1362550-90-0Relevant academic research and scientific papers
Comparison of 68Ga-labeled RGD mono- and multimers based on a clickable siderophore-based scaffold
Kaeopookum, Piriya,Petrik, Milos,Summer, Dominik,Klinger, Maximilian,Zhai, Chuangyan,Rangger, Christine,Haubner, Roland,Haas, Hubertus,Hajduch, Marian,Decristoforo, Clemens
, p. 1 - 10 (2019/11/03)
Cyclic pentapeptides containing the amino acid sequence arginine-glycine-aspartic (RGD) have been widely applied to target αvβ3 integrin, which is upregulated in various tumors during tumor-induced angiogenesis. Multimeric cyclic RGD peptides have been reported to be advantageous over monomeric counterparts for angiogenesis imaging. Here, we prepared mono-, di-, and trimeric cyclic arginine-glycine-aspartic-D-phenylalanine-lysine (c (RGDfK)) derivatives by conjugation with the natural chelator fusarinine C (FSC) using click chemistry based on copper (I)-catalyzed azide-alkyne cycloaddition (CuAAC). The αvβ3 binding properties of 68Ga-labeled mono-, di-, and trimeric c(RGDfK) peptides were evaluated in vitro as well as in vivo and compared with the references monomeric [68Ga]GaNODAGA-c(RGDfK) and trimeric [68Ga]GaFSC(suc-c(RGDfK))3. All 68Ga-labeled c(RGDfK) peptides displayed hydrophilicity (logD = ?2.96 to ?3.80), low protein binding and were stable in phosphate buffered-saline (PBS) and serum up to 2 h. In vitro internalization assays with human melanoma M21 (αvβ3-positive) and M21-L (αvβ3-negative) cell lines showed specific uptake of all derivatives and increased in the series: mono- 68Ga]GaMAFC(c(RGDfK)aza)2. In conclusion, we developed a novel strategy for direct, straight forward preparation of mono-, di-, and trimeric c(RGDfK) conjugates based on the FSC scaffold. Interestingly, the best αvβ3 imaging properties were found for the dimeric [68Ga]GaMAFC(c(RGDfK)aza)2.
TRIAZACYCLONONANE-BASED PHOSPHINATE LIGAND AND ITS USE FOR MOLECULAR IMAGING
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Page/Page column 20-21, (2012/07/28)
The present invention relates to the field of molecular imaging, i.e. nuclear and fluorescent imaging using metal ion radionuclides in combination with chelates highly functionalized with peptidic, nonpeptidic or protein ligands or additional signalling m
TRAP, a powerful and versatile framework for gallium-68 radiopharmaceuticals
Notni, Johannes,Simecek, Jakub,Hermann, Petr,Wester, Hans-Juergen
supporting information; experimental part, p. 14718 - 14722 (2012/02/06)
A veritable gallium TRAP: Triazacyclononane-phosphinic acid chelators (TRAP) form highly stable complexes with Ga3+ (see figure) extremely efficiently over a wide pH range. Homo- and heteromultimeric bioconjugates can be synthesized in a straig
