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| 001 | 834113 | ||
| 005 | 20210129230542.0 | ||
| 024 | 7 | _ | |a 10.18632/oncotarget.15437 |2 doi |
| 024 | 7 | _ | |a WOS:000396877500053 |2 WOS |
| 037 | _ | _ | |a FZJ-2017-04114 |
| 041 | _ | _ | |a English |
| 082 | _ | _ | |a 610 |
| 100 | 1 | _ | |a Morgenroth, Agnieszka |0 P:(DE-HGF)0 |b 0 |e Corresponding author |
| 245 | _ | _ | |a Radioiodinated indomethacin amide for molecular imaging of cyclooxygenase-2 expressing tumorsinm-5 |
| 260 | _ | _ | |a [S.l.] |c 2017 |b Impact Journals LLC |
| 336 | 7 | _ | |a article |2 DRIVER |
| 336 | 7 | _ | |a Output Types/Journal article |2 DataCite |
| 336 | 7 | _ | |a Journal Article |b journal |m journal |0 PUB:(DE-HGF)16 |s 1501140895_26322 |2 PUB:(DE-HGF) |
| 336 | 7 | _ | |a ARTICLE |2 BibTeX |
| 336 | 7 | _ | |a JOURNAL_ARTICLE |2 ORCID |
| 336 | 7 | _ | |a Journal Article |0 0 |2 EndNote |
| 520 | _ | _ | |a Cyclooxygenase-2 (COX-2) is an important biomarker in several tumors. Available imaging probes display relatively low tumor to background ratios (smaller than 2:1). We evaluated newly developed indomethacin (Ind) derivatives for in vivo molecular imaging of COX-2 expressing carcinoma. Radioiodinated Ind derivatives Ind-NH-(CH2)4-NH-3-[I-125]I-Bz ([I-125]5), Ind-NH-(CH2)4-NH-5-[I-124/125]I-Nic ([I-124/125]6) and Ind-NH-(CH2)4-NH-5-[I-125]I-Iphth ([I-125]7) were prepared from the respective SnBu3-precursors (45–80% radiochemical yield; > 95% radiochemical purity). The cellular uptake of [I-125]5 and [I-125]6 correlated with COX-2 expression determined by SDS page/Western blot analysis. [I-125]5 was predominantly localized in the cell membrane while [I-125]6 was internalized and displayed a diffuse and favorable cytoplasmic distribution. In contrast, [I-125]7 showed only low uptake in COX-2 positive cells. Co-incubation with the COX-2 inhibitor Celecoxib led to an almost complete suppression of cellular uptake of [I-125]5 and [I-125]6. In vivo molecular imaging using positron emission tomography (PET) in SCID mice xenografted with COX-2+ (HT29) and COX-2− (HCT116) human colorectal carcinoma cells was performed for [I-124]6. HT29 xenografts displayed a significantly higher uptake than HCT-116 xenografts (5.6 ± 1.5 vs. 0.5 ± 0.1 kBq/g, P < 0.05) with an extraordinary high tumor to muscle ratio (50.3 ± 1.5). Immunohistological staining correlated with the imaging data. In conclusion, the novel radioiodinated indomethacin derivative ([I-124/125]6) could become a valuable tool for development of molecular imaging probes for visualization of COX-2 expressing tumors. |
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| 700 | 1 | _ | |a Vogg, Andreas T. J. |0 P:(DE-HGF)0 |b 1 |
| 700 | 1 | _ | |a Neumaier, Bernd |0 P:(DE-Juel1)166419 |b 2 |u fzj |
| 700 | 1 | _ | |a Mottaghy, Felix M. |0 P:(DE-Juel1)132318 |b 3 |u fzj |
| 700 | 1 | _ | |a Zlatopolskiy, Boris D. |0 P:(DE-HGF)0 |b 4 |
| 773 | _ | _ | |a 10.18632/oncotarget.15437 |0 PERI:(DE-600)2560162-3 |n 11 |p 18059-18069 |t OncoTarget |v 8 |y 2017 |x 1949-2553 |
| 856 | 4 | _ | |u https://juser.fz-juelich.de/record/834113/files/15437-227981-3-PB.pdf |y Restricted |
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