S-Space College of Medicine/School of Medicine (의과대학/대학원) Nuclear Medicine (핵의학전공) Journal Papers (저널논문_핵의학전공)
Tumor imaging with (68)Ga-positron emission tomography: synthesis and characterization of macrocycle-amino acid derivatives
- Shetty, Dinesh; Jeong, Jae Min; Ju, Chang Hwan; Lee, Yun-Sang; Chung, June-Key; Lee, Myung Chul; Lee, Doug Soo
- Issue Date
- ELSEVIER SCIENCE INC
- NUCLEAR MEDICINE AND BIOLOGY; Vol.37 6; 688-689
- 68Ga positron emission tomography (PET) imaging in clinical oncology is a
noted development due to cyclotron independent availability. Labeled
amino acid derivatives have been proved useful in imaging many kinds of
tumors. We synthesized 3-aminoalanine, 4-aminohomoalanine and lysine
derivatives of macrocyclic chelating agents by conjugating amino acids to
mono carboxylic group of NOTA and DOTA using either EDC or DCC.
Pure compounds were labeled with 68Ga (labeling efficiency N95%, Specific
Activity ~ 1.94-9.21 GBq/μmol). The preliminary evaluation was studied in
Hep3B and CT-26 cancer cells, which showed high uptake of these
derivatives. Highest in vivo tumor uptake was showed by 68Ga-NOTAaminohomoalanine
(2.40±0.85% ID/g) at 30 min. PET images in mice bearing CT-26 xenografts showed high tumor uptake for 68Ga-NOTAaminohomoalanine
(standard uptake value ratio=12.3±0.05), followed by
68Ga-DOTA-aminoalanine (5.9±0.4). The co-ordination chemistry of
NOTA-mono amide compound was studied by multinuclear nuclear
magnetic resonance analysis. These studies showed the feasibility of using
68Ga amino acid PET for tumor diagnosis.
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