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| Description
| - Introduction: Ga-68-labeled RGD peptides in combination with PET allow non-invasive determination of alpha(v)beta(3) integrin expression which is highly increased during tumor-induced angiogenesis. The aim of this study was to synthesize and evaluate two RGD peptides containing alternative chelating systems, namely [Ga-68]NS3-RGD and [Ga-68]Oxo-DO3A-RGD and to compare their in vitro and in vivo properties with [Ga-68]DOTA- and [Ga-68]NODAGA-RGD. Methods: Syntheses of both radiotracers followed standard SPPS protocols. For in vitro characterization distribution coefficients, protein binding abilities, serum stablities, and alpha(v)beta(3) integrin binding affinities were determined. For in vitro tests as well as for the biodistribution assay alpha(v)beta(3) positive human melanoma M21 and alpha(v)beta(3) negative M21-L cells were used. Results: Ga-68-labeling of NS3-RGD resulted in good radiochemical purity, whereas HPLC analysis showed two peaks with a ratio of 1:6 for [Ga-68]Oxo-DO3A-RGD. Distribution coefficients were -3.4 for [Ga-68]Oxo-DO3A-RGD and -2.9 for [Ga-68]NS3-RGD. Both radiotracers were stable in PBS solution at 37 degrees C for 2h but lack stability in human serum. Protein binding was approximately 40% of the total activity for [Ga-68]NS3-RGD and 70% for [Ga-68]Oxo-DO3A-RGD, respectively, resulting in high blood pool activities. Biodistribution assays confirmed these findings and showed an additional high uptake in liver and kidneys, especially for (Ga-68]NS3-RGD. Furthermore, [Ga-68]Oxo-DO3A-RGD showed nearly the same activity concentrations in alpha(v)beta(3) positive and alpha(v)beta(3) negative tumors. Conclusions: [Ga-68]Oxo-DO3A-RGD and [Ga-68]NS3-RGD have inferior characteristics compared to already existing Ga-68-labeled RGD peptides and thus, both are not suited to image alpha(v)beta(3) integrin expression. Of all our tested RGD peptides, [Ga-68]NODAGA-RGD still possesses the most favorable imaging properties...
- Introduction: Ga-68-labeled RGD peptides in combination with PET allow non-invasive determination of alpha(v)beta(3) integrin expression which is highly increased during tumor-induced angiogenesis. The aim of this study was to synthesize and evaluate two RGD peptides containing alternative chelating systems, namely [Ga-68]NS3-RGD and [Ga-68]Oxo-DO3A-RGD and to compare their in vitro and in vivo properties with [Ga-68]DOTA- and [Ga-68]NODAGA-RGD. Methods: Syntheses of both radiotracers followed standard SPPS protocols. For in vitro characterization distribution coefficients, protein binding abilities, serum stablities, and alpha(v)beta(3) integrin binding affinities were determined. For in vitro tests as well as for the biodistribution assay alpha(v)beta(3) positive human melanoma M21 and alpha(v)beta(3) negative M21-L cells were used. Results: Ga-68-labeling of NS3-RGD resulted in good radiochemical purity, whereas HPLC analysis showed two peaks with a ratio of 1:6 for [Ga-68]Oxo-DO3A-RGD. Distribution coefficients were -3.4 for [Ga-68]Oxo-DO3A-RGD and -2.9 for [Ga-68]NS3-RGD. Both radiotracers were stable in PBS solution at 37 degrees C for 2h but lack stability in human serum. Protein binding was approximately 40% of the total activity for [Ga-68]NS3-RGD and 70% for [Ga-68]Oxo-DO3A-RGD, respectively, resulting in high blood pool activities. Biodistribution assays confirmed these findings and showed an additional high uptake in liver and kidneys, especially for (Ga-68]NS3-RGD. Furthermore, [Ga-68]Oxo-DO3A-RGD showed nearly the same activity concentrations in alpha(v)beta(3) positive and alpha(v)beta(3) negative tumors. Conclusions: [Ga-68]Oxo-DO3A-RGD and [Ga-68]NS3-RGD have inferior characteristics compared to already existing Ga-68-labeled RGD peptides and thus, both are not suited to image alpha(v)beta(3) integrin expression. Of all our tested RGD peptides, [Ga-68]NODAGA-RGD still possesses the most favorable imaging properties... (en)
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| Title
| - [(68)Ga]NS(3)-RGD and [(68)Ga] Oxo-DO3A-RGD for imaging alfa(v)beta(3) integrin expression: synthesis, evaluation, and comparison
- [(68)Ga]NS(3)-RGD and [(68)Ga] Oxo-DO3A-RGD for imaging alfa(v)beta(3) integrin expression: synthesis, evaluation, and comparison (en)
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| skos:prefLabel
| - [(68)Ga]NS(3)-RGD and [(68)Ga] Oxo-DO3A-RGD for imaging alfa(v)beta(3) integrin expression: synthesis, evaluation, and comparison
- [(68)Ga]NS(3)-RGD and [(68)Ga] Oxo-DO3A-RGD for imaging alfa(v)beta(3) integrin expression: synthesis, evaluation, and comparison (en)
|
| skos:notation
| - RIV/61989592:15110/13:33145217!RIV14-MSM-15110___
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| http://linked.open...avai/predkladatel
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| http://linked.open...avai/riv/aktivita
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| http://linked.open...avai/riv/aktivity
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| http://linked.open...iv/cisloPeriodika
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| http://linked.open...vai/riv/dodaniDat
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| http://linked.open...aciTvurceVysledku
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| http://linked.open.../riv/druhVysledku
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| http://linked.open...iv/duvernostUdaju
| |
| http://linked.open...titaPredkladatele
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| http://linked.open...dnocenehoVysledku
| |
| http://linked.open...ai/riv/idVysledku
| - RIV/61989592:15110/13:33145217
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| http://linked.open...riv/jazykVysledku
| |
| http://linked.open.../riv/klicovaSlova
| - Angiogenesis; Molecular imaging; alpha(v)beta(3); RGD; Ga-68 (en)
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| http://linked.open.../riv/klicoveSlovo
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| http://linked.open...odStatuVydavatele
| - US - Spojené státy americké
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| http://linked.open...ontrolniKodProRIV
| |
| http://linked.open...i/riv/nazevZdroje
| - Nuclear Medicine and Biology
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| http://linked.open...in/vavai/riv/obor
| |
| http://linked.open...ichTvurcuVysledku
| |
| http://linked.open...cetTvurcuVysledku
| |
| http://linked.open...vavai/riv/projekt
| |
| http://linked.open...UplatneniVysledku
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| http://linked.open...v/svazekPeriodika
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| http://linked.open...iv/tvurceVysledku
| - Decristoforo, Clemens
- Petřík, Miloš
- Haubner, Roland
- Knetsch, Peter A.
- Pietzsch, Hans-Jürgen
- Rangger, Christine
- Seidel, Gesine
- Virgolini, Irene
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| http://linked.open...ain/vavai/riv/wos
| |
| issn
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| number of pages
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| http://bibframe.org/vocab/doi
| - 10.1016/j.nucmedbio.2012.09.006
|
| http://localhost/t...ganizacniJednotka
| |
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