Micro-PET Imaging of αβ-Integrin Expression with F-Labeled Dimeric RGD Peptide
The α v integrins, which act as cell adhesion molecules, are closely involved with tumor invasion and angiogenesis. In particular, α v β 3 integrin, which is specifically expressed on proliferating endothelial cells and tumor cells, is a logical target for development of a radiotracer method to asse...
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| Format: | Article |
| Language: | English |
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SAGE Publishing
2004-04-01
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| Series: | Molecular Imaging |
| Online Access: | https://doi.org/10.1162/15353500200404109 |
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| _version_ | 1832544563141541888 |
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| author | Xiaoyuan Chen Michel Tohme Ryan Park Yingping Hou James R. Bading Peter S. Conti |
| author_facet | Xiaoyuan Chen Michel Tohme Ryan Park Yingping Hou James R. Bading Peter S. Conti |
| author_sort | Xiaoyuan Chen |
| collection | DOAJ |
| description | The α v integrins, which act as cell adhesion molecules, are closely involved with tumor invasion and angiogenesis. In particular, α v β 3 integrin, which is specifically expressed on proliferating endothelial cells and tumor cells, is a logical target for development of a radiotracer method to assess angiogenesis and anti-angiogenic therapy. In this study, a dimeric cyclic RGD peptide E[c(RGDyK)] 2 was labeled with 18 F ( t 1 /2 = 109.7 min) by using a prosthetic 4-[ 18 F]fluorobenzoyl moiety to the amino group of the glutamate. The resulting [ 18 F]FB-E[c(RGDyK)] 2 , with high specific activity (200–250 GBq/μmol at the end of synthesis), was administered to subcutaneous U87MG glioblastoma xenograft models for micro-PET and autoradiographic imaging as well as direct tissue sampling to assess tumor targeting efficacy and in vivo kinetics of this PET tracer. The dimeric RGD peptide demonstrated significantly higher tumor uptake and prolonged tumor retention in comparison with a monomeric RGD peptide analog [ 18 F]FB-c(RGDyK). The dimeric RGD peptide had predominant renal excretion, whereas the monomeric analog was excreted primarily through the biliary route. Micro-PET imaging 1 hr after injection of the dimeric RGD peptide exhibited tumor to contralateral background ratio of 9.5 ± 0.8. The synergistic effect of polyvalency and improved pharmacokinetics may be responsible for the superior imaging characteristics of [ 18 F]FB-E[c(RGDyK)] 2 . |
| format | Article |
| id | doaj-art-9db334e23ff745d8a242f188f9dbea47 |
| institution | Kabale University |
| issn | 1536-0121 |
| language | English |
| publishDate | 2004-04-01 |
| publisher | SAGE Publishing |
| record_format | Article |
| series | Molecular Imaging |
| spelling | doaj-art-9db334e23ff745d8a242f188f9dbea472025-02-03T10:08:13ZengSAGE PublishingMolecular Imaging1536-01212004-04-01310.1162/1535350020040410910.1162_15353500200404109Micro-PET Imaging of αβ-Integrin Expression with F-Labeled Dimeric RGD PeptideXiaoyuan ChenMichel TohmeRyan ParkYingping HouJames R. BadingPeter S. ContiThe α v integrins, which act as cell adhesion molecules, are closely involved with tumor invasion and angiogenesis. In particular, α v β 3 integrin, which is specifically expressed on proliferating endothelial cells and tumor cells, is a logical target for development of a radiotracer method to assess angiogenesis and anti-angiogenic therapy. In this study, a dimeric cyclic RGD peptide E[c(RGDyK)] 2 was labeled with 18 F ( t 1 /2 = 109.7 min) by using a prosthetic 4-[ 18 F]fluorobenzoyl moiety to the amino group of the glutamate. The resulting [ 18 F]FB-E[c(RGDyK)] 2 , with high specific activity (200–250 GBq/μmol at the end of synthesis), was administered to subcutaneous U87MG glioblastoma xenograft models for micro-PET and autoradiographic imaging as well as direct tissue sampling to assess tumor targeting efficacy and in vivo kinetics of this PET tracer. The dimeric RGD peptide demonstrated significantly higher tumor uptake and prolonged tumor retention in comparison with a monomeric RGD peptide analog [ 18 F]FB-c(RGDyK). The dimeric RGD peptide had predominant renal excretion, whereas the monomeric analog was excreted primarily through the biliary route. Micro-PET imaging 1 hr after injection of the dimeric RGD peptide exhibited tumor to contralateral background ratio of 9.5 ± 0.8. The synergistic effect of polyvalency and improved pharmacokinetics may be responsible for the superior imaging characteristics of [ 18 F]FB-E[c(RGDyK)] 2 .https://doi.org/10.1162/15353500200404109 |
| spellingShingle | Xiaoyuan Chen Michel Tohme Ryan Park Yingping Hou James R. Bading Peter S. Conti Micro-PET Imaging of αβ-Integrin Expression with F-Labeled Dimeric RGD Peptide Molecular Imaging |
| title | Micro-PET Imaging of αβ-Integrin Expression with F-Labeled Dimeric RGD Peptide |
| title_full | Micro-PET Imaging of αβ-Integrin Expression with F-Labeled Dimeric RGD Peptide |
| title_fullStr | Micro-PET Imaging of αβ-Integrin Expression with F-Labeled Dimeric RGD Peptide |
| title_full_unstemmed | Micro-PET Imaging of αβ-Integrin Expression with F-Labeled Dimeric RGD Peptide |
| title_short | Micro-PET Imaging of αβ-Integrin Expression with F-Labeled Dimeric RGD Peptide |
| title_sort | micro pet imaging of αβ integrin expression with f labeled dimeric rgd peptide |
| url | https://doi.org/10.1162/15353500200404109 |
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