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      Chelators for 68Ga radiopharmaceuticals

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      https://www.riss.kr/link?id=A105944657

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      다국어 초록 (Multilingual Abstract)

      68Ga is a promising radionuclide for positron emission tomography (PET). It is a generator-produced (68Ge/68Ga-generator) radionuclide with a half-life of 68 min. The employment of 68Ga for basic research and clinical applications is growing exponenti...

      68Ga is a promising radionuclide for positron emission tomography (PET). It is a generator-produced (68Ge/68Ga-generator) radionuclide with a half-life of 68 min. The employment of 68Ga for basic research and clinical applications is growing exponentially. Bifunctional chelators (BFCs) that can be efficiently radiolabeled with 68Ga to yield complexes with good in vivo stability are needed. Given the practical advantages of 68Ga in PET applications, gallium complexes are gaining increasing attention in biomedical imaging. However, new 68Ga-labeled radiopharmaceuticals that can replace 18F-labeled agents like [18F]fluorodeoxyglucose (FDG) are needed. The majority of 68Ga-labeled derivatives currently in use consist of peptide agents, but the development of other agents, such as amino acid or nitroimidazole derivatives and glycosylated human serum albumin, is being actively pursued in many laboratories. Thus, the availability of new 68Ga-labeled radiopharmaceuticals with high impact is expected in the near future. Here, we present an overview of the different new classes of chelators for application in molecular imaging using 68Ga PET. J Radiopharm Mol Prob 2(1):22-36, 2016

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      참고문헌 (Reference)

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      1 Knetsch PA, "[68Ga]NS3-RGD and [68Ga] Oxo-DO3A-RGD for imaging αvβ3 integrin expression: synthesis, evaluation, and comparison" 40 : 65-72, 2013

      2 Motekaitis RJ, "The Gallium(III) and Indium(III) Complexes of Tris(2-mercaptobenzyl) amine and Tris(2-hydroxybenzyl)amine" 37 : 5902-5911, 1998

      3 Bartholomä MD, "Technetium and gallium derived radiopharmaceuticals: comparing and contrasting the chemistry of two important radiometals for the molecular imaging era" 110 : 2903-2920, 2010

      4 Notni J, "TRAP, a Powerful and Versatile Framework for Gallium‐68 Radiopharmaceuticals" 17 : 14718-14722, 2011

      5 Arslantas E, "TAME-Hex A - A Novel Bifunctional Chelating Agent for Radioimmunoimaging" 2004 : 3979-3984, 2004

      6 Behnam Azad B, "Synthesis, radiometal labeling and in vitro evaluation of a targeted PPIX derivative" 70 : 505-511, 2012

      7 Shetty D, "Synthesis of novel< sup> 68 Ga-labeled amino acid derivatives for positron emission tomography of cancer cells" 37 : 893-902, 2010

      8 Cai H, "Synthesis of a novel bifunctional chelator AmBaSar based on sarcophagine for peptide conjugation and 64Cu radiolabelling" (27) : 5395-6400, 2009

      9 Green MA, "Synthesis and crystallographic characterization of a gallium salicylaldimine complex of radiopharmaceutical interest" 106 : 3689-3691, 1984

      10 Guerra Gomez FL, "Synthesis and Evaluation of Diastereoisomers of 1, 4, 7-Triazacyclononane-1, 4, 7-tris-(glutaric acid)(NOTGA) for Multimeric Radiopharmaceuticals of Gallium" 23 : 2229-2238, 2012

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      14 Eder M, "ScVEGF-PEG-HBED-CC and scVEGF-PEG-NOTA conjugates: comparison of easy-to-label recombinant proteins for [68Ga]PET imaging of VEGF receptors in angiogenic vasculature" 37 : 405-412, 2010

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      22 Eder M, "Novel Preclinical and Radiopharmaceutical Aspects of [68Ga]Ga-PSMA-HBED-CC: A New PET Tracer for Imaging of Prostate Cancer" 7 : 779-796, 2014

      23 Ma MT, "New Tris(hydroxypyridinone) Bifunctional Chelators Containing Isothiocyanate Groups Provide a Versatile Platform for Rapid One-Step Labeling and PET Imaging with 68Ga3+" 27 : 309-318, 2016

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      28 Zhou T, "Iron binding dendrimers: a novel approach for the treatment of haemochromatosis" 49 : 4171-4182, 2006

      29 Sun Y, "Indium (III) and gallium (III) complexes of bis(aminoethanethiol) ligands with different denticities: stabilities, molecular modeling, and in vivo behavior" 39 : 458-470, 1996

      30 Kunstler J-U, "Impact of functionalized coligands on the pharmacokinetics of 99mTc(III) ‘4 + 1’ mixed-ligand complexes conjugated to bombesin" 105 : 1383-1390, 2011

      31 Ma MT, "Gallium-68 complex of a macrobicyclic cage amine chelator tethered to two integrin-targeting peptides for diagnostic tumor imaging" 22 : 2093-2103, 2011

      32 Boros E, "Evaluation of the H2dedpa Scaffold and its cRGDyK Conjugates for Labeling with 64Cu" 51 : 6279-6284, 2012

      33 Ferreira CL, "Evaluation of bifunctional chelates for the development of gallium-based radiopharmaceuticals" 21 : 531-536, 2010

      34 Berry DJ, "Efficient bifunctional gallium-68 chelators for positron emission tomography: tris(hydroxypyridinone) ligands" 47 : 7068-7070, 2011

      35 Cho YH, "Development of an automatic synthesis module for 68Ga radiopharmaceutical and its application" 52 (52): 2332-, 2011

      36 Seelam SR, "Development of 68Ga-labeled multivalent nitroimidazole derivatives for hypoxia imaging" 23 : 7743-7750, 2015

      37 Šimeček J, "Complexation of metal ions with TRAP (1, 4, 7-triazacyclononane phosphinic acid) ligands and 1, 4, 7-triazacyclononane-1, 4, 7-triacetic acid: Phosphinate-containing ligands as unique chelators for trivalent gallium" 51 : 577-590, 2011

      38 Hueting R, "Bis(thiosemicarbazones) as bifunctional chelators for the room temperature 64-copper labeling of peptides" 39 : 3620-3632, 2010

      39 Boros E, "Acyclic Chelate with Ideal Properties for 68Ga PET Imaging Agent Elaboration" 132 : 15726-15733, 2010

      40 Ma MT, "A new bifunctional chelator for copper radiopharmaceuticals : a cage amine ligand with a carboxylate functional group for conjugation to peptides" 3237-3239, 2009

      41 Simecek J, "A cyclen-based tetraphosphinate chelator for the preparation of radiolabeled tetrameric bioconjugates" 19 : 7748-7757, 2013

      42 Ren G, "A 2-helix small protein labeled with 68Ga for PET imaging of HER2 expression" 50 : 1492-1499, 2009

      43 Blom E, "68Ga-labeling of biotin analogues and their characterization" 20 : 1146-1151, 2009

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      45 Maecke HR, "68Ga-PET radiopharmacy: A generatorbased alternative to 18F-radiopharmacy" (62) : 215-242, 2007

      46 Blom E, "68Ga-Autoclabeling of DOTA-TATE and DOTA-NOC" 70 : 980-983, 2012

      47 Decristoforo C, "68Ga- and 111Inlabelled DOTA-RGD peptides for imaging of alphavbeta3 integrin expression" 35 : 1507-1515, 2008

      48 Ferreira CL, "68Ga small peptide imaging: comparison of NOTA and PCTA" 23 : 2239-2246, 2012

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