Phase-plate cryo-EM structure of a biased agonist-bound human GLP-1 receptor-Gs complex.

scientific article published on 21 February 2018

Phase-plate cryo-EM structure of a biased agonist-bound human GLP-1 receptor-Gs complex. is …
instance of (P31):
scholarly articleQ13442814

External links are
P356DOI10.1038/NATURE25773
P2888exact matchhttps://scigraph.springernature.com/pub.10.1038/nature25773
P698PubMed publication ID29466332

P50authorArthur ChristopoulosQ18977850
Sebastian FurnessQ57072112
David M ThalQ58208912
Alisa GlukhovaQ59822075
Radostin DanevQ87416556
Peishen ZhaoQ90469982
Laurence J MillerQ96046330
Cassandra KooleQ114366385
Yi-Lynn LiangQ114366405
Maryam KhoshoueiQ114366408
Lachlan ClydesdaleQ114366409
Saifei LeiQ114366410
Patrick M. SextonQ39936838
Denise WoottenQ43294588
P2093author name stringWolfgang Baumeister
Ming-Wei Wang
Mazdak Radjainia
Tin T Truong
P2860cites workStructure of class B GPCR corticotropin-releasing factor receptor 1Q24309523
Structure of the human glucagon class B G-protein-coupled receptorQ24601619
MolProbity: all-atom structure validation for macromolecular crystallographyQ24649111
PHENIX: a comprehensive Python-based system for macromolecular structure solutionQ24654617
Volta phase plate cryo-EM of the small protein complex Prx3Q27334242
A Hydrogen-Bonded Polar Network in the Core of the Glucagon-Like Peptide-1 Receptor Is a Fulcrum for Biased Agonism: Lessons from Class B Crystal StructuresQ27345100
Crystal structure of the ligand-bound glucagon-like peptide-1 receptor extracellular domainQ27649890
Coot: model-building tools for molecular graphicsQ27860505
UCSF Chimera--a visualization system for exploratory research and analysisQ27860666
EMAN2: an extensible image processing suite for electron microscopyQ27861052
Glucagon-Like Peptide-1 and Its Class B G Protein-Coupled Receptors: A Long March to Therapeutic SuccessesQ28067465
Structural Determinants of Binding the Seven-transmembrane Domain of the Glucagon-like Peptide-1 Receptor (GLP-1R)Q28274664
The Extracellular Surface of the GLP-1 Receptor Is a Molecular Trigger for Biased AgonismQ28276469
Key interactions by conserved polar amino acids located at the transmembrane helical boundaries in Class B GPCRs modulate activation, effector specificity and biased signalling in the glucagon-like peptide-1 receptorQ28278129
Automated electron microscope tomography using robust prediction of specimen movementsQ29616585
Volta potential phase plate for in-focus phase contrast transmission electron microscopy.Q34480911
A Gsalpha mutant designed to inhibit receptor signaling through Gs.Q34817858
Glucagon-like peptide-1 (GLP-1) analogs: recent advances, new possibilities, and therapeutic implications.Q35087846
Ligand binding pocket formed by evolutionarily conserved residues in the glucagon-like peptide-1 (GLP-1) receptor core domainQ35126680
Allosteric ligands of the glucagon-like peptide 1 receptor (GLP-1R) differentially modulate endogenous and exogenous peptide responses in a pathway-selective manner: implications for drug screening.Q35454522
Second extracellular loop of human glucagon-like peptide-1 receptor (GLP-1R) has a critical role in GLP-1 peptide binding and receptor activationQ35763258
Autocrine selection of a GLP-1R G-protein biased agonist with potent antidiabetic effectsQ35856484
Polar transmembrane interactions drive formation of ligand-specific and signal pathway-biased family B G protein-coupled receptor conformationsQ36729833
Peptide binding at the GLP-1 receptor.Q36883903
Accelerated cryo-EM structure determination with parallelisation using GPUs in RELION-2.Q37643700
Single-molecule analysis of ligand efficacy in β2AR-G-protein activationQ38728709
Characterization of signal bias at the GLP-1 receptor induced by backbone modification of GLP-1.Q38864019
A simple method to generate stable cell lines for the analysis of transient protein-protein interactions.Q39167406
The peptide agonist-binding site of the glucagon-like peptide-1 (GLP-1) receptor based on site-directed mutagenesis and knowledge-based modellingQ40284076
A highly effective dominant negative alpha s construct containing mutations that affect distinct functions inhibits multiple Gs-coupled receptor signaling pathwaysQ40740952
Cryo-EM structure of haemoglobin at 3.2 Å determined with the Volta phase plate.Q40964898
The N54 mutant of Galphas has a conditional dominant negative phenotype which suppresses hormone-stimulated but not basal cAMP levelsQ40973473
Cryo-EM structure of the activated GLP-1 receptor in complex with a G proteinQ41597824
Phase-plate cryo-EM structure of a class B GPCR-G-protein complexQ41598194
MotionCor2: anisotropic correction of beam-induced motion for improved cryo-electron microscopyQ41598828
Gctf: Real-time CTF determination and correctionQ41603517
Identification of effector-activating residues of Gs alphaQ41927516
Residues within the transmembrane domain of the glucagon-like peptide-1 receptor involved in ligand binding and receptor activation: modelling the ligand-bound receptorQ42289659
β-Arrestin-Biased Agonists of the GLP-1 Receptor from β-Amino Acid Residue Incorporation into GLP-1 Analogues.Q43294448
The relationship between muscarinic receptor occupancy and adenylate cyclase inhibition in the rabbit myocardiumQ44750185
The G226A mutant of Gs alpha highlights the requirement for dissociation of G protein subunitsQ48547818
Crystal structure of the GLP-1 receptor bound to a peptide agonist.Q50968563
Ligand-Dependent Modulation of G Protein Conformation Alters Drug Efficacy.Q51413360
Differential activation and modulation of the glucagon-like peptide-1 receptor by small molecule ligands.Q51755093
P433issue7694
P407language of work or nameEnglishQ1860
P921main subjectcryogenic electron microscopyQ5190506
P304page(s)121-125
P577publication date2018-02-21
P1433published inNatureQ180445
P1476titlePhase-plate cryo-EM structure of a biased agonist-bound human GLP-1 receptor-Gs complex.
P478volume555

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cites work (P2860)
Q61797498A conserved molecular switch in Class F receptors regulates receptor activation and pathway selection
Q91793624A free-energy landscape for the glucagon-like peptide 1 receptor GLP1R
Q90702264A tetrapeptide class of biased analgesics from an Australian fungus targets the µ-opioid receptor
Q102389011A unique hormonal recognition feature of the human glucagon-like peptide-2 receptor
Q92503863Activation of the GLP-1 receptor by a non-peptidic agonist
Q92966015Adhesion G protein-coupled receptors: opportunities for drug discovery
Q96132105Advances in therapeutic peptides targeting G protein-coupled receptors
Q92726723Agonist-induced membrane nanodomain clustering drives GLP-1 receptor responses in pancreatic beta cells
Q97424458Allosteric interactions in the parathyroid hormone GPCR-arrestin complex formation
Q63384169An online resource for GPCR structure determination and analysis
Q91028738Angiotensin Analogs with Divergent Bias Stabilize Distinct Receptor Conformations
Q57178721Cryo-EM in drug discovery: achievements, limitations and prospects
Q98513557Cryo-EM structure of an activated VIP1 receptor-G protein complex revealed by a NanoBiT tethering strategy
Q59054344Cryo-EM structure of the active, G-protein complexed, human CGRP receptor
Q55072103Cryo-EM structure of the adenosine A2A receptor coupled to an engineered heterotrimeric G protein.
Q90208754Cryo-EM structure of the human PAC1 receptor coupled to an engineered heterotrimeric G protein
Q89665174Cryo-EM structures of PAC1 receptor reveal ligand binding mechanism
Q90227702Crystal structure of misoprostol bound to the labor inducer prostaglandin E2 receptor
Q90700746Deconvoluting the Molecular Control of Binding and Signaling at the Amylin 3 Receptor: RAMP3 Alters Signal Propagation through Extracellular Loops of the Calcitonin Receptor
Q58743879Development of an antibody fragment that stabilizes GPCR/G-protein complexes
Q90700653Dominant Negative G Proteins Enhance Formation and Purification of Agonist-GPCR-G Protein Complexes for Structure Determination
Q53819708Emerging Paradigm of Intracellular Targeting of G Protein-Coupled Receptors.
Q49898093Extracellular loops 2 and 3 of the calcitonin receptor selectively modify agonist binding and efficacy.
Q64245124G-Protein-Coupled Receptors Are Dynamic Regulators of Digestion and Targets for Digestive Diseases
Q99557365IMPROvER: the Integral Membrane Protein Stability Selector
Q91877264In vitro expansion of pancreatic islet clusters facilitated by hormones and chemicals
Q89999018Ligand-induced conformational changes in a SMALP-encapsulated GPCR
Q90929094Mechanisms of signalling and biased agonism in G protein-coupled receptors
Q91595350Molecular pharmacology of metabotropic receptors targeted by neuropsychiatric drugs
Q92905229Nature-Derived Peptides: A Growing Niche for GPCR Ligand Discovery
Q68687096O-GlcNAc Engineering of GPCR Peptide-Agonists Improves Their Stability and in Vivo Activity
Q57799810Off-axis rotor in Enterococcus hirae V-ATPase visualized by Zernike phase plate single-particle cryo-electron microscopy
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
Q90700670Rules of Engagement: GPCRs and G Proteins
Q90727051State-dependent Lipid Interactions with the A2a Receptor Revealed by MD Simulations Using In Vivo-Mimetic Membranes
Q101573412Structural basis for GLP-1 receptor activation by LY3502970, an orally active nonpeptide agonist
Q100632913Structural basis for activation of the growth hormone-releasing hormone receptor
Q57830732Structural basis for signal recognition and transduction by platelet-activating-factor receptor
Q97650820Structural basis of GPBAR activation and bile acid recognition
Q57472386Structural biology of G protein-coupled receptor signaling complexes
Q51761770Structural biology of G protein-coupled receptors: new opportunities from XFELs and cryoEM.
Q112701327Structural determinants of dual incretin receptor agonism by tirzepatide
Q59082343Structural insights into G-protein-coupled receptor allostery
Q98175934Structural insights into differences in G protein activation by family A and family B GPCRs
Q98158665Structural insights into the activation of GLP-1R by a small molecule agonist
Q60958062Structural organization of a major neuronal G protein regulator, the RGS7-Gβ5-R7BP complex
Q98564759Structure and dynamics of the active Gs-coupled human secretin receptor
Q93040409Structure and dynamics of the active human parathyroid hormone receptor-1
Q91330297Structure of an endosomal signaling GPCR-G protein-β-arrestin megacomplex
Q59060936Structure of the adenosine-bound human adenosine A1 receptor–Gi complex
Q91827049Targeting G protein-coupled receptor signalling by blocking G proteins
Q91717863Targeting the PAC1 Receptor for Neurological and Metabolic Disorders
Q90700712The Molecular Control of Calcitonin Receptor Signaling
Q90008664The atomistic level structure for the activated human κ-opioid receptor bound to the full Gi protein and the MP1104 agonist
Q53282873Two distinct domains of the glucagon-like peptide-1 receptor control peptide-mediated biased agonism.
Q89520120Ureidopeptide GLP-1 analogues with prolonged activity in vivo via signal bias and altered receptor trafficking
Q90335850β2 Adrenergic Receptor Complexes with the L-Type Ca2+ Channel CaV1.2 and AMPA-Type Glutamate Receptors: Paradigms for Pharmacological Targeting of Protein Interactions

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