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- PDB-2bcj: Crystal Structure of G Protein-Coupled Receptor Kinase 2 in Compl... -
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Basic information
Entry | Database: PDB / ID: 2bcj | ||||||
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Title | Crystal Structure of G Protein-Coupled Receptor Kinase 2 in Complex with Galpha-q and Gbetagamma Subunits | ||||||
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![]() | TRANSFERASE/HYDROLASE / Peripheral membrane complex / protein kinase / RGS domain / WD40 protein / heterotrimeric G protein / TRANSFERASE-HYDROLASE COMPLEX | ||||||
Function / homology | ![]() Fatty Acids bound to GPR40 (FFAR1) regulate insulin secretion / Acetylcholine regulates insulin secretion / PLC beta mediated events / forebrain neuron development / regulation of melanocyte differentiation / Calmodulin induced events / beta-adrenergic-receptor kinase / negative regulation of the force of heart contraction by chemical signal / negative regulation of relaxation of smooth muscle / Activation of SMO ...Fatty Acids bound to GPR40 (FFAR1) regulate insulin secretion / Acetylcholine regulates insulin secretion / PLC beta mediated events / forebrain neuron development / regulation of melanocyte differentiation / Calmodulin induced events / beta-adrenergic-receptor kinase / negative regulation of the force of heart contraction by chemical signal / negative regulation of relaxation of smooth muscle / Activation of SMO / Cooperation of PDCL (PhLP1) and TRiC/CCT in G-protein beta folding / Thromboxane signalling through TP receptor / beta-adrenergic receptor kinase activity / G protein-coupled receptor kinase activity / Thrombin signalling through proteinase activated receptors (PARs) / Edg-2 lysophosphatidic acid receptor binding / alpha-2A adrenergic receptor binding / Extra-nuclear estrogen signaling / G-protein activation / Adenylate cyclase inhibitory pathway / G alpha (q) signalling events / endothelin receptor signaling pathway / ion channel modulating, G protein-coupled receptor signaling pathway / phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathway / Olfactory Signaling Pathway / developmental pigmentation / Sensory perception of sweet, bitter, and umami (glutamate) taste / Synthesis, secretion, and inactivation of Glucagon-like Peptide-1 (GLP-1) / negative regulation of striated muscle contraction / desensitization of G protein-coupled receptor signaling pathway / positive regulation of protein localization to cilium / Cargo recognition for clathrin-mediated endocytosis / phospholipase C-activating dopamine receptor signaling pathway / cranial skeletal system development / ADP signalling through P2Y purinoceptor 1 / regulation of platelet activation / regulation of the force of heart contraction / Activation of the phototransduction cascade / maternal behavior / positive regulation of smoothened signaling pathway / G protein-coupled receptor internalization / Adrenaline,noradrenaline inhibits insulin secretion / ADP signalling through P2Y purinoceptor 12 / glutamate receptor signaling pathway / GTPase activating protein binding / negative regulation of synaptic transmission / G alpha (i) signalling events / Activation of G protein gated Potassium channels / G-protein activation / G beta:gamma signalling through PI3Kgamma / Prostacyclin signalling through prostacyclin receptor / G beta:gamma signalling through PLC beta / ADP signalling through P2Y purinoceptor 1 / Thromboxane signalling through TP receptor / Presynaptic function of Kainate receptors / G beta:gamma signalling through CDC42 / Inhibition of voltage gated Ca2+ channels via Gbeta/gamma subunits / Glucagon-type ligand receptors / Adrenaline,noradrenaline inhibits insulin secretion / G alpha (12/13) signalling events / G beta:gamma signalling through BTK / alkylglycerophosphoethanolamine phosphodiesterase activity / ADP signalling through P2Y purinoceptor 12 / Cooperation of PDCL (PhLP1) and TRiC/CCT in G-protein beta folding / Thrombin signalling through proteinase activated receptors (PARs) / Ca2+ pathway / G alpha (z) signalling events / Extra-nuclear estrogen signaling / G alpha (s) signalling events / G alpha (q) signalling events / action potential / G alpha (i) signalling events / Glucagon-like Peptide-1 (GLP1) regulates insulin secretion / neuron remodeling / embryonic digit morphogenesis / Vasopressin regulates renal water homeostasis via Aquaporins / ligand-gated ion channel signaling pathway / negative regulation of potassium ion transport / regulation of signal transduction / positive regulation of protein localization to cell cortex / regulation of cAMP-mediated signaling / D2 dopamine receptor binding / G protein-coupled serotonin receptor binding / cardiac muscle contraction / enzyme regulator activity / regulation of mitotic spindle organization / cellular response to forskolin / GTPase activator activity / post-embryonic development / G protein activity / skeletal system development / caveola / cell projection / G protein-coupled receptor binding / positive regulation of smooth muscle cell proliferation / intracellular protein transport / G-protein beta/gamma-subunit complex binding / adenylate cyclase-modulating G protein-coupled receptor signaling pathway / adenylate cyclase-activating G protein-coupled receptor signaling pathway / positive regulation of insulin secretion Similarity search - Function | ||||||
Biological species | ![]() ![]() ![]() ![]() ![]() ![]() | ||||||
Method | ![]() ![]() ![]() | ||||||
![]() | Tesmer, J.J.G. | ||||||
![]() | ![]() Title: Snapshot of Activated G Proteins at the Membrane: The Gq-GRK2-G Complex Authors: Tesmer, V.M. / Kawano, T. / Shankaranarayanan, A. / Kozasa, T. / Tesmer, J.J.G. | ||||||
History |
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Structure visualization
Structure viewer | Molecule: ![]() ![]() |
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Downloads & links
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Download
PDBx/mmCIF format | ![]() | 282.5 KB | Display | ![]() |
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PDB format | ![]() | 221.8 KB | Display | ![]() |
PDBx/mmJSON format | ![]() | Tree view | ![]() | |
Others | ![]() |
-Validation report
Summary document | ![]() | 865.4 KB | Display | ![]() |
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Full document | ![]() | 874.3 KB | Display | |
Data in XML | ![]() | 44.7 KB | Display | |
Data in CIF | ![]() | 61.7 KB | Display | |
Arichive directory | ![]() ![]() | HTTPS FTP |
-Related structure data
Related structure data | ![]() 1omwS S: Starting model for refinement |
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Similar structure data |
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Links
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Assembly
Deposited unit | ![]()
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Unit cell |
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Components
-Protein , 1 types, 1 molecules A
#1: Protein | Mass: 79749.922 Da / Num. of mol.: 1 / Fragment: residues 28-689 / Mutation: S670A Source method: isolated from a genetically manipulated source Source: (gene. exp.) ![]() ![]() ![]() References: UniProt: P21146, beta-adrenergic-receptor kinase |
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-Guanine nucleotide-binding protein ... , 3 types, 3 molecules BGQ
#2: Protein | Mass: 37311.770 Da / Num. of mol.: 1 Source method: isolated from a genetically manipulated source Source: (gene. exp.) ![]() ![]() ![]() |
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#3: Protein | Mass: 7845.078 Da / Num. of mol.: 1 / Mutation: C68S Source method: isolated from a genetically manipulated source Source: (gene. exp.) ![]() ![]() ![]() |
#4: Protein | Mass: 41298.895 Da / Num. of mol.: 1 Source method: isolated from a genetically manipulated source Source: (gene. exp.) ![]() ![]() ![]() ![]() Genus: Rattus, Mus / Species: , / Gene: Gnai1, Gnai-1, Gnaq / Plasmid: pFastBacHTA / Cell line (production host): High-5 cells / Production host: ![]() |
-Non-polymers , 4 types, 8 molecules ![](data/chem/img/MG.gif)
![](data/chem/img/ALF.gif)
![](data/chem/img/GDP.gif)
![](data/chem/img/HOH.gif)
![](data/chem/img/ALF.gif)
![](data/chem/img/GDP.gif)
![](data/chem/img/HOH.gif)
#5: Chemical | ChemComp-MG / |
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#6: Chemical | ChemComp-ALF / |
#7: Chemical | ChemComp-GDP / |
#8: Water | ChemComp-HOH / |
-Experimental details
-Experiment
Experiment | Method: ![]() |
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Sample preparation
Crystal | Density Matthews: 3.22 Å3/Da / Density % sol: 61.81 % |
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Crystal grow | Temperature: 277 K / Method: vapor diffusion, hanging drop / pH: 6.5 Details: 9% PEG8000, 1M NaCl, 0.1M MES, pH 6.5, VAPOR DIFFUSION, HANGING DROP, temperature 277K |
-Data collection
Diffraction | Mean temperature: 100 K |
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Diffraction source | Source: ![]() ![]() ![]() |
Detector | Type: ADSC QUANTUM 4 / Detector: CCD / Date: Apr 7, 2005 |
Radiation | Monochromator: Si(111) / Protocol: SINGLE WAVELENGTH / Monochromatic (M) / Laue (L): M / Scattering type: x-ray |
Radiation wavelength | Wavelength: 1.116 Å / Relative weight: 1 |
Reflection | Resolution: 3.06→46.78 Å / Num. all: 37836 / Num. obs: 37836 / % possible obs: 100 % / Observed criterion σ(F): 0 / Observed criterion σ(I): -2 / Redundancy: 5.7 % / Biso Wilson estimate: 75 Å2 / Rsym value: 0.133 / Net I/σ(I): 13.55 |
Reflection shell | Resolution: 3.06→3.21 Å / Mean I/σ(I) obs: 1.1 / Num. unique all: 3738 / Rsym value: 0.849 / % possible all: 99.9 |
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Processing
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Refinement | Method to determine structure: ![]() Starting model: PDB ENTRY 1OMW, homology model of Galphaq Resolution: 3.061→46.78 Å / Cor.coef. Fo:Fc: 0.943 / SU B: 50.535 / SU ML: 0.343 / TLS residual ADP flag: LIKELY RESIDUAL / Isotropic thermal model: isotropic / σ(F): 0 / Stereochemistry target values: MAXIMUM LIKELIHOOD Details: HYDROGENS HAVE BEEN ADDED IN THE RIDING POSITIONS. Rfree was not used for the last three rounds of refinement.
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Solvent computation | Ion probe radii: 0.8 Å / Shrinkage radii: 0.8 Å / VDW probe radii: 1.2 Å / Solvent model: MASK | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Displacement parameters | Biso mean: 99.74 Å2
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Refinement step | Cycle: LAST / Resolution: 3.061→46.78 Å
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Refine LS restraints |
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LS refinement shell | Resolution: 3.061→3.141 Å / Total num. of bins used: 20
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Refinement TLS params. | Method: refined / Origin x: 16.358 Å / Origin y: -1.5957 Å / Origin z: 6.6176 Å
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Refinement TLS group | Refine-ID: X-RAY DIFFRACTION / Refine TLS-ID: 1 / Selection: ALL
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