Conformational flexibility and structural dynamics in GPCR-mediated G protein activation: a perspective

scientific article published on 16 April 2013

Conformational flexibility and structural dynamics in GPCR-mediated G protein activation: a perspective is …
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scholarly articleQ13442814

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P356DOI10.1016/J.JMB.2013.04.011
P932PMC publication ID3686903
P698PubMed publication ID23602809

P50authorJens MeilerQ29315318
Anita PreiningerQ43164356
P2093author name stringHeidi E Hamm
P2860cites workStructure of an agonist-bound human A2A adenosine receptorQ24296388
Agonist-bound adenosine A2A receptor structures reveal common features of GPCR activationQ24303747
The structural basis for agonist and partial agonist action on a β(1)-adrenergic receptorQ24594844
Structure of a nanobody-stabilized active state of the β(2) adrenoceptorQ24597139
Structure and function of an irreversible agonist-β(2) adrenoceptor complexQ24620291
Crystal structure of the β2 adrenergic receptor-Gs protein complexQ24635327
Identification of two distinct inactive conformations of the beta2-adrenergic receptor reconciles structural and biochemical observationsQ24645752
The 2.6 angstrom crystal structure of a human A2A adenosine receptor bound to an antagonistQ24654563
Crystal structure of rhodopsin: A G protein-coupled receptorQ27625972
Crystal structure of the human beta2 adrenergic G-protein-coupled receptorQ27648868
Crystal structure of the ligand-free G-protein-coupled receptor opsinQ27650885
Structure of a beta1-adrenergic G-protein-coupled receptorQ27651011
Crystal structure of opsin in its G-protein-interacting conformationQ27652301
Helix Dipole Movement and Conformational Variability Contribute to Allosteric GDP Release in Gα i Subunits † , ‡Q27653830
Structural evidence for a sequential release mechanism for activation of heterotrimeric G proteinsQ27657143
Conserved Binding Mode of Human β 2 Adrenergic Receptor Inverse Agonists and Antagonist Revealed by X-ray CrystallographyQ27663654
Crystal structure of metarhodopsin IIQ27666911
The structural basis of agonist-induced activation in constitutively active rhodopsinQ27667245
Structural Basis for Allosteric Regulation of GPCRs by Sodium IonsQ27670746
Structures of active conformations of Gi alpha 1 and the mechanism of GTP hydrolysisQ27730891
The 2.2 A crystal structure of transducin-alpha complexed with GTP gamma SQ27731495
Crystal structure of the catalytic domains of adenylyl cyclase in a complex with Gsalpha.GTPgammaSQ27748762
Inhibition of inositol phosphate second messenger formation by intracellular loop one of a human calcitonin receptor. Expression and mutational analysis of synthetic receptor genesQ28240879
The second intracellular loop of the m5 muscarinic receptor is the switch which enables G-protein couplingQ28281974
Mapping of single amino acid residues required for selective activation of Gq/11 by the m3 muscarinic acetylcholine receptorQ28294870
GDP release preferentially occurs on the phosphate side in heterotrimeric G-proteinsQ28481401
Molecular simulations and solid-state NMR investigate dynamical structure in rhodopsin activationQ30406132
Myristoylation exerts direct and allosteric effects on Gα conformation and dynamics in solutionQ30413000
Single amino acid substitutions and deletions that alter the G protein coupling properties of the V2 vasopressin receptor identified in yeast by receptor random mutagenesisQ30662392
Internal hydration increases during activation of the G-protein-coupled receptor rhodopsinQ31160779
A lipid pathway for ligand binding is necessary for a cannabinoid G protein-coupled receptorQ33885350
The nucleotide exchange factor Ric-8A is a chaperone for the conformationally dynamic nucleotide-free state of Gαi1.Q33996965
Molecular signatures of G-protein-coupled receptorsQ34327700
Structural determinants in the second intracellular loop of the human cannabinoid CB1 receptor mediate selective coupling to Gs and GiQ34442426
Mechanism of the receptor-catalyzed activation of heterotrimeric G proteinsQ34554804
Local peptide movement in the photoreaction intermediate of rhodopsinQ35021777
Interaction of a G protein with an activated receptor opens the interdomain interface in the alpha subunitQ35034989
Structural and dynamical changes in an alpha-subunit of a heterotrimeric G protein along the activation pathwayQ35133731
Structural flexibility of the G alpha s alpha-helical domain in the beta2-adrenoceptor Gs complexQ35229205
Activation mechanism of the β2-adrenergic receptorQ35558683
Ligand-specific interactions modulate kinetic, energetic, and mechanical properties of the human β2 adrenergic receptorQ35863890
Agonist dynamics and conformational selection during microsecond simulations of the A(2A) adenosine receptorQ35926130
Conformational dynamics of activation for the pentameric complex of dimeric G protein-coupled receptor and heterotrimeric G proteinQ35957944
Conformational changes in the G protein Gs induced by the β2 adrenergic receptorQ36252945
Cholesterol heterogeneity in bovine rod outer segment disk membranesQ36483416
Cholesterol increases kinetic, energetic, and mechanical stability of the human β2-adrenergic receptor.Q36483829
The dynamic process of β(2)-adrenergic receptor activationQ36651876
The highly conserved DRY motif of class A G protein-coupled receptors: beyond the ground state.Q36693902
Predictions for cholesterol interaction sites on the A2A adenosine receptorQ36838702
Conformational complexity of G-protein-coupled receptorsQ36880905
Linking receptor activation to changes in Sw I and II of Gα proteinsQ37053797
From valleys to ridges: exploring the dynamic energy landscape of single membrane proteins.Q37112719
Role of the extracellular loops of G protein-coupled receptors in ligand recognition: a molecular modeling study of the human P2Y1 receptor.Q37143313
Structural basis for ligand binding and specificity in adrenergic receptors: implications for GPCR-targeted drug discovery.Q37281064
Recent progress in the study of G protein-coupled receptors with molecular dynamics computer simulationsQ37858664
Mutation of tyrosine-141 inhibits insulin-promoted tyrosine phosphorylation and increased responsiveness of the human beta 2-adrenergic receptor.Q38289177
Ligand-dependent perturbation of the conformational ensemble for the GPCR β2 adrenergic receptor revealed by HDX.Q38462134
Evaluating cellular impedance assays for detection of GPCR pleiotropic signaling and functional selectivityQ39884754
Disease-causing mutation in GPR54 reveals the importance of the second intracellular loop for class A G-protein-coupled receptor functionQ39943167
Activation of the beta 2-adrenergic receptor involves disruption of an ionic lock between the cytoplasmic ends of transmembrane segments 3 and 6.Q40803165
G alpha minigenes expressing C-terminal peptides serve as specific inhibitors of thrombin-mediated endothelial activationQ40818013
Hydrophobic amino acid in the i2 loop plays a key role in receptor-G protein coupling.Q41519901
Dynamic structure of retinylidene ligand of rhodopsin probed by molecular simulationsQ41771911
Biased signaling pathways in β2-adrenergic receptor characterized by 19F-NMR.Q41775482
Receptor-mediated changes at the myristoylated amino terminus of Galpha(il) proteins.Q41838778
Interruption of the ionic lock in the bradykinin B2 receptor results in constitutive internalization and turns several antagonists into strong agonistsQ42514634
A concerted mechanism for opening the GDP binding pocket and release of the nucleotide in hetero-trimeric G-proteinsQ42604469
Concerted interconversion between ionic lock substates of the beta(2) adrenergic receptor revealed by microsecond timescale molecular dynamicsQ42844366
Impact of the DRY motif and the missing "ionic lock" on constitutive activity and G-protein coupling of the human histamine H4 receptorQ43182572
Rapid activation of transducin by mutations distant from the nucleotide-binding site: evidence for a mechanistic model of receptor-catalyzed nucleotide exchange by G proteinsQ43610785
Disruption of the alpha5 helix of transducin impairs rhodopsin-catalyzed nucleotide exchangeQ44008700
Molecular dynamics simulations of the adenosine A2a receptor: structural stability, sampling, and convergence.Q44228364
Reconstitution reveals additional roles for N- and C-terminal domains of g(alpha) in muscarinic receptor couplingQ44479702
Rhodopsin activation exposes a key hydrophobic binding site for the transducin alpha-subunit C terminusQ44834954
Conformational changes associated with receptor-stimulated guanine nucleotide exchange in a heterotrimeric G-protein alpha-subunit: NMR analysis of GTPgammaS-bound statesQ46890300
Potent peptide analogues of a G protein receptor-binding region obtained with a combinatorial libraryQ46989688
Molecular dynamics simulations of transducin: interdomain and front to back communication in activation and nucleotide exchange.Q47772278
Activation of Gi protein by peptide structures of the muscarinic M2 receptor second intracellular loopQ48139595
The metabotropic glutamate receptors: their second intracellular loop plays a critical role in the G-protein coupling specificity.Q49067385
Two amino acids within the alpha4 helix of Galphai1 mediate coupling with 5-hydroxytryptamine1B receptorsQ57129658
Critical Role for the Second Extracellular Loop in the Binding of Both Orthosteric and Allosteric G Protein-coupled Receptor LigandsQ57838214
Site of G protein binding to rhodopsin mapped with synthetic peptides from the alpha subunitQ70399454
A novel site on the Galpha -protein that recognizes heptahelical receptorsQ73067495
Phenylalanine 138 in the second intracellular loop of human thromboxane receptor is critical for receptor-G-protein couplingQ73098013
The N-terminal extension of Galphaq is critical for constraining the selectivity of receptor couplingQ73541773
Molecular aspects of vasopressin receptor functionQ74457839
Roles of the transducin alpha-subunit alpha4-helix/alpha4-beta6 loop in the receptor and effector interactionsQ74602426
The receptor-bound "empty pocket" state of the heterotrimeric G-protein alpha-subunit is conformationally dynamicQ79292619
The membrane complex between transducin and dark-state rhodopsin exhibits large-amplitude interface dynamics on the sub-microsecond timescale: insights from all-atom MD simulationsQ83035606
P433issue13
P407language of work or nameEnglishQ1860
P921main subjectG protein-coupled receptorQ38173
P304page(s)2288-2298
P577publication date2013-04-16
P1433published inJournal of Molecular BiologyQ925779
P1476titleConformational flexibility and structural dynamics in GPCR-mediated G protein activation: a perspective
P478volume425

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cites work (P2860)
Q493446005-HT2C Receptor Structures Reveal the Structural Basis of GPCR Polypharmacology.
Q51052184A conformation-equilibrium model captures ligand-ligand interactions and ligand-biased signalling by G-protein coupled receptors.
Q28543750A dynamic view of molecular switch behavior at serotonin receptors: implications for functional selectivity
Q28249697A functional selectivity mechanism at the serotonin-2A GPCR involves ligand-dependent conformations of intracellular loop 2
Q27681985A transient interaction between the phosphate binding loop and switch I contributes to the allosteric network between receptor and nucleotide in Gαi1.
Q47979078Activation processes in ligand-activated G protein-coupled receptors: A case study of the adenosine A2A receptor
Q35188726Active-state model of a dopamine D2 receptor-Gαi complex stabilized by aripiprazole-type partial agonists
Q91958978Assembly of a GPCR-G Protein Complex
Q35134557Bacterial chemoreceptor dynamics correlate with activity state and are coupled over long distances
Q91156903Biased Agonist TRV027 Determinants in AT1R by Molecular Dynamics Simulations
Q35752199Biased signaling: potential agonist and antagonist of PAR2.
Q30368025Chemistry and biology of the initial steps in vision: the Friedenwald lecture.
Q48118681Comprehensive analysis of sphingosine-1-phosphate receptor mutants during zebrafish embryogenesis
Q28265667Conformational states of the full-length glucagon receptor
Q41151319Conformational thermostabilisation of corticotropin releasing factor receptor 1.
Q36394992Crucial role of the orexin-B C-terminus in the induction of OX1 receptor-mediated apoptosis: analysis by alanine scanning, molecular modelling and site-directed mutagenesis.
Q60921876Crystal structures of the human neurokinin 1 receptor in complex with clinically used antagonists
Q35198382Crystallization scale preparation of a stable GPCR signaling complex between constitutively active rhodopsin and G-protein
Q52604833Design, Synthesis, and Characterization of 4-Undecylpiperidine-2-carboxamides as Positive Allosteric Modulators of the Serotonin (5-HT) 5-HT2C Receptor.
Q37626332Energetic analysis of the rhodopsin-G-protein complex links the α5 helix to GDP release
Q30394046Exploring the mechanism of F282L mutation-caused constitutive activity of GPCR by a computational study
Q42699012Frustration-guided motion planning reveals conformational transitions in proteins
Q38211688Harnessing allostery: a novel approach to drug discovery
Q89982570Heterotrimeric Gq proteins as therapeutic targets?
Q43182019In vitro screening of major neurotransmitter systems possibly involved in the mechanism of action of antibodies to S100 protein in released-active form.
Q91710471Mechanistic Insights into Specific G Protein Interactions with Adenosine Receptors
Q34041202Mechanistic insights into the allosteric modulation of opioid receptors by sodium ions
Q64086965Molecular Dynamics Simulations of the Allosteric Modulation of the Adenosine A2A Receptor by a Mini-G Protein
Q28546825Nullspace Sampling with Holonomic Constraints Reveals Molecular Mechanisms of Protein Gαs
Q36096058Opioid receptors: Structural and mechanistic insights into pharmacology and signaling
Q35611767Quantifying conformational changes in GPCRs: glimpse of a common functional mechanism.
Q64229278Rational design of a heterotrimeric G protein α subunit with artificial inhibitor sensitivity
Q37551902Recent Progress in Understanding the Conformational Mechanism of Heterotrimeric G Protein Activation
Q91620038Recent advances in computational studies of GPCR-G protein interactions
Q64282228Receptor selectivity between the G proteins Gα and Gα is defined by a single leucine-to-isoleucine variation
Q56979785Simulation of spontaneous G protein activation reveals a new intermediate driving GDP unbinding
Q42694413Structural Basis for G Protein-Coupled Receptor Activation
Q28237034Structural approaches to understanding retinal proteins needed for vision
Q33931230Structural basis of G protein-coupled receptor-Gi protein interaction: formation of the cannabinoid CB2 receptor-Gi protein complex
Q96640363Structural mechanism underlying primary and secondary coupling between GPCRs and the Gi/o family
Q49895947Tauroursodeoxycholic acid binds to the G-protein site on light activated rhodopsin.
Q44441472The future of drug discovery: enabling technologies for enhancing lead characterization and profiling therapeutic potential
Q50249181The nucleotide-free state of heterotrimeric G proteins α-subunit adopts a highly stable conformation.
Q92616378The steroid hormone 20-hydroxyecdysone binds to dopamine receptor to repress lepidopteran insect feeding and promote pupation
Q64998361Tracking yeast pheromone receptor Ste2 endocytosis using fluorogen-activating protein tagging.
Q36269542Unifying view of mechanical and functional hotspots across class A GPCRs.
Q36899633Universal allosteric mechanism for Gα activation by GPCRs
Q43155783What can we learn from molecular dynamics simulations for GPCR drug design?

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