Initial preclinical evaluation of 68 Ga-DOTA-(Ser) 3 -LTVSPWY peptide as a PET radiotracer for glioblastoma targeting and imaging
Copyright © 2022 Wolters Kluwer Health, Inc. All rights reserved..
PURPOSE: Imaging of glioblastoma multiform (GBM) tumor using 68 -Galium-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraaceticacid-Ser-Ser-Ser-Leu-Thr-Val-Ser-Pro-Trp-Tyr ( 68 Ga-DOTA-(Ser)3-LTVSPWY) as a PET radiotracer for HER2 receptor due to fact that this receptor plays a pivotal role in the tumorigenesis and tumor progression in a wide range of cancer.
METHODS: 68 Ga-DOTA-(Ser) 3 -LTVSPWY was produced with high radiochemical purity. The affinity and specificity of this radiotracer toward HER2 receptor on the surface of glioma glioblastoma (U-87 MG) cell line were evaluated. Furthermore, the biodistribution and PET imaging of this radiolabeled peptide were investigated on xenografted U-87 MG tumor-bearing mice.
RESULTS: The in-vitro specific binding study revealed that the 68 Ga-DOTA-(Ser) 3 -LTVSPWY binds to different cell lines with respect to their level of HER2 expression. The calculated K D and B max of radiolabeled peptide toward U-87 MG cell line were 5.5 ± 2.4 nmol/l and (2.4 ± 0.3) × 10 5 receptors per cell, respectively. The highest tumor uptake was observed at 30-min postinjection, whereas the tumor-to-muscle ratio was about four-fold. The acquired PET images distinctively show tumor site, which was blocked with excess nonlabeled peptide that revealed specific in-vivo targeting of 68 Ga-DOTA-(Ser) 3 -LTVSPWY for glioma.
CONCLUSION: 68 Ga-DOTA-(Ser) 3 -LTVSPWY specifically recognizes HER2 receptors and could be a potential candidate for GBM imaging.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2022 |
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| Erschienen: |
2022 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:43 |
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| Enthalten in: |
Nuclear medicine communications - 43(2022), 8 vom: 01. Aug., Seite 945-951 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Ranjbar, Venousheh [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 18.07.2022 Date Revised 17.09.2023 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1097/MNM.0000000000001590 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
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| 100 | 1 | |a Ranjbar, Venousheh |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a Initial preclinical evaluation of 68 Ga-DOTA-(Ser) 3 -LTVSPWY peptide as a PET radiotracer for glioblastoma targeting and imaging |
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| 500 | |a Date Revised 17.09.2023 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Copyright © 2022 Wolters Kluwer Health, Inc. All rights reserved. | ||
| 520 | |a PURPOSE: Imaging of glioblastoma multiform (GBM) tumor using 68 -Galium-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraaceticacid-Ser-Ser-Ser-Leu-Thr-Val-Ser-Pro-Trp-Tyr ( 68 Ga-DOTA-(Ser)3-LTVSPWY) as a PET radiotracer for HER2 receptor due to fact that this receptor plays a pivotal role in the tumorigenesis and tumor progression in a wide range of cancer | ||
| 520 | |a METHODS: 68 Ga-DOTA-(Ser) 3 -LTVSPWY was produced with high radiochemical purity. The affinity and specificity of this radiotracer toward HER2 receptor on the surface of glioma glioblastoma (U-87 MG) cell line were evaluated. Furthermore, the biodistribution and PET imaging of this radiolabeled peptide were investigated on xenografted U-87 MG tumor-bearing mice | ||
| 520 | |a RESULTS: The in-vitro specific binding study revealed that the 68 Ga-DOTA-(Ser) 3 -LTVSPWY binds to different cell lines with respect to their level of HER2 expression. The calculated K D and B max of radiolabeled peptide toward U-87 MG cell line were 5.5 ± 2.4 nmol/l and (2.4 ± 0.3) × 10 5 receptors per cell, respectively. The highest tumor uptake was observed at 30-min postinjection, whereas the tumor-to-muscle ratio was about four-fold. The acquired PET images distinctively show tumor site, which was blocked with excess nonlabeled peptide that revealed specific in-vivo targeting of 68 Ga-DOTA-(Ser) 3 -LTVSPWY for glioma | ||
| 520 | |a CONCLUSION: 68 Ga-DOTA-(Ser) 3 -LTVSPWY specifically recognizes HER2 receptors and could be a potential candidate for GBM imaging | ||
| 650 | 4 | |a Journal Article | |
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