A crystal structureQ45029374
Coupling ligand structure to specific conformational switches in the beta2-adrenoceptorQ46120520
Structure and conformational changes in the C-terminal domain of the beta2-adrenoceptor: insights from fluorescence resonance energy transfer studiesQ46260678
Probing the beta2 adrenoceptor binding site with catechol reveals differences in binding and activation by agonists and partial agonistsQ46427567
The conserved seven-transmembrane sequence NP(X)2,3Y of the G-protein-coupled receptor superfamily regulates multiple properties of the beta 2-adrenergic receptorQ71570263
The role of the seventh transmembrane region in high affinity binding of a beta 2-selective agonist TA-2005Q74095224
P433issue5854
P407language of work or nameEnglishQ1860
P921main subjectG protein-coupled receptorQ38173
P304page(s)1266-73
P577publication date2007-11-23
P1433published inScienceQ192864
P1476titleGPCR engineering yields high-resolution structural insights into beta2-adrenergic receptor function
P478volume318

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Q34359302Highly conserved tyrosine stabilizes the active state of rhodopsin
Q38812016Hitchhiking on the heptahelical highway: structure and function of 7TM receptor complexes.
Q42212856Hologram quantitative structure activity relationship, docking, and molecular dynamics studies of inhibitors for CXCR4.
Q35181896Homology Model Versus X-ray Structure in Receptor-based Drug Design: A Retrospective Analysis with the Dopamine D3 Receptor
Q44530514Homology model and docking studies on porcine β₂ adrenoceptor: description of two binding sites.
Q51784685Homology modeling and flex-ligand docking studies on the guinea pig beta(2) adrenoceptor: structural and experimental similarities/ differences with the human beta(2).
Q42806068Homology modeling of a Class A GPCR in the inactive conformation: A quantitative analysis of the correlation between model/template sequence identity and model accuracy
Q35967081Homology modeling of class a G protein-coupled receptors
Q43276048Homology modelling of the human adenosine A2B receptor based on X-ray structures of bovine rhodopsin, the beta2-adrenergic receptor and the human adenosine A2A receptor
Q36421791How Can Mutations Thermostabilize G-Protein-Coupled Receptors?
Q47194737Human Adenosine A2A Receptor: Molecular Mechanism of Ligand Binding and Activation.
Q37305302Human Serotonin 5-HT2C G Protein-Coupled Receptor Homology Model from the β2 Adrenoceptor Structure: Ligand Docking and Mutagenesis Studies
Q61798028Human substance P receptor binding mode of the antagonist drug aprepitant by NMR and crystallography
Q33996731Hydrophobic residues in helix 8 of cannabinoid receptor 1 are critical for structural and functional properties
Q37979710Ice breaking in GPCR structural biology
Q35554301Identification of destabilizing and stabilizing mutations of Ste2p, a G protein-coupled receptor in Saccharomyces cerevisiae
Q37438039Identification of specific transmembrane residues and ligand-induced interface changes involved in homo-dimer formation of a yeast G protein-coupled receptor
Q33887246Identification of the GPR55 agonist binding site using a novel set of high-potency GPR55 selective ligands
Q35387937Identification of the differentially expressed genes associated with familial combined hyperlipidemia using bioinformatics analysis
Q24645752Identification of two distinct inactive conformations of the beta2-adrenergic receptor reconciles structural and biochemical observations
Q33400428Identifying conformational changes of the beta(2) adrenoceptor that enable accurate prediction of ligand/receptor interactions and screening for GPCR modulators
Q38023797Impact of helix irregularities on sequence alignment and homology modeling of G protein-coupled receptors
Q49507908Improved in Vitro Folding of the Y2 G Protein-Coupled Receptor into Bicelles.
Q27316812In meso in situ serial X-ray crystallography of soluble and membrane proteins at cryogenic temperatures
Q35057759In silico analysis of the binding of agonists and blockers to the β2-adrenergic receptor.
Q42979856In silico analysis of the histaprodifen induced activation pathway of the guinea-pig histamine H(1)-receptor
Q42730804In silico identification of new ligands for GPR17: a promising therapeutic target for neurodegenerative diseases
Q35693310In silico screening for agonists and blockers of the β(2) adrenergic receptor: implications of inactive and activated state structures
Q47213731Increasing the Stability of Recombinant Human Green Cone Pigment.
Q33767121Increasingly accurate dynamic molecular models of G-protein coupled receptor oligomers: Panacea or Pandora's box for novel drug discovery?
Q93143025Influence of the Structural Accuracy of Homology Models on Their Applicability to Docking-Based Virtual Screening: The β2 Adrenergic Receptor as a Case Study
Q56648606Insights into signaling from the β2-adrenergic receptor structure
Q44346651Insights into subtype selectivity of opioid agonists by ligand-based and structure-based methods
Q87345890Insights into the influence of 5-HT2c aminoacidic variants with the inhibitory action of serotonin inverse agonists and antagonists
Q53189799Insilico study of the A(2A)R-D (2)R kinetics and interfacial contact surface for heteromerization.
Q37520862Interaction and conformational dynamics of membrane-spanning protein helices
Q48812098Interactions of recombinant human histamine H₁R, H₂R, H₃R, and H₄R receptors with 34 antidepressants and antipsychotics.
Q47953339Interleukin-1β causes anxiety by interacting with the endocannabinoid system.
Q37782458Internally bridging water molecule in transmembrane α-helical kink
Q24623433International Union of Basic and Clinical Pharmacology. LXXV. Nomenclature, classification, and pharmacology of G protein-coupled melatonin receptors
Q90484890Interplay between the electrostatic membrane potential and conformational changes in membrane proteins
Q35977592Intracellular Loop 2 Peptides of the Human 5HT1a Receptor are Differential Activators of Gi.
Q39264759Involvement of the first transmembrane segment of human α(2) -adrenoceptors in the subtype-selective binding of chlorpromazine, spiperone and spiroxatrine.
Q38706167Isolation and structure-function characterization of a signaling-active rhodopsin-G protein complex
Q47163479Isomeric Detergent Comparison for Membrane Protein Stability: Importance of Inter-Alkyl-Chain Distance and Alkyl Chain Length.
Q41961309LCP-FRAP Assay for Pre-Screening Membrane Proteins for in Meso Crystallization
Q33795500LCP-Tm: an assay to measure and understand stability of membrane proteins in a membrane environment
Q26866010Large-scale production and protein engineering of G protein-coupled receptors for structural studies
Q24623930Lessons from the lysozyme of phage T4
Q41829504Ligand Binding Ensembles Determine Graded Agonist Efficacies at a G Protein-coupled Receptor
Q34412157Ligand Binding Sensitivity of the Extracellular Loop Two of the Cannabinoid Receptor 1.
Q37464148Ligand and structure-based methodologies for the prediction of the activity of G protein-coupled receptor ligands
Q33636089Ligand and structure-based models for the prediction of ligand-receptor affinities and virtual screenings: Development and application to the beta(2)-adrenergic receptor
Q42933080Ligand entry and exit pathways in the beta2-adrenergic receptor
Q42380834Ligand modulation of sidechain dynamics in a wild-type human GPCR.
Q33650270Ligand-based peptide design and combinatorial peptide libraries to target G protein-coupled receptors
Q41823093Ligand-regulated oligomerization of beta(2)-adrenoceptors in a model lipid bilayer
Q35863890Ligand-specific interactions modulate kinetic, energetic, and mechanical properties of the human β2 adrenergic receptor
Q27646733Ligand-specific regulation of the extracellular surface of a G-protein-coupled receptor
Q30153243Lipid bilayer-bound conformation of an integral membrane beta barrel protein by multidimensional MAS NMR.
Q35008243Lipid cubic phase as a membrane mimetic for integral membrane protein enzymes
Q42660693Lipid protein interactions couple protonation to conformation in a conserved cytosolic domain of G protein-coupled receptors
Q47223560Locking the Elbow: Improved Antibody Fab Fragments as Chaperones for Structure Determination.
Q36930850Lysophospholipid interactions with protein targets
Q34712509Maltose-neopentyl glycol (MNG) amphiphiles for solubilization, stabilization and crystallization of membrane proteins
Q34054370Mapping the druggable allosteric space of G-protein coupled receptors: a fragment-based molecular dynamics approach
Q35192004Mechanism for adhesion G protein-coupled receptor GPR56-mediated RhoA activation induced by collagen III stimulation.
Q45938036Mechanism of intracellular allosteric β2AR antagonist revealed by X-ray crystal structure.
Q36737228Mechanism of signal propagation upon retinal isomerization: insights from molecular dynamics simulations of rhodopsin restrained by normal modes
Q41645695Mechanisms involved in VPAC receptors activation and regulation: lessons from pharmacological and mutagenesis studies
Q27681476Mechanistic Strategies for Catalysis Adopted by Evolutionary Distinct Family 43 Arabinanases
Q42072255MemProtMD: Automated Insertion of Membrane Protein Structures into Explicit Lipid Membranes.
Q36654207Membrane cholesterol affects stimulus-activity coupling in type 1, but not type 2, CCK receptors: use of cell lines with elevated cholesterol.
Q30155276Membrane protein structure determination using crystallography and lipidic mesophases: recent advances and successes
Q33880152Mesitylene-Cored Glucoside Amphiphiles (MGAs) for Membrane Protein Studies: Importance of Alkyl Chain Density in Detergent Efficacy.
Q40274047Metal ions-binding T4 lysozyme as an intramolecular protein purification tag compatible with X-ray crystallography
Q26991511Metaphors, naming and new signaling paradigms by G-protein-coupled receptors
Q38318691Methodological advances: the unsung heroes of the GPCR structural revolution.
Q30412884Methods of protein structure comparison
Q37691765Microbial and animal rhodopsins: structures, functions, and molecular mechanisms.
Q34498063Modeling G Protein-Coupled Receptors: a Concrete Possibility
Q34167891Modeling of ligand binding to G protein coupled receptors: cannabinoid CB1, CB2 and adrenergic β 2 AR.
Q89810534Modeling the allosteric modulation on a G-Protein Coupled Receptor: the case of M2 muscarinic Acetylcholine Receptor in complex with LY211960
Q33937574Modern homology modeling of G-protein coupled receptors: which structural template to use?
Q27650678Modest stabilization by most hydrogen-bonded side-chain interactions in membrane proteins
Q35533294Modified T4 Lysozyme Fusion Proteins Facilitate G Protein-Coupled Receptor Crystallogenesis
Q37060802Molecular Determinants for Ligand Binding at Serotonin 5-HT2A and 5-HT2C GPCRs: Experimental Affinity Results Analyzed by Molecular Modeling and Ligand Docking Studies
Q51603697Molecular Modelling of G Protein-Coupled Receptors Through the Web.
Q36002904Molecular basis for binding and subtype selectivity of 1,4-benzodiazepine antagonist ligands of the cholecystokinin receptor
Q33858991Molecular determinants of ligand binding at the human histamine H1 receptor: Site-directed mutagenesis results analyzed with ligand docking and molecular dynamics studies at H1 homology and crystal structure models
Q52309570Molecular dynamics simulation of d-Benzedrine transmitting through molecular channels within D3R.
Q42754544Molecular dynamics simulations on the Tre1 G protein-coupled receptor: exploring the role of the arginine of the NRY motif in Tre1 structure
Q28542663Molecular insights into the dynamics of pharmacogenetically important N-terminal variants of the human β2-adrenergic receptor
Q36773326Molecular mechanism of β-arrestin-biased agonism at seven-transmembrane receptors
Q37234988Molecular mechanisms of mechanosensing and their roles in fungal contact sensing
Q42582195Molecular modeling of the M3 acetylcholine muscarinic receptor and its binding site
Q46409320Molecular modeling studies give hint for the existence of a symmetric hβ₂R-Gαβγ-homodimer
Q91595350Molecular pharmacology of metabotropic receptors targeted by neuropsychiatric drugs
Q37111743Molecular properties of muscarinic acetylcholine receptors
Q34327700Molecular signatures of G-protein-coupled receptors
Q30406132Molecular simulations and solid-state NMR investigate dynamical structure in rhodopsin activation
Q43195607Monitoring protein conformational changes and dynamics using stable-isotope labeling and mass spectrometry
Q46605612Multi-receptor binding profile of clozapine and olanzapine: a structural study based on the new beta2 adrenergic receptor template
Q36115098Multiple ligand-specific conformations of the β2-adrenergic receptor
Q40024079Multiple roles for the C-terminal tail of the chemokine scavenger D6.
Q38218059Muscarinic acetylcholine receptors: novel opportunities for drug development
Q39906654N(G)-acylated aminothiazolylpropylguanidines as potent and selective histamine H(2) receptor agonists
Q27674422N-Terminal T4 Lysozyme Fusion Facilitates Crystallization of a G Protein Coupled Receptor
Q47194753Na+-mimicking ligands stabilize the inactive state of leukotriene B4 receptor BLT1.
Q30382600Nanobodies as Probes for Protein Dynamics in Vitro and in Cells.
Q33880125Nanobodies to Study G Protein-Coupled Receptor Structure and Function
Q27690729Nanobody stabilization of G protein-coupled receptor conformational states.
Q38060667Neuropeptides and neuropeptide receptors: drug targets, and peptide and non-peptide ligands: a tribute to Prof. Dieter Seebach
Q37323435Neurotransmitter receptor heteromers in neurodegenerative diseases and neural plasticity.
Q96161939New Malonate-Derived Tetraglucoside Detergents for Membrane Protein Stability
Q38933295New Trends in Inspecting GPCR-ligand Recognition Process: the Contribution of the Molecular Modeling Section (MMS) at the University of Padova
Q39332114New approaches towards the understanding of integral membrane proteins: A structural perspective on G protein-coupled receptors
Q26991761New insights for drug design from the X-ray crystallographic structures of G-protein-coupled receptors
Q38815332New paradigms in chemokine receptor signal transduction: Moving beyond the two-site model.
Q47797929New penta-saccharide-bearing tripod amphiphiles for membrane protein structure studies
Q48287996Nobel Prize for Chemistry 2012: GPCRs seen through a crystal ball.
Q30374996Novel Xylene-Linked Maltoside Amphiphiles (XMAs) for Membrane Protein Stabilisation
Q38259766Novel approaches for targeting the adenosine A2A receptor
Q37495839Novel carvedilol analogues that suppress store-overload-induced Ca2+ release
Q51522567Novel computational methodologies for structural modeling of spacious ligand binding sites of G-protein-coupled receptors: development and application to human leukotriene B4 receptor.
Q37626522Novel tripod amphiphiles for membrane protein analysis
Q56592630Odorant Receptor 7D4 Activation Dynamics
Q36744266On the applicability of GPCR homology models to computer-aided drug discovery: a comparison between in silico and crystal structures of the beta2-adrenergic receptor.
Q56877460One hundred years of X-ray diffraction, 50 years of structural biology
Q44333492Opioid receptors revealed
Q37249017Opioid receptors: from binding sites to visible molecules in vivo
Q26866088Opportunities and challenges for time-resolved studies of protein structural dynamics at X-ray free-electron lasers
Q34670650Opsin is a phospholipid flippase
Q30401692Overcoming barriers to membrane protein structure determination
Q34803434Overcoming the challenges of membrane protein crystallography.
Q39470722Overexpressing human membrane proteins in stably transfected and clonal human embryonic kidney 293S cells
Q24317396PROKR2 missense mutations associated with Kallmann syndrome impair receptor signalling activity
Q30503489Pathway and mechanism of drug binding to G-protein-coupled receptors.
Q96302430Pendant-bearing glucose-neopentyl glycol (P-GNG) amphiphiles for membrane protein manipulation: Importance of detergent pendant chain for protein stabilization
Q41774653Perspective: Markov models for long-timescale biomolecular dynamics
Q36316813Pharmacological Analysis and Structure Determination of 7-Methylcyanopindolol-Bound β1-Adrenergic Receptor.
Q38944804Pharmacological Characterization of Human Histamine Receptors and Histamine Receptor Mutants in the Sf9 Cell Expression System.
Q39704718Pharmacological characterization of 30 human melanocortin-4 receptor polymorphisms with the endogenous proopiomelanocortin-derived agonists, synthetic agonists, and the endogenous agouti-related protein antagonist
Q39640436Phe369(7.38) at human 5-HT(7) receptors confers interspecies selectivity to antagonists and partial agonists.
Q42425022PheVI:09 (Phe6.44) as a sliding microswitch in seven-transmembrane (7TM) G protein-coupled receptor activation
Q37366101Phospholipids are needed for the proper formation, stability, and function of the photoactivated rhodopsin-transducin complex
Q48240503Phosphorylation-induced conformation of β2-adrenoceptor related to arrestin recruitment revealed by NMR.
Q38016154Physiology and emerging biochemistry of the glucagon-like peptide-1 receptor
Q41243070Platform for the rapid construction and evaluation of GPCRs for crystallography in Saccharomyces cerevisiae
Q38028542Platforms for the identification of GPCR targets, and of orthosteric and allosteric modulators.
Q42741366Polymer-based cell-free expression of ligand-binding family B G-protein coupled receptors without detergents
Q26849743Post-expression strategies for structural investigations of membrane proteins
Q38946091Predicting phenotype from genotype: Improving accuracy through more robust experimental and computational modeling
Q92594361Prediction of Conformation Specific Thermostabilizing Mutations for Class A G Protein-Coupled Receptors
Q36077712Preparation of an activated rhodopsin/transducin complex using a constitutively active mutant of rhodopsin
Q37020421Probes for narcotic receptor mediated phenomena. 37. Synthesis and opioid binding affinity of the final pair of oxide-bridged phenylmorphans, the ortho- and para-b-isomers and their N-phenethyl analogues, and the synthesis of the N-phenethyl analogu
Q46718105Probing distal regions of the A2B adenosine receptor by quantitative structure-activity relationship modeling of known and novel agonists.
Q37274469Probing the role of the cation-pi interaction in the binding sites of GPCRs using unnatural amino acids.
Q38671723Production of Chemokine/Chemokine Receptor Complexes for Structural Biophysical Studies.
Q50512769Production of the stable human histamine H₁ receptor in Pichia pastoris for structural determination.
Q36747747Profile of Brian K. Kobilka and Robert J. Lefkowitz, 2012 Nobel laureates in chemistry
Q34358923Profiling the interaction mechanism of quinoline/quinazoline derivatives as MCHR1 antagonists: an in silico method
Q35095066Progress in elucidating the structural and dynamic character of G Protein-Coupled Receptor oligomers for use in drug discovery
Q56979272Progress in the structural prediction of G protein-coupled receptors: D3 receptor in complex with eticlopride
Q37362453Promiscuous drugs as therapeutics for chemokine receptors
Q89843914Protein Footprinting: Auxiliary Engine to Power the Structural Biology Revolution
Q27687870Protein design by fusion: implications for protein structure prediction and evolution
Q42071118Protein microcrystallography using synchrotron radiation
Q47857119Protein structures: Structures of desire
Q37446783Purification and functional reconstitution of monomeric mu-opioid receptors: allosteric modulation of agonist binding by Gi2.
Q44607630Putative cholesterol-binding sites in human immunodeficiency virus (HIV) coreceptors CXCR4 and CCR5.
Q90156829RCSB Protein Data Bank: Enabling biomedical research and drug discovery
Q53188593Radioligand binding analysis as a tool for quality control of GPCR production for structural characterization: adenosine A(2a)R as a template for study.
Q34503044Rapid Computational Prediction of Thermostabilizing Mutations for G Protein-Coupled Receptors.
Q94445335Rapid identification of highly potent human anti-GPCR antagonist monoclonal antibodies
Q33747204Rastering strategy for screening and centring of microcrystal samples of human membrane proteins with a sub-10 microm size X-ray synchrotron beam.
Q37334040Ratiocinative screen of eukaryotic integral membrane protein expression and solubilization for structure determination
Q61904303Rationally Engineered Tandem Facial Amphiphiles for Improved Membrane Protein Stabilization Efficacy
Q35048773Reassessment of the unique mode of binding between angiotensin II type 1 receptor and their blockers
Q37416441Recent advances in structure-based virtual screening of G-protein coupled receptors
Q34278937Recent progress in the structure determination of GPCRs, a membrane protein family with high potential as pharmaceutical targets
Q36785514Regulation of α2B-Adrenerigc Receptor Export Trafficking by Specific Motifs
Q37589121Retinal dynamics during light activation of rhodopsin revealed by solid-state NMR spectroscopy
Q26747130Revealing Atomic-Level Mechanisms of Protein Allostery with Molecular Dynamics Simulations
Q42269169Reversed binding of a small molecule ligand in homologous chemokine receptors - differential role of extracellular loop 2.
Q28266829Reviews in molecular biology and biotechnology: transmembrane signaling by G protein-coupled receptors
Q33569254Rhodopsin and the others: a historical perspective on structural studies of G protein-coupled receptors
Q38862301Role of Conserved Disulfide Bridges and Aromatic Residues in Extracellular Loop 2 of Chemokine Receptor CCR8 for Chemokine and Small Molecule Binding
Q39498635Role of the second and third extracellular loops of the histamine H(4) receptor in receptor activation
Q90700670Rules of Engagement: GPCRs and G Proteins
Q35091511S-nitrosylation-regulated GPCR signaling
Q58568349Science Librarians Analysis of the 2012 Nobel Prize in Chemistry: The Work of Robert Lefkowitz and Brian Kobilka
Q37137758Selecting optimum eukaryotic integral membrane proteins for structure determination by rapid expression and solubilization screening
Q34962263Selective 5-hydroxytryptamine 2C receptor agonists derived from the lead compound tranylcypromine: identification of drugs with antidepressant-like action
Q36186107Selectivity in the Use of Gi/o Proteins Is Determined by the DRF Motif in CXCR6 and Is Cell-Type Specific
Q93056270Self-Assembly Behavior and Application of Terphenyl-Cored Trimaltosides for Membrane-Protein Studies: Impact of Detergent Hydrophobic Group Geometry on Protein Stability
Q92999325Self-Assembly Behaviors of a Penta-Phenylene Maltoside and Its Application for Membrane Protein Study
Q28649590Sequence, structure and ligand binding evolution of rhodopsin-like G protein-coupled receptors: a crystal structure-based phylogenetic analysis
Q33890786Seven transmembrane receptors as shapeshifting proteins: the impact of allosteric modulation and functional selectivity on new drug discovery
Q38775792Similarity- and Substructure-Based Development of β2-Adrenergic Receptor Ligands Based on Unusual Scaffolds
Q44559624Simulations of a G protein-coupled receptor homology model predict dynamic features and a ligand binding site
Q34782818Single-molecule force spectroscopy of G-protein-coupled receptors.
Q40054046Site-specific incorporation of keto amino acids into functional G protein-coupled receptors using unnatural amino acid mutagenesis.
Q28480422Small molecules with similar structures exhibit agonist, neutral antagonist or inverse agonist activity toward angiotensin II type 1 receptor
Q33633178Solution conformation of non-mammalian tachykinin physalaemin in lipid micelles by nuclear magnetic resonance
Q38448843Sphingosine-1-phosphate metabolism: A structural perspective
Q47849019Spirohexene-Tetrazine Ligation Enables Bioorthogonal Labeling of Class B G Protein-Coupled Receptors in Live Cells
Q27680775Split green fluorescent protein as a modular binding partner for protein crystallization
Q35486811Stabilization of G protein-coupled receptors by point mutations
Q40020328Stabilization of the human beta2-adrenergic receptor TM4-TM3-TM5 helix interface by mutagenesis of Glu122(3.41), a critical residue in GPCR structure
Q44608235Stealth carriers for low-resolution structure determination of membrane proteins in solution
Q52585354Steroid-based amphiphiles for membrane protein study: Importance of alkyl spacer for protein stability.
Q27676750Steroid-based facial amphiphiles for stabilization and crystallization of membrane proteins
Q37776038Strategies for the cloning and expression of membrane proteins
Q27680463Structural Analysis and Optimization of the Covalent Association between SpyCatcher and a Peptide Tag
Q51337340Structural Analysis of the Histamine H1 Receptor.
Q51539813Structural Basis and Mechanism of Chiral Benzedrine Molecules Interacting With Third Dopamine Receptor.
Q92817538Structural Basis for Allosteric Ligand Recognition in the Human CC Chemokine Receptor 7
Q42694413Structural Basis for G Protein-Coupled Receptor Activation
Q27652199Structural Basis of CXCR4 Sulfotyrosine Recognition by the Chemokine SDF-1/CXCL12
Q39084919Structural Insights into Sigma1 Function
Q35638953Structural Insights into the Dynamic Process of β2-Adrenergic Receptor Signaling
Q38831305Structural Reconstruction of Protein-Protein Complexes Involved in Intracellular Signaling
Q26783016Structural Studies of G Protein-Coupled Receptors
Q27678733Structural Studies of Wnts and Identification of an LRP6 Binding Site
Q90659183Structural Variability in the RLR-MAVS Pathway and Sensitive Detection of Viral RNAs
Q93006962Structural Variability of EspG Chaperones from Mycobacterial ESX-1, ESX-3, and ESX-5 Type VII Secretion Systems
Q37232161Structural analysis of the human cannabinoid receptor one carboxyl-terminus identifies two amphipathic helices.
Q36188948Structural and Functional Effect of an Oscillating Electric Field on the Dopamine-D3 Receptor: A Molecular Dynamics Simulation Study
Q30152958Structural and biophysical characterization of an epitope-specific engineered Fab fragment and complexation with membrane proteins: implications for co-crystallization
Q33913886Structural and dynamic effects of cholesterol at preferred sites of interaction with rhodopsin identified from microsecond length molecular dynamics simulations
Q100755370Structural and functional characterization of G protein-coupled receptors with deep mutational scanning
Q28237034Structural approaches to understanding retinal proteins needed for vision
Q35790289Structural aspects of M₃ muscarinic acetylcholine receptor dimer formation and activation
Q34073218Structural basis for μ-opioid receptor binding and activation
Q97650820Structural basis of GPBAR activation and bile acid recognition
Q38734550Structural basis of activation of bitter taste receptor T2R1 and comparison with Class A G-protein-coupled receptors (GPCRs)
Q90665799Structural basis of chemokine and receptor interactions: Key regulators of leukocyte recruitment in inflammatory responses
Q52316530Structural basis of ligand binding modes at the neuropeptide Y Y1 receptor.
Q37454403Structural basis of the interaction between chemokine stromal cell-derived factor-1/CXCL12 and its G-protein-coupled receptor CXCR4.
Q37441082Structural basis of the selectivity of the beta(2)-adrenergic receptor for fluorinated catecholamines.
Q51761770Structural biology of G protein-coupled receptors: new opportunities from XFELs and cryoEM.
Q38204271Structural biology of the S1P1 receptor
Q43145800Structural biology: A moving story of receptors
Q43235004Structural biology: How opioid drugs bind to receptors
Q87422328Structural biology: Snapshot of an activated peptide receptor
Q57185649Structural biology: The gatekeepers revealed
Q42152281Structural constraints for the binding of short peptides to claudin-4 revealed by surface plasmon resonance
Q37455434Structural determinants underlying constitutive dimerization of unoccupied human follitropin receptors
Q57151843Structural diversity and flexibility of diabodies
Q92784480Structural equilibrium underlying ligand-dependent activation of β2-adrenoreceptor
Q35093808Structural features of β2 adrenergic receptor: crystal structures and beyond
Q37310590Structural insights into G-protein-coupled receptor activation
Q37854213Structural insights into adrenergic receptor function and pharmacology
Q57452393Structural insights into binding specificity, efficacy and bias of a βAR partial agonist
Q41866579Structural insights into conformational stability of wild-type and mutant beta1-adrenergic receptor.
Q28088311Structural insights into ligand recognition and selectivity for classes A, B, and C GPCRs
Q34488374Structural insights into µ-opioid receptor activation
Q24595276Structural 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
Q30380117Structural waters define a functional channel mediating activation of the GPCR, rhodopsin.
Q57015852Structure and Modeling of GPCRs: Implications for Drug Discovery
Q37479887Structure and dynamics of a constitutively active neurotensin receptor
Q27677433Structure and dynamics of the M3 muscarinic acetylcholine receptor
Q24620291Structure and function of an irreversible agonist-β(2) adrenoceptor complex
Q27704228Structure and ligand-binding mechanism of the human OX1 and OX2 orexin receptors
Q26824924Structure determination of membrane proteins by nuclear magnetic resonance spectroscopy
Q42285749Structure determination of membrane proteins in their native phospholipid bilayer environment by rotationally aligned solid-state NMR spectroscopy
Q96302945Structure of a D2 dopamine receptor-G-protein complex in a lipid membrane
Q27651011Structure of a beta1-adrenergic G-protein-coupled receptor
Q60300327Structure of a human intramembrane ceramidase explains enzymatic dysfunction found in leukodystrophy
Q24597139Structure of a nanobody-stabilized active state of the β(2) adrenoceptor
Q24296388Structure of an agonist-bound human A2A adenosine receptor
Q90975764Structure of an allosteric modulator bound to the CB1 cannabinoid receptor
Q27672832Structure of the Adenosine A2A Receptor in Complex with ZM241385 and the Xanthines XAC and Caffeine
Q52315658Structure of the D2 dopamine receptor bound to the atypical antipsychotic drug risperidone.
Q27666030Structure of the Human Dopamine D3 Receptor in Complex with a D2/D3 Selective Antagonist
Q59060936Structure of the adenosine-bound human adenosine A1 receptor–Gi complex
Q27674395Structure of the agonist-bound neurotensin receptor
Q27674645Structure of the chemokine receptor CXCR1 in phospholipid bilayers
Q24628686Structure of the human M2 muscarinic acetylcholine receptor bound to an antagonist
Q100750121Structure of the human gonadotropin-releasing hormone receptor GnRH1R reveals an unusual ligand binding mode
Q24595968Structure of the human histamine H1 receptor complex with doxepin
Q24308048Structure of the human κ-opioid receptor in complex with JDTic
Q36497002Structure, function and physiological consequences of virally encoded chemokine seven transmembrane receptors
Q33560239Structure-based discovery of A2A adenosine receptor ligands
Q33426241Structure-based discovery of beta2-adrenergic receptor ligands
Q30435017Structure-based discovery of novel chemotypes for adenosine A(2A) receptor antagonists
Q34983219Structure-based ligand discovery targeting orthosteric and allosteric pockets of dopamine receptors
Q30576993Structure-function of the G protein-coupled receptor superfamily
Q39121630Study of two G-protein coupled receptor variants of human trace amine-associated receptor 5.
Q33615741Subtype selectivity of dopamine receptor ligands: insights from structure and ligand-based methods
Q93054793Surface Plasmon Resonance as a Tool for Ligand Binding Investigation of Engineered GPR17 Receptor, a G Protein Coupled Receptor Involved in Myelination
Q30887281Surface plasmon resonance for high-throughput ligand screening of membrane-bound proteins
Q36431626Synthesis and structure-affinity relationships of selective high-affinity 5-HT(4) receptor antagonists: application to the design of new potential single photon emission computed tomography tracers
Q27665931Synthetic symmetrization in the crystallization and structure determination of CelA fromThermotoga maritima
Q88994083T4 lysozyme-facilitated crystallization of the human molybdenum cofactor-dependent enzyme mARC
Q42244148T4-lysozyme fusion for the production of human formyl peptide receptors for structural determination
Q33738010Tandem facial amphiphiles for membrane protein stabilization
Q33822322Tandem malonate-based glucosides (TMGs) for membrane protein structural studies
Q42331678Tandem neopentyl glycol maltosides (TNMs) for membrane protein stabilisation
Q90529594Targeting of G-protein coupled receptors in sepsis
Q30252224The "Sticky Patch" Model of Crystallization and Modification of Proteins for Enhanced Crystallizability
Q27682443The 2.1 Å Resolution Structure of Cyanopindolol-Bound β1-Adrenoceptor Identifies an Intramembrane Na+ Ion that Stabilises the Ligand-Free Receptor
Q24654563The 2.6 angstrom crystal structure of a human A2A adenosine receptor bound to an antagonist
Q37957791The A3 adenosine receptor as multifaceted therapeutic target: pharmacology, medicinal chemistry, and in silico approaches
Q27680068The Crystal Structure of the Orphan Nuclear Receptor NR2E3/PNR Ligand Binding Domain Reveals a Dimeric Auto-Repressed Conformation
Q35685881The Effects of the Recombinant CCR5 T4 Lysozyme Fusion Protein on HIV-1 Infection
Q38682286The Energetics of Chromophore Binding in the Visual Photoreceptor Rhodopsin.
Q84603072The Family of G Protein-Coupled Receptors: An Example of Membrane Proteins
Q37045212The GPCR Network: a large-scale collaboration to determine human GPCR structure and function
Q27677349The Glove-like Structure of the Conserved Membrane Protein TatC Provides Insight into Signal Sequence Recognition in Twin-Arginine Translocation
Q47780061The Human Orexin/Hypocretin Receptor Crystal Structures
Q64987318The Molecular Basis of G Protein-Coupled Receptor Activation.
Q30415339The Protein Structure Initiative: achievements and visions for the future
Q42042812The Recognition of Identical Ligands by Unrelated Proteins
Q27678608The Structure of the Mercury Transporter MerF in Phospholipid Bilayers: A Large Conformational Rearrangement Results from N-Terminal Truncation
Q42325394The arginine of the DRY motif in transmembrane segment III functions as a balancing micro-switch in the activation of the β2-adrenergic receptor
Q46137779The azulene framework as a novel arene bioisostere: design of potent dopamine D4 receptor ligands inducing penile erection
Q34363831The chemical basis of pharmacology
Q35216471The design, synthesis and pharmacological characterization of novel β₂-adrenoceptor antagonists.
Q97568780The discovery of a new antibody for BRIL-fused GPCR structure determination
Q36651876The dynamic process of β(2)-adrenergic receptor activation
Q37200963The effect of ligand efficacy on the formation and stability of a GPCR-G protein complex
Q36000382The evolving impact of g protein-coupled receptor kinases in cardiac health and disease
Q42948753The fifth transmembrane domain of angiotensin II Type 1 receptor participates in the formation of the ligand-binding pocket and undergoes a counterclockwise rotation upon receptor activation
Q27701469The high-resolution crystal structure of phosphatidylinositol 4-kinase IIβ and the crystal structure of phosphatidylinositol 4-kinase IIα containing a nucleoside analogue provide a structural basis for isoform-specific inhibitor design
Q24628661The impact of GPCR structures on pharmacology and structure-based drug design
Q30277230The impact of structural genomics: the first quindecennial
Q57901310The importance of solvation in the design of ligands targeting membrane proteins
Q102075582The importance of the membrane for biophysical measurements
Q41823226The importance of valine 114 in ligand binding in beta(2)-adrenergic receptor
Q48251393The macro domain as fusion tag for carrier-driven crystallization
Q37344009The magnitude of the light-induced conformational change in different rhodopsins correlates with their ability to activate G proteins
Q36003378The melanocortin-4 receptor: physiology, pharmacology, and pathophysiology.
Q41906066The micelle-associated 3D structures of Boc-Y(SO3)-Nle-G-W-Nle-D-2-phenylethylester (JMV-180) and CCK-8(s) share conformational elements of a calculated CCK1 receptor-bound model.
Q37179691The molecular basis of species-specific ligand activation of trace amine-associated receptor 1 (TAAR(1)).
Q38204270The organization of the sphingosine 1-phosphate signaling system
Q37381287The role of a sodium ion binding site in the allosteric modulation of the A(2A) adenosine G protein-coupled receptor
Q30377191The role of experimental and computational structural approaches in 7TM drug discovery.
Q38188734The role of protein dynamics in GPCR function: insights from the β2AR and rhodopsin
Q30416991The role of protein structural analysis in the next generation sequencing era.
Q48982673The roles of computational chemistry in the ligand design of G protein-coupled receptors: how far have we come and what should we expect?
Q48287610The seven pillars of molecular pharmacology: GPCR research honored with Nobel Prize for chemistry.
Q35264433The significance of G protein-coupled receptor crystallography for drug discovery
Q33651185The structural basis of G-protein-coupled receptor signaling (Nobel Lecture)
Q29616792The structure and function of G-protein-coupled receptors
Q38062457The very large G protein coupled receptor (Vlgr1) in hair cells
Q37078649The α-Arrestin ARRDC3 Regulates the Endosomal Residence Time and Intracellular Signaling of the β2-Adrenergic Receptor
Q45332213Thermodynamic studies of ligand binding to the human homopentameric glycine receptor using isothermal titration calorimetry
Q35546383Thermodynamics of peptide and non-peptide interactions with the human 5HT1a receptor
Q36917238Thermostabilisation of the serotonin transporter in a cocaine-bound conformation
Q37032791Thermostabilization of the β1-adrenergic receptor correlates with increased entropy of the inactive state
Q41493054Thioredoxin as a fusion tag for carrier-driven crystallization
Q37937552Third-generation long-acting β₂-adrenoceptor agonists: medicinal chemistry strategies employed in the identification of once-daily inhaled β₂-adrenoceptor agonists
Q41542396Three "hotspots" important for adenosine A(2B) receptor activation: a mutational analysis of transmembrane domains 4 and 5 and the second extracellular loop
Q33775572Thyrotropin (TSH) receptor residue E251 in the extracellular leucine-rich repeat domain is critical for linking TSH binding to receptor activation
Q26991608To fuse or not to fuse: what is your purpose?
Q28468674Todralazine protects zebrafish from lethal effects of ionizing radiation: role of hematopoietic cell expansion
Q37269754Toward deciphering the code to aminergic G protein-coupled receptor drug design
Q34111760Toward structure determination using membrane-protein nanocrystals and microcrystals
Q60228969Toward the design of cannabinoid CB1 receptor inverse agonists and neutral antagonists
Q42240327Toward the three-dimensional structure and lysophosphatidic acid binding characteristics of the LPA(4)/p2y(9)/GPR23 receptor: a homology modeling study
Q34611560Towards improved quality of GPCR models by usage of multiple templates and profile-profile comparison
Q92188624Trehalose-cored amphiphiles for membrane protein stabilization: importance of the detergent micelle size in GPCR stability
Q43112410Two amino acid substitutions within the first external loop of CCR5 induce human immunodeficiency virus-blocking antibodies in mice and chickens
Q37081904Two arginine-glutamate ionic locks near the extracellular surface of FFAR1 gate receptor activation.
Q34663887Understanding cadherin EGF LAG seven-pass G-type receptors.
Q27687653Understanding functional residues of the cannabinoid CB1.
Q42064855Unique interaction pattern for a functionally biased ghrelin receptor agonist
Q26852233Unlocking the secrets of the gatekeeper: methods for stabilizing and crystallizing GPCRs
Q30383769Unraveling the structure and function of G protein-coupled receptors through NMR spectroscopy.
Q104473866Use of cyclic peptides to induce crystallization: case study with prolyl hydroxylase domain 2
Q36829195Use of multidimensional fluorescence resonance energy transfer to establish the orientation of cholecystokinin docked at the type A cholecystokinin receptor
Q30384065Visualizing water molecules in transmembrane proteins using radiolytic labeling methods.
Q52346929Vitamin E-based glycoside amphiphiles for membrane protein structural studies.
Q38680670What Do Structures Tell Us About Chemokine Receptor Function and Antagonism?
Q34981578Why we need many more G protein-coupled receptor structures
Q30397964X-ray diffraction from membrane protein nanocrystals
Q38093833X-ray structural information of GPCRs in drug design: what are the limitations and where do we go?
Q82816211hβ2R-Gαs complex: prediction versus crystal structure--how valuable are predictions based on molecular modeling studies?
Q44988763mGluR5: exploration of orthosteric and allosteric ligand binding pockets and their applications to drug discovery
Q33989429ss-TEA: Entropy based identification of receptor specific ligand binding residues from a multiple sequence alignment of class A GPCRs
Q37102508β-arrestin-biased signaling through the β2-adrenergic receptor promotes cardiomyocyte contraction
Q41367007β1-adrenergic receptor O-glycosylation regulates N-terminal cleavage and signaling responses in cardiomyocytes
Q39191447β2-Adrenergic Receptor Conformational Response to Fusion Protein in the Third Intracellular Loop
Q41813394β2-Adrenergic receptor solutions for structural biology analyzed with microscale NMR diffusion measurements

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