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Gastrin-releasing peptide receptor (GRP-R) (GRP-preferring bombesin receptor)

 GRPR_HUMAN              Reviewed;         384 AA.
P30550; B2R910;
01-APR-1993, integrated into UniProtKB/Swiss-Prot.
01-APR-1993, sequence version 1.
13-FEB-2019, entry version 162.
RecName: Full=Gastrin-releasing peptide receptor;
Short=GRP-R;
AltName: Full=GRP-preferring bombesin receptor;
Name=GRPR;
Homo sapiens (Human).
Eukaryota; Metazoa; Chordata; Craniata; Vertebrata; Euteleostomi;
Mammalia; Eutheria; Euarchontoglires; Primates; Haplorrhini;
Catarrhini; Hominidae; Homo.
NCBI_TaxID=9606;
[1]
NUCLEOTIDE SEQUENCE [MRNA], FUNCTION, AND SUBCELLULAR LOCATION.
TISSUE=Lung;
PubMed=1655761;
Corjay M.H., Dobrzanski D.J., Way J.M., Viallet J., Shapira H.,
Worland P., Sausville E.A., Battey J.F.;
"Two distinct bombesin receptor subtypes are expressed and functional
in human lung carcinoma cells.";
J. Biol. Chem. 266:18771-18779(1991).
[2]
NUCLEOTIDE SEQUENCE [GENOMIC DNA], AND TISSUE SPECIFICITY.
PubMed=11245983; DOI=10.1016/S0378-1119(00)00596-5;
Xiao D., Wang J., Hampton L.L., Weber H.C.;
"The human gastrin-releasing peptide receptor gene structure, its
tissue expression and promoter.";
Gene 264:95-103(2001).
[3]
NUCLEOTIDE SEQUENCE [LARGE SCALE MRNA].
TISSUE=Mammary gland;
PubMed=14702039; DOI=10.1038/ng1285;
Ota T., Suzuki Y., Nishikawa T., Otsuki T., Sugiyama T., Irie R.,
Wakamatsu A., Hayashi K., Sato H., Nagai K., Kimura K., Makita H.,
Sekine M., Obayashi M., Nishi T., Shibahara T., Tanaka T., Ishii S.,
Yamamoto J., Saito K., Kawai Y., Isono Y., Nakamura Y., Nagahari K.,
Murakami K., Yasuda T., Iwayanagi T., Wagatsuma M., Shiratori A.,
Sudo H., Hosoiri T., Kaku Y., Kodaira H., Kondo H., Sugawara M.,
Takahashi M., Kanda K., Yokoi T., Furuya T., Kikkawa E., Omura Y.,
Abe K., Kamihara K., Katsuta N., Sato K., Tanikawa M., Yamazaki M.,
Ninomiya K., Ishibashi T., Yamashita H., Murakawa K., Fujimori K.,
Tanai H., Kimata M., Watanabe M., Hiraoka S., Chiba Y., Ishida S.,
Ono Y., Takiguchi S., Watanabe S., Yosida M., Hotuta T., Kusano J.,
Kanehori K., Takahashi-Fujii A., Hara H., Tanase T.-O., Nomura Y.,
Togiya S., Komai F., Hara R., Takeuchi K., Arita M., Imose N.,
Musashino K., Yuuki H., Oshima A., Sasaki N., Aotsuka S.,
Yoshikawa Y., Matsunawa H., Ichihara T., Shiohata N., Sano S.,
Moriya S., Momiyama H., Satoh N., Takami S., Terashima Y., Suzuki O.,
Nakagawa S., Senoh A., Mizoguchi H., Goto Y., Shimizu F., Wakebe H.,
Hishigaki H., Watanabe T., Sugiyama A., Takemoto M., Kawakami B.,
Yamazaki M., Watanabe K., Kumagai A., Itakura S., Fukuzumi Y.,
Fujimori Y., Komiyama M., Tashiro H., Tanigami A., Fujiwara T.,
Ono T., Yamada K., Fujii Y., Ozaki K., Hirao M., Ohmori Y.,
Kawabata A., Hikiji T., Kobatake N., Inagaki H., Ikema Y., Okamoto S.,
Okitani R., Kawakami T., Noguchi S., Itoh T., Shigeta K., Senba T.,
Matsumura K., Nakajima Y., Mizuno T., Morinaga M., Sasaki M.,
Togashi T., Oyama M., Hata H., Watanabe M., Komatsu T.,
Mizushima-Sugano J., Satoh T., Shirai Y., Takahashi Y., Nakagawa K.,
Okumura K., Nagase T., Nomura N., Kikuchi H., Masuho Y., Yamashita R.,
Nakai K., Yada T., Nakamura Y., Ohara O., Isogai T., Sugano S.;
"Complete sequencing and characterization of 21,243 full-length human
cDNAs.";
Nat. Genet. 36:40-45(2004).
[4]
NUCLEOTIDE SEQUENCE [LARGE SCALE GENOMIC DNA].
Mural R.J., Istrail S., Sutton G.G., Florea L., Halpern A.L.,
Mobarry C.M., Lippert R., Walenz B., Shatkay H., Dew I., Miller J.R.,
Flanigan M.J., Edwards N.J., Bolanos R., Fasulo D., Halldorsson B.V.,
Hannenhalli S., Turner R., Yooseph S., Lu F., Nusskern D.R.,
Shue B.C., Zheng X.H., Zhong F., Delcher A.L., Huson D.H.,
Kravitz S.A., Mouchard L., Reinert K., Remington K.A., Clark A.G.,
Waterman M.S., Eichler E.E., Adams M.D., Hunkapiller M.W., Myers E.W.,
Venter J.C.;
Submitted (JUL-2005) to the EMBL/GenBank/DDBJ databases.
[5]
NUCLEOTIDE SEQUENCE [LARGE SCALE MRNA].
TISSUE=Brain;
PubMed=15489334; DOI=10.1101/gr.2596504;
The MGC Project Team;
"The status, quality, and expansion of the NIH full-length cDNA
project: the Mammalian Gene Collection (MGC).";
Genome Res. 14:2121-2127(2004).
-!- FUNCTION: Receptor for gastrin-releasing peptide (GRP)
(PubMed:1655761). Signals via association with G proteins that
activate a phosphatidylinositol-calcium second messenger system,
resulting in Akt phosphorylation. Contributes to the regulation of
food intake. Contributes to the perception of prurient stimuli and
transmission of itch signals in the spinal cord that promote
scratching behavior, but does not play a role in the perception of
pain. Contributes primarily to nonhistaminergic itch sensation.
Contributes to long-term fear memory, but not normal spatial
memory (By similarity). {ECO:0000250|UniProtKB:P21729,
ECO:0000269|PubMed:1655761}.
-!- SUBCELLULAR LOCATION: Cell membrane {ECO:0000269|PubMed:1655761};
Multi-pass membrane protein {ECO:0000255}.
-!- TISSUE SPECIFICITY: Highly expressed in pancreas. Also expressed
in stomach, adrenal cortex and brain.
{ECO:0000269|PubMed:11245983}.
-!- SIMILARITY: Belongs to the G-protein coupled receptor 1 family.
{ECO:0000255|PROSITE-ProRule:PRU00521}.
-----------------------------------------------------------------------
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EMBL; M73481; AAA88050.1; -; mRNA.
EMBL; AF293323; AAL96377.1; -; Genomic_DNA.
EMBL; AF293321; AAL96377.1; JOINED; Genomic_DNA.
EMBL; AF293322; AAL96377.1; JOINED; Genomic_DNA.
EMBL; AK313588; BAG36357.1; -; mRNA.
EMBL; CH471074; EAW98909.1; -; Genomic_DNA.
EMBL; BC074733; AAH74733.1; -; mRNA.
CCDS; CCDS14174.1; -.
PIR; A41007; A41007.
RefSeq; NP_005305.1; NM_005314.2.
UniGene; Hs.567282; -.
ProteinModelPortal; P30550; -.
SMR; P30550; -.
BioGrid; 109181; 63.
STRING; 9606.ENSP00000369643; -.
BindingDB; P30550; -.
ChEMBL; CHEMBL4959; -.
GuidetoPHARMACOLOGY; 39; -.
iPTMnet; P30550; -.
PhosphoSitePlus; P30550; -.
BioMuta; GRPR; -.
DMDM; 232185; -.
EPD; P30550; -.
PaxDb; P30550; -.
PeptideAtlas; P30550; -.
PRIDE; P30550; -.
ProteomicsDB; 54720; -.
Ensembl; ENST00000380289; ENSP00000369643; ENSG00000126010.
GeneID; 2925; -.
KEGG; hsa:2925; -.
CTD; 2925; -.
DisGeNET; 2925; -.
EuPathDB; HostDB:ENSG00000126010.5; -.
GeneCards; GRPR; -.
HGNC; HGNC:4609; GRPR.
HPA; HPA069604; -.
MIM; 305670; gene.
neXtProt; NX_P30550; -.
OpenTargets; ENSG00000126010; -.
PharmGKB; PA29002; -.
eggNOG; KOG3656; Eukaryota.
eggNOG; ENOG410XRW9; LUCA.
GeneTree; ENSGT00940000153205; -.
HOGENOM; HOG000230781; -.
HOVERGEN; HBG004898; -.
InParanoid; P30550; -.
KO; K04169; -.
OMA; NICHEGY; -.
OrthoDB; 1129049at2759; -.
PhylomeDB; P30550; -.
TreeFam; TF331292; -.
Reactome; R-HSA-375276; Peptide ligand-binding receptors.
Reactome; R-HSA-416476; G alpha (q) signalling events.
SIGNOR; P30550; -.
ChiTaRS; GRPR; human.
GeneWiki; Gastrin-releasing_peptide_receptor; -.
GenomeRNAi; 2925; -.
PRO; PR:P30550; -.
Proteomes; UP000005640; Chromosome X.
Bgee; ENSG00000126010; Expressed in 48 organ(s), highest expression level in body of pancreas.
ExpressionAtlas; P30550; baseline and differential.
Genevisible; P30550; HS.
GO; GO:0005887; C:integral component of plasma membrane; IMP:UniProtKB.
GO; GO:0005886; C:plasma membrane; IDA:HPA.
GO; GO:0008528; F:G protein-coupled peptide receptor activity; IDA:UniProtKB.
GO; GO:0004930; F:G protein-coupled receptor activity; IBA:GO_Central.
GO; GO:0042923; F:neuropeptide binding; IEA:Ensembl.
GO; GO:0008188; F:neuropeptide receptor activity; ISS:UniProtKB.
GO; GO:0008283; P:cell population proliferation; TAS:ProtInc.
GO; GO:0007186; P:G protein-coupled receptor signaling pathway; IBA:GO_Central.
GO; GO:0007611; P:learning or memory; IEA:Ensembl.
GO; GO:0061744; P:motor behavior; ISS:UniProtKB.
GO; GO:0007200; P:phospholipase C-activating G protein-coupled receptor signaling pathway; ISS:UniProtKB.
GO; GO:0036343; P:psychomotor behavior; IEA:Ensembl.
GO; GO:0042127; P:regulation of cell population proliferation; IEA:Ensembl.
GO; GO:0043207; P:response to external biotic stimulus; IEA:Ensembl.
GO; GO:0035176; P:social behavior; ISS:UniProtKB.
CDD; cd15124; 7tmA_GRPR; 1.
InterPro; IPR001556; Bombsn_rcpt-like.
InterPro; IPR001966; Gastrin_pep_rcpt.
InterPro; IPR000276; GPCR_Rhodpsn.
InterPro; IPR017452; GPCR_Rhodpsn_7TM.
Pfam; PF00001; 7tm_1; 1.
PRINTS; PR00358; BOMBESINR.
PRINTS; PR00640; GASTRINRELPR.
PRINTS; PR00237; GPCRRHODOPSN.
SMART; SM01381; 7TM_GPCR_Srsx; 1.
PROSITE; PS00237; G_PROTEIN_RECEP_F1_1; 1.
PROSITE; PS50262; G_PROTEIN_RECEP_F1_2; 1.
2: Evidence at transcript level;
Cell membrane; Complete proteome; Disulfide bond;
G-protein coupled receptor; Glycoprotein; Lipoprotein; Membrane;
Palmitate; Phosphoprotein; Receptor; Reference proteome; Transducer;
Transmembrane; Transmembrane helix.
CHAIN 1 384 Gastrin-releasing peptide receptor.
/FTId=PRO_0000069662.
TOPO_DOM 1 38 Extracellular. {ECO:0000255}.
TRANSMEM 39 62 Helical; Name=1. {ECO:0000255}.
TOPO_DOM 63 76 Cytoplasmic. {ECO:0000255}.
TRANSMEM 77 96 Helical; Name=2. {ECO:0000255}.
TOPO_DOM 97 114 Extracellular. {ECO:0000255}.
TRANSMEM 115 136 Helical; Name=3. {ECO:0000255}.
TOPO_DOM 137 152 Cytoplasmic. {ECO:0000255}.
TRANSMEM 153 174 Helical; Name=4. {ECO:0000255}.
TOPO_DOM 175 208 Extracellular. {ECO:0000255}.
TRANSMEM 209 234 Helical; Name=5. {ECO:0000255}.
TOPO_DOM 235 264 Cytoplasmic. {ECO:0000255}.
TRANSMEM 265 285 Helical; Name=6. {ECO:0000255}.
TOPO_DOM 286 298 Extracellular. {ECO:0000255}.
TRANSMEM 299 325 Helical; Name=7. {ECO:0000255}.
TOPO_DOM 326 384 Cytoplasmic. {ECO:0000255}.
MOD_RES 350 350 Phosphoserine.
{ECO:0000250|UniProtKB:O54799}.
LIPID 339 339 S-palmitoyl cysteine. {ECO:0000250}.
CARBOHYD 20 20 N-linked (GlcNAc...) asparagine.
{ECO:0000255}.
DISULFID 113 196 {ECO:0000255|PROSITE-ProRule:PRU00521}.
SEQUENCE 384 AA; 43199 MW; 70A75F11D9C82F19 CRC64;
MALNDCFLLN LEVDHFMHCN ISSHSADLPV NDDWSHPGIL YVIPAVYGVI ILIGLIGNIT
LIKIFCTVKS MRNVPNLFIS SLALGDLLLL ITCAPVDASR YLADRWLFGR IGCKLIPFIQ
LTSVGVSVFT LTALSADRYK AIVRPMDIQA SHALMKICLK AAFIWIISML LAIPEAVFSD
LHPFHEESTN QTFISCAPYP HSNELHPKIH SMASFLVFYV IPLSIISVYY YFIAKNLIQS
AYNLPVEGNI HVKKQIESRK RLAKTVLVFV GLFAFCWLPN HVIYLYRSYH YSEVDTSMLH
FVTSICARLL AFTNSCVNPF ALYLLSKSFR KQFNTQLLCC QPGLIIRSHS TGRSTTCMTS
LKSTNPSVAT FSLINGNICH ERYV


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Pathways :
WP2355: Corticotropin-releasing hormone
WP1004: Kit Receptor Signaling Pathway
WP1011: T Cell Receptor Signaling Pathway
WP1014: Androgen receptor signaling pathway
WP1025: B Cell Receptor Signaling Pathway
WP1045: TGF-beta Receptor Signaling Pathway
WP1046: Signaling of Hepatocyte Growth Factor Receptor
WP1067: Toll-like receptor signaling pathway
WP1112: EPO Receptor Signaling
WP1121: Kit Receptor Signaling Pathway
WP1130: T Cell Receptor Signaling Pathway
WP1133: Androgen receptor signaling pathway
WP1144: B Cell Receptor Signaling Pathway
WP1161: TGF-beta Receptor Signaling Pathway
WP1162: Signaling of Hepatocyte Growth Factor Receptor
WP1183: Toll-like receptor signaling pathway
WP1206: Signaling of Hepatocyte Growth Factor Receptor
WP1235: Signaling of Hepatocyte Growth Factor Receptor
WP1249: EPO Receptor Signaling
WP1271: Toll-like receptor signaling pathway
WP1284: EPO Receptor Signaling
WP1309: Toll-like receptor signaling pathway
WP1336: EPO Receptor Signaling
WP1341: Kit Receptor Signaling Pathway
WP1345: T Cell Receptor Signaling Pathway

Related Genes :
[Grpr] Gastrin-releasing peptide receptor (GRP-R) (GRP-preferring bombesin receptor)
[Grpr] Gastrin-releasing peptide receptor (GRP-R) (GRP-preferring bombesin receptor)
[GRPR] Gastrin-releasing peptide receptor (GRP-R) (GRP-preferring bombesin receptor)
[CCKBR CCKRB] Gastrin/cholecystokinin type B receptor (CCK-B receptor) (CCK-BR) (Cholecystokinin-2 receptor) (CCK2-R)
[HSPA5 GRP78] Endoplasmic reticulum chaperone BiP (EC 3.6.4.10) (78 kDa glucose-regulated protein) (GRP-78) (Binding-immunoglobulin protein) (BiP) (Heat shock protein 70 family protein 5) (HSP70 family protein 5) (Heat shock protein family A member 5) (Immunoglobulin heavy chain-binding protein)
[CRHR1 CRFR CRFR1 CRHR] Corticotropin-releasing factor receptor 1 (CRF-R-1) (CRF-R1) (CRFR-1) (Corticotropin-releasing hormone receptor 1) (CRH-R-1) (CRH-R1)
[GHSR] Growth hormone secretagogue receptor type 1 (GHS-R) (GH-releasing peptide receptor) (GHRP) (Ghrelin receptor)
[Ghsr] Growth hormone secretagogue receptor type 1 (GHS-R) (GH-releasing peptide receptor) (GHRP) (Ghrelin receptor)
[Crhr1 Crhr] Corticotropin-releasing factor receptor 1 (CRF-R-1) (CRF-R1) (CRFR-1) (Corticotropin-releasing hormone receptor 1) (CRH-R-1) (CRH-R1)
[HSP90B1 GRP94 TRA1] Endoplasmin (94 kDa glucose-regulated protein) (GRP-94) (Heat shock protein 90 kDa beta member 1) (Tumor rejection antigen 1) (gp96 homolog)
[Crhr1 Crhr] Corticotropin-releasing factor receptor 1 (CRF-R-1) (CRF-R1) (CRFR-1) (Corticotropin-releasing hormone receptor 1) (CRH-R-1) (CRH-R1)
[Ghsr] Growth hormone secretagogue receptor type 1 (GHS-R) (GH-releasing peptide receptor) (GHRP) (Ghrelin receptor)
[Hspa5 Grp78] Endoplasmic reticulum chaperone BiP (EC 3.6.4.10) (78 kDa glucose-regulated protein) (GRP-78) (Binding-immunoglobulin protein) (BiP) (Heat shock protein 70 family protein 5) (HSP70 family protein 5) (Heat shock protein family A member 5) (Immunoglobulin heavy chain-binding protein)
[Hspa5 Grp78] Endoplasmic reticulum chaperone BiP (EC 3.6.4.10) (78 kDa glucose-regulated protein) (GRP-78) (Binding-immunoglobulin protein) (BiP) (Heat shock protein 70 family protein 5) (HSP70 family protein 5) (Heat shock protein family A member 5) (Immunoglobulin heavy chain-binding protein) (Steroidogenesis-activator polypeptide)
[GHSR] Growth hormone secretagogue receptor type 1 (GHS-R) (GH-releasing peptide receptor) (GHRP) (Ghrelin receptor)
[Hspa9 Grp75 Hspa9a] Stress-70 protein, mitochondrial (75 kDa glucose-regulated protein) (GRP-75) (Heat shock 70 kDa protein 9) (Mortalin) (Peptide-binding protein 74) (PBP74) (mtHSP70)
[Hsp90b1 Grp94 Tra-1 Tra1] Endoplasmin (94 kDa glucose-regulated protein) (GRP-94) (Endoplasmic reticulum resident protein 99) (ERp99) (Heat shock protein 90 kDa beta member 1) (Polymorphic tumor rejection antigen 1) (Tumor rejection antigen gp96)
[HSPA9 GRP75 HSPA9B mt-HSP70] Stress-70 protein, mitochondrial (75 kDa glucose-regulated protein) (GRP-75) (Heat shock 70 kDa protein 9) (Mortalin) (MOT) (Peptide-binding protein 74) (PBP74)
[Hspa9 Grp75 Hsp74 Hspa9a] Stress-70 protein, mitochondrial (75 kDa glucose-regulated protein) (GRP-75) (Heat shock 70 kDa protein 9) (Mortalin) (Peptide-binding protein 74) (PBP74) (p66 MOT)
[HSPA5 GRP78] Endoplasmic reticulum chaperone BiP (EC 3.6.4.10) (78 kDa glucose-regulated protein) (GRP-78) (Binding-immunoglobulin protein) (BiP) (Heat shock protein 70 family protein 5) (HSP70 family protein 5) (Heat shock protein family A member 5) (Immunoglobulin heavy chain-binding protein)
[grp CG17161] Serine/threonine-protein kinase grp (EC 2.7.11.1) (Chk1 homolog) (Protein grapes)
[HSPA5 GRP78] Endoplasmic reticulum chaperone BiP (EC 3.6.4.10) (78 kDa glucose-regulated protein) (GRP-78) (Binding-immunoglobulin protein) (BiP) (Heat shock protein 70 family protein 5) (HSP70 family protein 5) (Heat shock protein family A member 5) (Immunoglobulin heavy chain-binding protein)
[GNRHR GRHR] Gonadotropin-releasing hormone receptor (GnRH receptor) (GnRH-R)
[GRP3 At2g05520 T20G20.13] Glycine-rich protein 3 (AtGRP-3)
[Fpr-s1 Fpr2 Fpr3 Fprl1 Lxa4r] Formyl peptide receptor-related sequence 1 (FMLP-related receptor I) (FMLP-R-I) (Formyl peptide receptor related sequence 1) (Formyl peptide receptor-like 1) (Lipoxin A4 receptor) (LXA4 receptor) (N-formyl peptide receptor 2) (N-formyl peptide receptor 3)
[KISS1R AXOR12 GPR54] KiSS-1 receptor (KiSS-1R) (G-protein coupled receptor 54) (G-protein coupled receptor OT7T175) (hOT7T175) (Hypogonadotropin-1) (Kisspeptins receptor) (Metastin receptor)
[CALR CRTC] Calreticulin (CRP55) (Calregulin) (Endoplasmic reticulum resident protein 60) (ERp60) (HACBP) (grp60)
[IFNLR1 IL28RA LICR2] Interferon lambda receptor 1 (IFN-lambda receptor 1) (IFN-lambda-R1) (Cytokine receptor class-II member 12) (Cytokine receptor family 2 member 12) (CRF2-12) (Interleukin-28 receptor subunit alpha) (IL-28 receptor subunit alpha) (IL-28R-alpha) (IL-28RA) (Likely interleukin or cytokine receptor 2) (LICR2)
[Kiss1r Gpr54] KiSS-1 receptor (KiSS-1R) (G-protein coupled receptor 54) (G-protein coupled receptor OT7T175) (mOT7T175) (Kisspeptins receptor) (Metastin receptor)
[HSP90B1 GRP94 TRA1] Endoplasmin (94 kDa glucose-regulated protein) (GRP-94) (Heat shock protein 90 kDa beta member 1)

Bibliography :
[30897789] Localization of Tc-GRP Analogs in GRPR-Expressing Tumors: Effects of Peptide Length and Neprilysin Inhibition on Biological Responses.
[30887136] HYNIC and DOMA conjugated radiolabeled bombesin analogs as receptor-targeted probes for scintigraphic detection of breast tumor.
[30840614] Constitutively active BRS3 is a genuinely orphan GPCR in placental mammals.
[30825867] Ions-free electrochemically synthetized in aqueous media flake-like CuO nanostructures as SERS reproducible substrates for the detection of neurotransmitters.
[30763290] Synthesis and preclinical evaluation of the 177Lu-DOTA-PSMA(inhibitor)-Lys3-bombesin heterodimer designed as a radiotheranostic probe for prostate cancer.
[30569349] Easy formulation of liposomal doxorubicin modified with a bombesin peptide analogue for selective targeting of GRP receptors overexpressed by cancer cells.
[30299570] Tumor targeting with Tc radiolabeled peptides: Clinical application and recent development.
[30278325] Single vial cold kits optimized for preparation of gastrin releasing peptide receptor (GRPR)-radioantagonist Ga-RM2 using three different Ge/Ga generators.
[30151920] Gastrin-Releasing Peptide Is Involved in the Establishment of Allergic Rhinitis in Mice.
[30036253] 68Ga-NOTA-RM26 PET/CT in the Evaluation of Breast Cancer: A Pilot Prospective Study.
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