The allosteric vestibule of a seven transmembrane helical receptor controls G-protein coupling

scientific article

The allosteric vestibule of a seven transmembrane helical receptor controls G-protein coupling is …
instance of (P31):
scholarly articleQ13442814

External links are
P819ADS bibcode2012NatCo...3.1044B
P6179Dimensions Publication ID1046138584
P356DOI10.1038/NCOMMS2028
P932PMC publication ID3658004
P698PubMed publication ID22948826
P5875ResearchGate publication ID230797734

P50authorUlrike HolzgrabeQ21264805
Andreas BockQ58898154
Clelia DallanoceQ39931326
Marco De AmiciQ39931394
Carlo MateraQ42870197
P2093author name stringEvi Kostenis
Anke Müller
Carsten Hoffmann
Jens Schmitz
Klaus Mohr
Christian Tränkle
Lucas Peters
Nicole Merten
Jessica Klöckner
Ramona Schrage
Julia Bätz
Katharina Simon
Anna Kebig
Jasmin Schrobang-Ley
P2860cites workAgonist-bound adenosine A2A receptor structures reveal common features of GPCR activationQ24303747
Structure of a nanobody-stabilized active state of the β(2) adrenoceptorQ24597139
Structure of the human M2 muscarinic acetylcholine receptor bound to an antagonistQ24628686
Crystal structure of the β2 adrenergic receptor-Gs protein complexQ24635327
Ligand-specific regulation of the extracellular surface of a G-protein-coupled receptorQ27646733
Crystal structure of opsin in its G-protein-interacting conformationQ27652301
How many drug targets are there?Q28276660
Dual effects of muscarinic M(2) acetylcholine receptors on the synthesis of cyclic AMP in CHO cells: dependence on time, receptor density and receptor agonistsQ28360158
A simple method for quantifying functional selectivity and agonist biasQ28728741
Structural diversity of G protein-coupled receptors and significance for drug discoveryQ29616716
Beta-arrestins and cell signalingQ29616793
Diversity of G proteins in signal transductionQ29618841
Pathway and mechanism of drug binding to G-protein-coupled receptors.Q30503489
Importance of the extracellular loops in G protein-coupled receptors for ligand recognition and receptor activationQ30522852
Identification of orthosteric and allosteric site mutations in M2 muscarinic acetylcholine receptors that contribute to ligand-selective signaling biasQ33748133
Seven transmembrane receptors as shapeshifting proteins: the impact of allosteric modulation and functional selectivity on new drug discoveryQ33890786
Teaching old receptors new tricks: biasing seven-transmembrane receptorsQ33985759
Molecular basis of ligand dissociation in β-adrenergic receptorsQ34018861
The binding site of aminergic G protein-coupled receptors: the transmembrane segments and second extracellular loopQ34504076
G protein-coupled receptor allosterism and complexingQ34523552
Energy landscapes as a tool to integrate GPCR structure, dynamics, and functionQ34664404
Fluorescent labeling of tetracysteine-tagged proteins in intact cellsQ34913250
Applying label-free dynamic mass redistribution technology to frame signaling of G protein-coupled receptors noninvasively in living cells.Q51513968
Operational models of pharmacological agonism.Q52699226
Allosteric Modulation of G Protein–Coupled ReceptorsQ56115675
Convergent, short synthesis of the muscarinic superagonist iperoxoQ58856252
Agonist-independent inhibition of G protein activation by muscarinic acetylcholine receptor antagonists in cardiac membranesQ68033081
Modification of the binding properties of muscarinic receptors by gallamineQ71773661
Linkage of G protein-coupled receptors to the MAPK signaling pathway through PI 3-kinase gammaQ71970954
Allosteric interactions with muscarinic acetylcholine receptors: complex role of the conserved tryptophan M2422Trp in a critical cluster of amino acids for baseline affinity, subtype selectivity, and cooperativityQ83206375
Principles: extending the utility of [35S]GTP gamma S binding assaysQ35057349
Scanning mutagenesis studies of the M1 muscarinic acetylcholine receptorQ35189839
Molecular mechanism of β-arrestin-biased agonism at seven-transmembrane receptorsQ36773326
Collateral efficacy in drug discovery: taking advantage of the good (allosteric) nature of 7TM receptorsQ36880900
The evasive nature of drug efficacy: implications for drug discoveryQ36894549
Muscarinic acetylcholine receptors: mutant mice provide new insights for drug developmentQ36925551
Heterotrimeric G protein activation by G-protein-coupled receptorsQ37017125
When simple agonism is not enough: emerging modalities of GPCR ligands.Q37775132
The best of both worlds? Bitopic orthosteric/allosteric ligands of g protein-coupled receptorsQ37930665
A fluorescence resonance energy transfer-based M2 muscarinic receptor sensor reveals rapid kinetics of allosteric modulationQ39615485
The C-terminal tail of CRTH2 is a key molecular determinant that constrains Galphai and downstream signaling cascade activationQ39916587
Dualsteric GPCR targeting: a novel route to binding and signaling pathway selectivityQ39931162
A novel mechanism of G protein-coupled receptor functional selectivity. Muscarinic partial agonist McN-A-343 as a bitopic orthosteric/allosteric ligand.Q39947679
Ras-dependent activation of MAP kinase pathway mediated by G-protein beta gamma subunits.Q41461969
Detection, quantitation, and verification of allosteric interactions of agents with labeled and unlabeled ligands at G protein-coupled receptors: interactions of strychnine and acetylcholine at muscarinic receptors.Q42277559
Probing the activation-promoted structural rearrangements in preassembled receptor-G protein complexes.Q42595255
Deconvolution of complex G protein-coupled receptor signaling in live cells using dynamic mass redistribution measurements.Q42937057
Measurement of the millisecond activation switch of G protein-coupled receptors in living cellsQ44479240
Allosteric site on muscarinic acetylcholine receptors: identification of two amino acids in the muscarinic M2 receptor that account entirely for the M2/M5 subtype selectivities of some structurally diverse allosteric ligands in N-methylscopolamine-oQ44483391
Interactions of orthosteric and allosteric ligands with [3H]dimethyl-W84 at the common allosteric site of muscarinic M2 receptorsQ44483424
Inhibition of the actions of carbachol and DFP on guinea pig isolated atria by alkane-bis-ammonium compoundsQ46165048
A FlAsH-based FRET approach to determine G protein-coupled receptor activation in living cellsQ46396170
Critical amino acid residues of the common allosteric site on the M2 muscarinic acetylcholine receptor: more similarities than differences between the structurally divergent agents gallamine and bis(ammonio)alkane-type hexamethylene-bis-[dimethyl-(3Q46529162
Allosteric small molecules unveil a role of an extracellular E2/transmembrane helix 7 junction for G protein-coupled receptor activationQ46985701
Functional reconstitution of purified muscarinic receptors and inhibitory guanine nucleotide regulatory protein.Q48461280
P275copyright licenseCreative Commons Attribution-NonCommercial-NoDerivs 3.0 UnportedQ19125045
P6216copyright statuscopyrightedQ50423863
P407language of work or nameEnglishQ1860
P921main subjecttransmembrane proteinQ424204
P304page(s)1044
P577publication date2012-01-01
P1433published inNature CommunicationsQ573880
P1476titleThe allosteric vestibule of a seven transmembrane helical receptor controls G-protein coupling
P478volume3

Reverse relations

cites work (P2860)
Q48136609A Photoswitchable Dualsteric Ligand Controlling Receptor Efficacy.
Q28543750A dynamic view of molecular switch behavior at serotonin receptors: implications for functional selectivity
Q50896283A muscarinic view on Gq.
Q28245604A new mechanism of allostery in a G protein-coupled receptor dimer
Q24308061Activation and allosteric modulation of a muscarinic acetylcholine receptor
Q36342155Advances in receptor conformation research: the quest for functionally selective conformations focusing on the β2-adrenoceptor
Q36836367Agonists with supraphysiological efficacy at the muscarinic M2 ACh receptor.
Q35860717Allosteric Activation of a G Protein-coupled Receptor with Cell-penetrating Receptor Mimetics
Q87410299Allostery: A GPCR's back door
Q55092101Binding, Thermodynamics, and Selectivity of a Non-peptide Antagonist to the Melanocortin-4 Receptor.
Q51266726Bitopic muscarinic agonists and antagonists and uses thereof: a patent evaluation of US20160136145A1.
Q92133857Cryptic pocket formation underlies allosteric modulator selectivity at muscarinic GPCRs
Q33964630Decoding signaling and function of the orphan G protein-coupled receptor GPR17 with a small-molecule agonist
Q60910349Designing Hybrids Targeting the Cholinergic System by Modulating the Muscarinic and Nicotinic Receptors: A Concept to Treat Alzheimer's Disease
Q33922348Differences in allosteric communication pipelines in the inactive and active states of a GPCR.
Q54629048Dynamic ligand binding dictates partial agonism at a G protein-coupled receptor.
Q38211688Harnessing allostery: a novel approach to drug discovery
Q39013350Label-free cell-based dynamic mass redistribution assays
Q41829504Ligand Binding Ensembles Determine Graded Agonist Efficacies at a G Protein-coupled Receptor
Q33577530Mapping of allosteric druggable sites in activation-associated conformers of the M2 muscarinic receptor
Q38066121Molecular alliance-from orthosteric and allosteric ligands to dualsteric/bitopic agonists at G protein coupled receptors
Q38846984Multivalent approaches and beyond: novel tools for the investigation of dopamine D2 receptor pharmacology.
Q38218059Muscarinic acetylcholine receptors: novel opportunities for drug development
Q92534625Novel BQCA- and TBPB-Derived M1 Receptor Hybrid Ligands: Orthosteric Carbachol Differentially Regulates Partial Agonism
Q56001241Novel bipharmacophoric inhibitors of the cholinesterases with affinity to the muscarinic receptors M1 and M2
Q38631744Optical probes based on G protein-coupled receptors - added work or added value?
Q34249775Semisynthetic analogues of toxiferine I and their pharmacological properties at α7 nAChRs, muscle-type nAChRs, and the allosteric binding site of muscarinic M2 receptors
Q38675922Signaling within Allosteric Machines: Signal Transmission Pathways Inside G Protein-Coupled Receptors.
Q51595080Structural Characteristics of the Allosteric Binding Site Represent a Key to Subtype Selective Modulators of Muscarinic Acetylcholine Receptors.
Q50470980Structural basis for modulation of a G-protein-coupled receptor by allosteric drugs.
Q42001057Structure-bias relationships for fenoterol stereoisomers in six molecular and cellular assays at the β2-adrenoceptor.
Q38567235Superagonism at G protein-coupled receptors and beyond
Q36442376The Orphan G Protein-coupled Receptor GPR17 Negatively Regulates Oligodendrocyte Differentiation via Gαi/o and Its Downstream Effector Molecules
Q90192895The Universal 3D QSAR Model for Dopamine D2 Receptor Antagonists
Q27334167The pathway of ligand entry from the membrane bilayer to a lipid G protein-coupled receptor
Q33613196Transmembrane peptides as unique tools to demonstrate the in vivo action of a cross-class GPCR heterocomplex.
Q33888491Tyrosine 308 is necessary for ligand-directed Gs protein-biased signaling of β2-adrenoceptor
Q92409897Utilization of Biased G Protein-Coupled ReceptorSignaling towards Development of Safer andPersonalized Therapeutics

Search more.