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1. Full Text Dopamine D4 receptor ubiquitination
by Skieterska, Kamila and Rondou, Pieter and Van Craenenbroeck, Kathleen
Biochemical Society Transactions, ISSN 0300-5127, 04/2016, Volume 44, Issue 2, pp. 601 - 605
Ubiquitination is a post-translational modification that targets proteins for degradation but can also regulate other cellular processes such as endocytosis,... 
G protein-coupled receptor (GPCR) | Non-lysine ubiquitination | Ubiquitination | Dopamine D | KLHL12 | receptor | Receptors, Dopamine D4 - metabolism | Lysine - metabolism | Microfilament Proteins - metabolism | Receptors, Dopamine D4 - chemistry | Humans
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2. Full Text Structure of the D2 dopamine receptor bound to the atypical antipsychotic drug risperidone
by Wang, Sheng and Che, Tao and Levit, Anat and Shoichet, Brian K and Wacker, Daniel and Roth, Bryan L and Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
Nature, ISSN 0028-0836, 03/2018, Volume 555, Issue 7695, pp. 269 - 273
Dopamine is a neurotransmitter that has been implicated in processes as diverse as reward, addiction, control of coordinated movement, metabolism and hormonal... 
LIGANDS | CLONING | CRYSTAL-STRUCTURE | PHARMACOLOGY | MULTIDISCIPLINARY SCIENCES | CHARGES | RHODOPSIN | MODEL | BETA-ADRENERGIC RECEPTOR | DISCOVERY | AGONIST | Receptors, Dopamine D4 - chemistry | Humans | Receptors, Dopamine D3 - chemistry | Receptors, Dopamine D3 - metabolism | Mutant Proteins - genetics | Models, Molecular | Crystallography, X-Ray | Mutant Proteins - metabolism | Risperidone - chemistry | Receptors, Dopamine D2 - metabolism | Receptors, Dopamine D2 - genetics | Antipsychotic Agents - chemistry | Mutant Proteins - chemistry | Drug Design | Hydrophobic and Hydrophilic Interactions | Receptors, Dopamine D2 - chemistry | Antipsychotic Agents - metabolism | Ligands | Receptors, Dopamine D4 - metabolism | Risperidone - metabolism | Kinetics | Mutation | Binding Sites | Pharmacology, Experimental | Drug interactions | Physiological aspects | Research | Risperidone | Structure | Dopamine receptors | Drugs | Attention deficit disorder | Neuroleptics | Parkinson's disease | Molecular structure | Mental disorders | Parkinsons disease | Schizophrenia | Mental depression | Proteins | Psychotropic drugs | Receptors | Vomiting | Reinforcement | Dopamine D2 receptors | Movement disorders | Crystal structure | Dopamine | Neurodegenerative diseases | Secretion | Attention deficit hyperactivity disorder | Nausea | Metabolism | Side effects | Addiction | Structure-function relationships
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3. Full Text Ultra-large library docking for discovering new chemotypes
by Lyu, Jiankun and Wang, Sheng and Balius, Trent E and Singh, Isha and Levit, Anat and Moroz, Yurii S and O’Meara, Matthew J and Che, Tao and Algaa, Enkhjargal and Tolmachova, Kateryna and Tolmachev, Andrey A and Shoichet, Brian K and Roth, Bryan L and Irwin, John J
Nature, ISSN 0028-0836, 02/2019, Volume 566, Issue 7743, pp. 224 - 229
Despite intense interest in expanding chemical space, libraries containing hundreds-of-millions to billions of diverse molecules have remained inaccessible.... 
RECEPTOR ANTAGONISTS | DATABASE | HIGH-THROUGHPUT | MULTIDISCIPLINARY SCIENCES | ALGORITHM | AUTOMATED DOCKING | DRUG DESIGN | VALIDATION | INHIBITORS | IDENTIFICATION | LIGAND DISCOVERY | Bacterial Proteins - antagonists & inhibitors | Molecular Docking Simulation - methods | Receptors, Dopamine D4 - chemistry | Receptors, Dopamine D4 - agonists | Humans | Bacterial Proteins - chemistry | Crystallography, X-Ray | Machine Learning | Dopamine Agonists - isolation & purification | Small Molecule Libraries - chemistry | beta-Lactamases - chemistry | Observation | beta-Lactamase Inhibitors - isolation & purification | Ligands | Receptors, Dopamine D4 - metabolism | Small Molecule Libraries - isolation & purification | Dopamine Agonists - chemistry | beta-Lactamase Inhibitors - chemistry | Beta lactamases | Health aspects | Libraries | Structure | Crystals | Enzymes | Dopamine | Dopamine D4 receptors | Digital libraries | Signal transduction | Organic chemistry | Inhibitors | Predictions | Docking | Chemical synthesis | Binding sites | Crystal structure
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4. Full Text D-4 dopamine receptor high-resolution structures enable the discovery of selective agonists
by Wang, S and Wacker, D and Levit, A and Che, T and Betz, RM and McCorvy, JD and Venkatakrishnan, AJ and Huang, XP and Dror, RO and Shoichet, BK and Roth, BL and Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
SCIENCE, ISSN 0036-8075, 10/2017, Volume 358, Issue 6361, pp. 381 - 381
Dopamine receptors are implicated in the pathogenesis and treatment of nearly every neuropsychiatric disorder. Although thousands of drugs interact with these... 
SODIUM | COMPLEX | PROTEIN | CRYSTAL-STRUCTURE | MULTIDISCIPLINARY SCIENCES | 2ND | MOLECULAR DETERMINANTS | D3 RECEPTORS | Dopamine Agonists - isolation & purification | Antipsychotic Agents - chemistry | Receptors, Dopamine D4 - chemistry | Receptors, Dopamine D4 - ultrastructure | Humans | Allosteric Site | Protein Conformation | Structure-Activity Relationship | Dopamine Agonists - chemistry | Benzamides - chemistry
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5. Full Text Dopamine D2 and D4 receptor heteromerization and its allosteric receptor–receptor interactions
by Borroto-Escuela, Dasiel O and Craenenbroeck, Kathleen Van and Romero-Fernandez, Wilber and Guidolin, Diego and Woods, Amina S and Rivera, Alicia and Haegeman, Guy and Agnati, Luigi F and Tarakanov, Alexander O and Fuxe, Kjell
Biochemical and Biophysical Research Communications, ISSN 0006-291X, 2011, Volume 404, Issue 4, pp. 928 - 934
► The discovery of D R–D R (D R, D R or D R) heteromers has been made in cellular models. ► D R and D R receptors being the least effective in forming... 
Dopamine D 2R receptor | G protein-coupled receptors | Protein–protein interactions | Allosteric modulation | Heteromerization | Dopamine D 4R receptor | R receptor | Dopamine D | Protein-protein interactions | BIOPHYSICS | Dopamine D2R receptor | BIOCHEMISTRY & MOLECULAR BIOLOGY | COMPLEXES | Dopamine D4R receptor | Amino Acid Sequence | Cell Line | Phosphorylation | Receptors, Dopamine D4 - chemistry | Allosteric Regulation | Humans | Protein Multimerization | Molecular Sequence Data | Receptors, Dopamine D4 - genetics | Receptors, Dopamine D2 - genetics | Mitogen-Activated Protein Kinase 3 - metabolism | Receptors, Dopamine D2 - chemistry | Protein Conformation | Mitogen-Activated Protein Kinase 1 - metabolism | Neurosciences | Human anatomy | Dopamine | Analysis | Physiological aspects | Phenols | Universities and colleges | Gene expression
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6. Full Text Dopamine D2, D3, and D4 Selective Phenylpiperazines as Molecular Probes To Explore the Origins of Subtype Specific Receptor Binding
by Ehrlich, Katharina and Götz, Angela and Bollinger, Stefan and Tschammer, Nuska and Bettinetti, Laura and Härterich, Steffen and Hübner, Harald and Lanig, Harald and Gmeiner, Peter
Journal of Medicinal Chemistry, ISSN 0022-2623, 08/2009, Volume 52, Issue 15, pp. 4923 - 4935
Assembling phenylpiperazines with 7a-azaindole via different spacer elements, we developed subtype selective dopamine receptor ligands of types 1a,c, 2a, and... 
Cricetinae | Mutagenesis, Site-Directed | Cricetulus | Receptors, Dopamine D4 - chemistry | Humans | Models, Molecular | Piperazines - metabolism | Structure-Activity Relationship | Receptors, Dopamine D2 - metabolism | Receptors, Dopamine D1 - metabolism | Animals | Spiperone - metabolism | Receptors, Dopamine D2 - chemistry | Ligands | Piperazines - chemical synthesis | Receptors, Dopamine D4 - metabolism | Radioligand Assay | Receptors, Dopamine D1 - chemistry | CHO Cells | Index Medicus
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7. Full Text Dopamine D4 receptor oligomerization – contribution to receptor biogenesis
by Van Craenenbroeck, Kathleen and Borroto‐Escuela, Dasiel O and Romero‐Fernandez, Wilber and Skieterska, Kamila and Rondou, Pieter and Lintermans, Béatrice and Vanhoenacker, Peter and Fuxe, Kjell and Ciruela, Francisco and Haegeman, Guy
The FEBS Journal, ISSN 1742-464X, 04/2011, Volume 278, Issue 8, pp. 1333 - 1344
Dopamine D4 receptors (D4Rs) are G protein‐coupled receptors that play a role in attention and cognition. In the present study, we investigated the... 
dimerization | receptor biogenesis | bioluminescence resonance energy transfer | G protein‐coupled receptors | dopamine D4 receptor | receptor | G protein-coupled receptors | dopamine D | Receptors, Dopamine D4 - chemistry | Humans | HEK293 Cells | Endoplasmic Reticulum - metabolism | Receptors, Dopamine D4 - metabolism | Luminescent Measurements | Dimerization | Protein Folding | Neurons | Genes | Dopamine
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8. Full Text Structural Insights into 5‑HT1A/D4 Selectivity of WAY-100635 Analogues: Molecular Modeling, Synthesis, and in Vitro Binding
by Dilly, Sébastien and Liégeois, Jean-François
Journal of Chemical Information and Modeling, ISSN 1549-9596, 07/2016, Volume 56, Issue 7, pp. 1324 - 1331
The resurgence of interest in 5-HT1A receptors as a therapeutic target requires the existence of highly selective 5-HT1A ligands. To date, WAY-100635 has been... 
Chemistry Techniques, Synthetic | Receptors, Dopamine D4 - chemistry | Pyridines - chemistry | Humans | Pyridines - chemical synthesis | Models, Molecular | Substrate Specificity | Piperazines - metabolism | Piperazines - chemistry | Receptors, Dopamine D4 - genetics | Spodoptera | Sf9 Cells | Animals | Pyridines - metabolism | Receptor, Serotonin, 5-HT1A - chemistry | Protein Binding | Ligands | Piperazines - chemical synthesis | Protein Conformation | Receptors, Dopamine D4 - metabolism | Molecular Docking Simulation | Mutation | Receptor, Serotonin, 5-HT1A - metabolism
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9. Full Text Isopeptide and ester bond ubiquitination both regulate degradation of the human dopamine receptor 4
by Peeler, Jennifer C and Schedin-Weiss, Sophia and Soula, Mariluz and Kazmi, Manija A and Sakmar, Thomas P
Journal of Biological Chemistry, ISSN 0021-9258, 2017, Volume 292, Issue 52, pp. 21623 - 21630
How an optimal level of human dopamine D4 receptor (hD4R) is maintained in synaptic membranes is not known. We show here that hD4R is ubiquitinated in primary... 
proteasome | NON-LYSINE UBIQUITINATION | COMPLEX | PROTEIN | BIOCHEMISTRY & MOLECULAR BIOLOGY | ADRENERGIC-RECEPTOR | dopamine receptor | E3 LIGASE | ubiquitylation (ubiquitination) | SERINE | G protein-coupled receptor (GPCR) | UBIQUITYLATION | ENDOPLASMIC-RETICULUM | RESIDUES | protein degradation | Amino Acid Sequence | Bortezomib | Receptors, Dopamine | Receptors, Dopamine D4 - chemistry | Humans | Ubiquitin - metabolism | Ubiquitination | Arginine | Lysine | HEK293 Cells | Protein Binding | Receptors, Dopamine D4 - metabolism | Neurons - metabolism | Proteasome Endopeptidase Complex - metabolism | Receptors, Dopamine D4 - physiology | Protein Synthesis and Degradation
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10. Full Text 4-[18f]fluorophenylpiperazines by improved hartwig-buchwald n-arylation of 4-[18f]fluoroiodobenzene, formed via hypervalent λ3-Iodane precursors: Application to build-up of the dopamine d4 ligand [18f]fauc 316
by Kügler, Fabian and Ermert, Johannes and Kaufholz, Peter and Coenen, Heinz H
Molecules, ISSN 1420-3049, 01/2015, Volume 20, Issue 1, pp. 470 - 486
Substituted phenylpiperazines are often neuropharmacologically active compounds and in many cases are essential pharmacophores of neuroligands for different... 
Iodonium ylides | Iodophenyl-iodonium compounds | Fluorine-18 | Hartwig-Buchwald n-arylation | Dopamine d4 radioligand | Magnetic Resonance Spectroscopy | Rats, Wistar | Receptors, Dopamine D4 - chemistry | Solvents - chemistry | Dimethyl Sulfoxide - chemistry | Rats | Piperazines - chemistry | Animals | Spectrometry, Mass, Electrospray Ionization | Female | Ligands | Benzene Derivatives - chemistry | Fluorine Radioisotopes - chemistry | Indoles - chemistry | Palladium - chemistry | Dimethylformamide - chemistry | Hartwig-Buchwald N-arylation | fluorine-18 | iodonium ylides | iodophenyl-iodonium compounds | dopamine D4 radioligand
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11. Full Text Discovery, characterization and biological evaluation of a novel (R)-4,4-difluoropiperidine scaffold as dopamine receptor 4 (D4R) antagonists
by Jeffries, Daniel E and Witt, Jonathan O and McCollum, Andrea L and Temple, Kayla J and Hurtado, Miguel A and Harp, Joel M and Blobaum, Anna L and Lindsley, Craig W and Hopkins, Corey R
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 12/2016, Volume 26, Issue 23, pp. 5757 - 5764
Herein, we report the synthesis and structure–activity relationship of a novel series of ( )-4,4-difluoropiperidine core scaffold as dopamine receptor 4 (D )... 
Selectivity | Difluoropiperidine | Addiction | PD-LIDs | Dopamine 4 receptor | SELECTIVE ANTAGONIST | CHEMISTRY, MEDICINAL | PROFILE | L-745,870 | CHEMISTRY, ORGANIC | INDUCED DYSKINESIA | Piperidines - chemistry | Receptors, Dopamine D4 - chemistry | Humans | Models, Molecular | Rats | Crystallography, X-Ray | Receptors, Dopamine D4 - antagonists & inhibitors | Antipsychotic Agents - pharmacokinetics | Drug Discovery | Isomerism | Antipsychotic Agents - chemical synthesis | Animals | Antipsychotic Agents - chemistry | Piperidines - pharmacology | Dopamine Antagonists - pharmacology | Halogenation | Piperidines - pharmacokinetics | Receptors, Dopamine D4 - metabolism | Antipsychotic Agents - pharmacology | Dopamine Antagonists - chemistry | Bisphenol-A | Analysis
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12. Full Text Click chemistry based synthesis of dopamine D4 selective receptor ligands for the selection of potential PET tracers
by Banerjee, Ashutosh and Maschauer, Simone and Hübner, Harald and Gmeiner, Peter and Prante, Olaf
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 11/2013, Volume 23, Issue 22, pp. 6079 - 6082
Taking advantage of click chemistry, a library of -arylpiperazinylmethyl triazoles bearing fluoro substituted appendages was synthesized and the target... 
Triazole | Dopamine | Click chemistry | D4 receptor | Fluorine | PET | D-4 RECEPTOR | SUBTYPE | PARTIAL AGONISTS | CHEMISTRY, MEDICINAL | RADIOLIGANDS | CHEMISTRY, ORGANIC | GLYCOSYLATION | POSITRON-EMISSION-TOMOGRAPHY | CELL-LINE | Hydrocarbons, Fluorinated - chemical synthesis | Alkynes - chemical synthesis | Receptors, Dopamine D4 - chemistry | Triazoles - chemistry | Humans | Click Chemistry - methods | Hydrocarbons, Fluorinated - chemistry | Alkynes - chemistry | Piperazines - chemistry | Structure-Activity Relationship | Positron-Emission Tomography - methods | Ligands | Piperazines - chemical synthesis | Receptors, Dopamine D4 - metabolism | Triazoles - chemical synthesis | Molecular Structure | Radioligand Assay
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13. Full Text Palmitoylation of the carboxyl-terminal tail of dopamine D-4 receptor is required for surface expression, endocytosis, and signaling
by Zhang, X and Kim, KM
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, ISSN 0006-291X, 10/2016, Volume 479, Issue 2, pp. 398 - 403
The amino acid sequences and signaling pathways of D2-like dopamine receptors (D2R, D3R, and D4R) are highly conserved. D4R has been suggested to be associated... 
POPULATION | Palmitoylation | PHOSPHORYLATION | BIOCHEMISTRY & MOLECULAR BIOLOGY | Surface expression | KINASE | PROTEIN-COUPLED RECEPTORS | HUMAN BETA-2-ADRENERGIC RECEPTOR | Signaling | Endocytosis | BIOPHYSICS | GENE | Dopamine D-4 receptor | NOVELTY SEEKING | RAT-BRAIN | CAVEOLAE | ASSOCIATION | Biotinylation | Lipoylation | Receptors, Dopamine D4 - chemistry | Signal Transduction | Humans | Receptors, Dopamine D3 - metabolism | Gene Expression Regulation | Cysteine - chemistry | Receptors, Dopamine D2 - metabolism | Plasmids - metabolism | Antipsychotic Agents - chemistry | HEK293 Cells | Palmitic Acids - chemistry | Protein Domains | Receptors, Dopamine D4 - metabolism | Cell Membrane - metabolism
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14. Full Text Structure and dynamics of DRD4 bound to an agonist and an antagonist using in silico approaches
by Jatana, Nidhi and Thukral, Lipi and Latha, N
Proteins: Structure, Function, and Bioinformatics, ISSN 0887-3585, 05/2015, Volume 83, Issue 5, pp. 867 - 880
ABSTRACT Human dopamine receptor D4 (DRD4), a member of G‐protein coupled receptor (GPCR) family, plays a central role in cell signaling and trafficking.... 
ligand binding; molecular dynamics simulations | GPCR | structure prediction | receptor activation mechanism | Structure prediction | Receptor activation mechanism | Ligand binding; molecular dynamics simulations | molecular dynamics simulations | SERINE RESIDUES | MOLECULAR-DYNAMICS | 3D STRUCTURE | BIOCHEMISTRY & MOLECULAR BIOLOGY | DOPAMINE D3 RECEPTOR | CONFORMATIONAL-CHANGES | BIOPHYSICS | HELIX GEOMETRY | BINDING-SITE | MEMBRANE-PROTEINS | ligand binding | PROTEIN-COUPLED-RECEPTOR | TRANSMEMBRANE SEGMENT | Dopamine - chemistry | Protein Structure, Tertiary | Protein Structure, Secondary | Receptors, Dopamine D4 - chemistry | Receptors, Dopamine D4 - agonists | Humans | Spiperone - chemistry | Receptors, Dopamine D4 - antagonists & inhibitors | Molecular Dynamics Simulation | Hydrogen Bonding | Protein Binding | Molecular Docking Simulation | Binding Sites | Dopamine Antagonists - chemistry | Dopamine Agonists - chemistry | Proteins | Nervous system diseases | Analysis | Proline | G proteins | Dopamine receptors | Protein binding
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15. Full Text Synthesis, pharmacological evaluation and molecular modeling studies of triazole containing dopamine D3 receptor ligands
by Peng, Xin and Wang, Qi and Mishra, Yogesh and Xu, Jinbin and Reichert, David E and Malik, Maninder and Taylor, Michelle and Luedtke, Robert R and Mach, Robert H
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 02/2015, Volume 25, Issue 3, pp. 519 - 523
A series of 2-methoxyphenyl piperazine analogues containing a triazole ring were synthesized and their in vitro binding affinities at human dopamine D and D... 
Dopamine D3 receptor selective ligands | Triazole | Molecular modeling | Dopamine receptors | Dopamine D | receptor selective ligands | Protein Structure, Tertiary | Dopamine Agonists - chemical synthesis | Receptors, Dopamine D4 - chemistry | Triazoles - chemistry | Humans | Receptors, Dopamine D2 - agonists | Receptors, Dopamine D3 - metabolism | Structure-Activity Relationship | Receptors, Dopamine D2 - metabolism | Molecular Dynamics Simulation | Receptors, Dopamine D2 - genetics | Receptors, Dopamine D3 - genetics | Receptors, Dopamine D3 - agonists | Triazoles - metabolism | Receptor, Serotonin, 5-HT1A - chemistry | HEK293 Cells | Protein Binding | Ligands | Receptors, Dopamine D4 - metabolism | Triazoles - chemical synthesis | Binding Sites | Dopamine Agonists - metabolism | Dopamine Agonists - chemistry | Receptor, Serotonin, 5-HT1A - metabolism | dopamine receptors | molecular modeling | dopamine D3 receptor selective ligands | triazole
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16. Full Text Variation at the DRD4 locus is associated with wariness and local site selection in urban black swans
by Van Dongen, Wouter F.D and Robinson, Randall W and Weston, Michael A and Mulder, Raoul A and Guay, Patrick-Jean
BMC Evolutionary Biology, ISSN 1471-2148, 12/2015, Volume 15, Issue 1, p. 253
Background: Interactions between wildlife and humans are increasing. Urban animals are often less wary of humans than their non-urban counterparts, which could... 
Urbanisation | SERT | Black swan | Habitat selection | Flight initiation distance | DRD4 | ANIMAL PERSONALITIES | EVOLUTIONARY TRAPS | TIT PARUS-MAJOR | SEROTONIN TRANSPORTER | GENE POLYMORPHISMS | FLIGHT-INITIATION DISTANCES | EVOLUTIONARY BIOLOGY | BEHAVIORAL SYNDROMES | GENETICS & HEREDITY | MICROSATELLITE MARKERS | CYGNUS-ATRATUS | Amino Acid Sequence | Avian Proteins - metabolism | Receptors, Dopamine D4 - chemistry | Molecular Sequence Data | Receptors, Dopamine D4 - genetics | Avian Proteins - chemistry | Polymorphism, Genetic | Sequence Alignment | Animals | Escape Reaction | Base Sequence | Receptors, Dopamine D4 - metabolism | Human Activities | Anseriformes - physiology | Anseriformes - genetics | Avian Proteins - genetics | Genetic aspects | Genes | Genetic polymorphisms | Dopamine receptors
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