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- PDB-3ah8: Structure of heterotrimeric G protein Galpha-q beta gamma in comp... -
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Basic information
Entry | Database: PDB / ID: 3ah8 | |||||||||
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Title | Structure of heterotrimeric G protein Galpha-q beta gamma in complex with an inhibitor YM-254890 | |||||||||
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![]() | SIGNALING PROTEIN/INHIBITOR / Heterotrimeric G protein / GTPase / Galpha-q / Gbeta / Ggamma / Inhibitor / YM-254890 / SIGNALING PROTEIN / SIGNALING PROTEIN-INHIBITOR 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 / Cooperation of PDCL (PhLP1) and TRiC/CCT in G-protein beta folding / Thromboxane signalling through TP receptor / Thrombin signalling through proteinase activated receptors (PARs) / Extra-nuclear estrogen signaling / G-protein activation ...Fatty Acids bound to GPR40 (FFAR1) regulate insulin secretion / Acetylcholine regulates insulin secretion / PLC beta mediated events / forebrain neuron development / regulation of melanocyte differentiation / Cooperation of PDCL (PhLP1) and TRiC/CCT in G-protein beta folding / Thromboxane signalling through TP receptor / Thrombin signalling through proteinase activated receptors (PARs) / 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) / phospholipase C-activating dopamine receptor signaling pathway / cranial skeletal system development / ADP signalling through P2Y purinoceptor 1 / regulation of platelet activation / Activation of the phototransduction cascade / maternal behavior / 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 / positive regulation of protein localization to cell cortex / regulation of cAMP-mediated signaling / D2 dopamine receptor binding / G protein-coupled serotonin receptor binding / 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 / G protein-coupled receptor binding / positive regulation of smooth muscle cell proliferation / 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 / photoreceptor disc membrane / regulation of blood pressure / cellular response to catecholamine stimulus / adenylate cyclase-activating dopamine receptor signaling pathway / cellular response to prostaglandin E stimulus / GDP binding / G-protein beta-subunit binding / heterotrimeric G-protein complex / signaling receptor complex adaptor activity / phospholipase C-activating G protein-coupled receptor signaling pathway / heart development / cell cortex / midbody / cell body / nuclear membrane / cell cycle / G protein-coupled receptor signaling pathway / cell division / GTPase activity / centrosome Similarity search - Function | |||||||||
Biological species | ![]() ![]() ![]() ![]() ![]() ![]() ![]() | |||||||||
Method | ![]() ![]() ![]() | |||||||||
![]() | Nishimura, A. / Kitano, K. / Takasaki, J. / Taniguchi, M. / Mizuno, N. / Tago, K. / Hakoshima, T. / Itoh, H. | |||||||||
![]() | ![]() Title: Structural basis for the specific inhibition of heterotrimeric Gq protein by a small molecule. Authors: Nishimura, A. / Kitano, K. / Takasaki, J. / Taniguchi, M. / Mizuno, N. / Tago, K. / Hakoshima, T. / Itoh, H. | |||||||||
History |
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Structure visualization
Structure viewer | Molecule: ![]() ![]() |
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Downloads & links
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Download
PDBx/mmCIF format | ![]() | 159.4 KB | Display | ![]() |
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PDB format | ![]() | 120.6 KB | Display | ![]() |
PDBx/mmJSON format | ![]() | Tree view | ![]() | |
Others | ![]() |
-Validation report
Summary document | ![]() | 798.4 KB | Display | ![]() |
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Full document | ![]() | 826.5 KB | Display | |
Data in XML | ![]() | 30.1 KB | Display | |
Data in CIF | ![]() | 40 KB | Display | |
Arichive directory | ![]() ![]() | HTTPS FTP |
-Related 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
#1: Protein | Mass: 41427.027 Da / Num. of mol.: 1 Fragment: UNP entry P10824 residues 2-28, UNP entry P21279 residues 37-359 Source method: isolated from a genetically manipulated source Source: (gene. exp.) ![]() ![]() ![]() ![]() Gene: gmhB / Production host: ![]() |
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#2: Protein | Mass: 37416.930 Da / Num. of mol.: 1 Source method: isolated from a genetically manipulated source Source: (gene. exp.) ![]() ![]() ![]() |
#3: Protein | Mass: 8592.894 Da / Num. of mol.: 1 / Mutation: C68S Source method: isolated from a genetically manipulated source Source: (gene. exp.) ![]() ![]() ![]() |
#4: Protein/peptide | |
#5: Chemical | ChemComp-GDP / |
-Experimental details
-Experiment
Experiment | Method: ![]() |
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Sample preparation
Crystal | Density Matthews: 2.59 Å3/Da / Density % sol: 52.5 % |
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Crystal grow | Temperature: 293 K / Method: vapor diffusion / pH: 5.1 Details: 7% PEG 4000, 30% (v/v) glycerol, 70 mM acetate-NaOH, pH 5.1, VAPOR DIFFUSION, temperature 293K |
-Data collection
Diffraction | Mean temperature: 100 K |
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Diffraction source | Source: ![]() ![]() ![]() |
Detector | Type: ADSC QUANTUM 315 / Detector: CCD / Date: Nov 24, 2007 |
Radiation | Protocol: SINGLE WAVELENGTH / Monochromatic (M) / Laue (L): M / Scattering type: x-ray |
Radiation wavelength | Wavelength: 1 Å / Relative weight: 1 |
Reflection | Resolution: 2.9→20 Å / Num. obs: 19018 / % possible obs: 94.1 % / Redundancy: 4.2 % / Rmerge(I) obs: 0.059 |
Reflection shell | Resolution: 2.9→3 Å / Redundancy: 4.1 % / Rmerge(I) obs: 0.526 / Mean I/σ(I) obs: 2.4 / % possible all: 76.9 |
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Processing
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Refinement | Method to determine structure: ![]() Starting model: PDB ENTRIES 2BCJ and 1GP2 Resolution: 2.9→20 Å / Isotropic thermal model: Isotropic / Cross valid method: THROUGHOUT
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Displacement parameters | Biso mean: 91.53 Å2 | ||||||||||||||||||||
Refinement step | Cycle: LAST / Resolution: 2.9→20 Å
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LS refinement shell | Resolution: 2.9→3 Å /
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