Positron emitting [68Ga]Ga-based imaging agents: Chemistry and diversity

Medicinal Chemistry

Volumn 7, Issue 5, 2011, Pages 345-379

  Velikyan, Irina ^a,b  

^a BIACORE AB   (Sweden)

^b UPPSALA UNIVERSITY   (Sweden)

Author keywords

68Ga; Conjugation chemistry; Coordination chemistry; Positron Emission Tomography; Radiochemistry

Indexed keywords

ANTISENSE OLIGONUCLEOTIDE; EPIDERMAL GROWTH FACTOR RECEPTOR; FOLATE RECEPTOR; GALLIUM 68; GASTRIN RELEASING PEPTIDE RECEPTOR; GLUCAGON LIKE PEPTIDE 1 RECEPTOR; GLYCOPROTEIN P; NEUROTENSIN RECEPTOR; PROSTATE SPECIFIC MEMBRANE ANTIGEN; SOMATOSTATIN; SOMATOSTATIN RECEPTOR; TRACER; DIAGNOSTIC AGENT; GALLIUM; RADIOPHARMACEUTICAL AGENT;

ATHEROSCLEROSIS; CELL PROLIFERATION; DRUG CONJUGATION; DRUG EFFICACY; DRUG HALF LIFE; DRUG PURIFICATION; DRUG STRUCTURE; DRUG SYNTHESIS; EARLY DIAGNOSIS; GLYCOLYSIS; GOOD MANUFACTURING PRACTICE; HEART MUSCLE; HUMAN; HYPOXIA; INFECTION; INFLAMMATION; ISOTOPE LABELING; MELANOMA; MOLECULAR IMAGING; NECROSIS; NONHUMAN; PANCREAS CANCER; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; RADIOACTIVITY; RADIOCHEMISTRY; REVIEW; THROMBOSIS; ANIMAL; CHEMISTRY; SYNTHESIS;

ANIMALS; GALLIUM RADIOISOTOPES; HUMANS; MOLECULAR IMAGING; POSITRON-EMISSION TOMOGRAPHY; RADIOPHARMACEUTICALS;

EID: 80052014406     PISSN: 15734064     EISSN: 18756638     Source Type: Journal    
DOI: 10.2174/157340611796799195     Document Type: Review

References (351)

1. Gronwall, C. Engineered affinity proteins-generation and applications. J. Biotechnol., 2009, 140, 254-269.
2. Nilsson, J.; Stahl, S.; Lundeberg, J.; Uhlen, M.; Nygren, P. A. Affinity fusion strategies for detection, purification, and immobilization of recombinant proteins. Protein Expr. Purif., 1997, 11, 1-16. (Pubitemid 27434126)
3. Zwick, M. B.; Shen, J.; Scott, J. K. Phage-displayed peptide libraries. Curr. Opin. Biotechnol., 1998, 9, 427-436. (Pubitemid 28395652)
4. Decristoforo, C.; Knopp, R.; von Guggenberg, E.; Rupprich, M.; Dreger, T.; Hess, A.; Virgolini, I.; Haubner, R. A fully automated synthesis for the preparation of 68Ga-labelled peptides. Nucl. Med. Commun., 2007, 28, 870-875. (Pubitemid 47494113)
5. Azhdarinia, A.; Yang, D. J.; Chao, C.; Mourtada, F. Infrared-based module for the synthesis of 68Ga-labeled radiotracers. Nucl. Med. Biol., 2007, 34, 121-127. (Pubitemid 46038154)
6. Cagnolini, A.; Chen, J.; Ramos, K.; Skedzielewski, T. M.; Lantry, L. E.; Nunn, A. D.; Swenson, R. E.; Linder, K. E. Automated synthesis, characterization and biological evaluation of [(68) Ga]Ga-AMBA, and the synthesis and characterization of (nat) Ga-AMBA and [(67) Ga]Ga-AMBA. Appl. Radiat. Isot., 2010, 68, 2285-2292.
7. Bauwens, M.; Chekol, R.; Vanbilloen, H.; Bormans, G.; Verbruggen, A. Optimal buffer choice of the radiosynthesis of Ga-68-Dotatoc for clinical application. Nucl. Med. Commun., 2010, 31, 753-758.
8. Meyer, G. J.; Macke, H.; Schuhmacher, J.; Knapp, W. H.; Hofmann, M. 68Ga-labelled DOTA-derivatised peptide ligands. Eur. J. Nucl. Med. Mol. Imag., 2004, 31, 1097-1104.
9. Rizzello, A.; Di Pierro, D.; Lodi, F.; Trespidi, S.; Cicoria, G.; Pancaldi, D.; Nanni, C.; Marengo, M.; Marzola, M. C.; Ai-Nahhas, A.; Rubello, D.; Boschi, S. Synthesis and quality control of Ga-68 citrate for routine clinical PET. Nucl. Med. Commun., 2009, 30, 542-545.
10. Al-Nahhas, A.; Win, Z.; Szyszko, T.; Singh, A.; Nanni, C.; Fanti, S.; Rubello, D. Gallium-68 PET: a new frontier in receptor cancer imaging. Anticancer Res., 2007, 27, 4087-4094.
11. Anderson, C. J., Welch, M. J. Radiometal-labeled agents (nontechnetium) for diagnostic imaging. Chem. Rev., 1999, 99, 2219-2234.
12. Baum, R. P.; Prasad, V.; Hommann, M.; Horsch, D. Receptor PET/CT imaging of neuroendocrine tumors. Recent Results Cancer Res., 2008, 170, 225-242.
13. Fani, M.; Andre, J. P.; Maecke, H. R. 68Ga-PET: a powerful generator-based alternative to cyclotron-based PET radiopharmaceuticals. Contrast Media Mol. Imag., 2008, 3, 67-77.
14. Fichna, J.; Janecka, A. Synthesis of target-specific radiolabeled peptides for diagnostic Imaging. Bioconjug. Chem., 2003, 14, 3-17. (Pubitemid 36172460)
15. Froidevaux, S.; Eberle, A. N. Somatostatin analogs and radiopeptides in cancer therapy. Biopolymers, 2002, 66, 161-183. (Pubitemid 35285217)
16. Ginj, M.; Maecke, H. R. Radiometallo-labeled peptides in tumor diagnosis and therapy. Met. Ions Biol. Syst., 2004, 42, 109-142.
17. Green, M. A.; Welch, M. J. Gallium radiopharmaceutical chemistry. Nucl. Med. Biol., 1989, 16, 435-448. (Pubitemid 19213884)
18. Hao, G.; Singh, A. N.; Liu, W.; Sun, X. PET with non-standard nuclides. Curr. Top Med. Chem., 2010, 10, 1096-1112.
19. 99mTc. Int. J. Appl. Radiat. Isotopes, 1977, 28, 169-181. (Pubitemid 8089059)
20. Khan, M. U.; Khan, S.; El-Refaie, S.; Win, Z.; Rubello, D.; Al-Nahhas, A. Clinical indications for Gallium-68 positron emission tomography imaging. Eur. J. Surg. Oncol., 2009, 35, 561-567.
21. Liu, S. The role of coordination chemistry in the development of target-specific radiopharmaceuticals. Chem. Soc. Rev., 2004, 33, 445-461. (Pubitemid 39461952)
22. Lundqvist, H.; Tolmachev, V. Targeting peptides and positron emission tomography. Biopolymers, 2002, 66, 381-392. (Pubitemid 36433533)
23. Maecke, H. R. Radiolabeled peptides in nuclear oncology: influence of peptide structure and labeling strategy on pharmacology. Ernst Schering Res Found Workshop, 2005, 43-72.
24. Maecke, H. R.; Hofmann, M.; Haberkorn, U. (68)Ga-labeled peptides in tumor imaging. J. Nucl. Med., 2005, 46 Suppl 1, 172S-178S.
25. Reichert, D. E.; Lewis, J. S.; Andreson, C. J. Metal complexes as diagnostic tools. Coord. Chem. Rev., 1999, 184, 3-66.
26. Reubi, J. C. Peptide receptors as molecular targets for cancer diagnosis and therapy. Endocr. Rev., 2003, 24, 389-427. (Pubitemid 37056239)
27. Tolmachev, V.; Stone-Elander, S. Radiolabelled proteins for positron emission tomography: Pros and cons of labelling methods. Biochim. Biophys. Acta., 2010, 1800, 487-510.
28. Win, Z.; Al-Nahhas, A.; Rubello, D.; Gross, M. D. Somatostatin receptor PET imaging with Gallium-68 labeled peptides. Q. J. Nucl. Med. Mol. Imag., 2007, 51, 244-250. (Pubitemid 47181084)
29. Bartholoma, M. D.; Louie, A. S.; Valliant, J. F.; Zubieta, J. Technetium and gallium derived radiopharmaceuticals: comparing and contrasting the chemistry of two important radiometals for the molecular imaging era. Chem. Rev., 2010, 110, 2903-2920.
30. Schottelius, M.; Wester, H. J. Molecular imaging targeting peptide receptors. Methods, 2009, 48, 161-177.
31. Mankoff, D. A.; Link, J. M.; Linden, H. M.; Sundararajan, L.; Krohn, K. A. Tumor receptor imaging. J. Nucl. Med., 2008, 49 Suppl 2, 149S-163S. (Pubitemid 351948042)
32. Yang, D. J.; Kim, E. E.; Inoue, T. Targeted molecular imaging in oncology. Ann. Nucl. Med., 2006, 20, 1-11. (Pubitemid 43356305)
33. Liu, S. Bifunctional coupling agents for radiolabeling of biornolecules and target-specific delivery of metallic radionuclides. Adv. Drug Deliv. Rev., 2008, 60, 1347-1370.
34. Reubi, J. C.; Maecke, H. R. Peptide-Based Probes for Cancer Imaging. J. Nucl. Med., 2008, 49, 1735-1738.
35. Maecke, H.; André, J. 68Ga-PET Radiopharmacy: A Generator-Based Alternative to 18F-Radiopharmacy. Ernst. Schering Res. Found Workshop., 2007, 215-242.
36. Dijkraaf, I.; Wester, H. J.: Peptides, multimers and polymers. in Handb Exp Pharmacol. 2008, 61-92.
37. Al-Nahhas, A.; Win, Z.; Szyszko, T.; Singh, A.; Khan, S.; Rubello, D. What can gallium-68 PET add to receptor and molecular imaging? Eur. J. Nucl. Med. Mol. Imag., 2007, 34, 1897-1901. (Pubitemid 350212142)
38. Antunes, P.; Ginj, M.; Zhang, H.; Waser, B.; Baum, R. P.; Reubi, J. C.; Maecke, H. Are radiogallium-labelled DOTA-conjugated somatostatin analogues superior to those labelled with other radiometals? Eur. J. Nucl. Med. Mol. Imagi., 2007, 34, 982-993. (Pubitemid 46919547)
39. Rosch, F.; Knapp, F.: Radionuclide generators. in Vertes A, Nagy S, Klencsar Z, Rosch F (eds): Handbook of Nuclear Chemistry. Dordrecht: Kluwer Academic Publishers, 2003, vol 4, 81-118.
40. Mirzadeh, S.; Lambrecht, R. M. Radiochemistry of germanium. J. Rad. Nucl. Chem., 1996, 202, 7-102. (Pubitemid 26056581)
41. Yano, Y.; Anger, H. O. A gallium68 positron cow for medical use. J. Nucl. Med., 1964, 5, 485-488.
42. Nakayama, M.; Haratake, M.; Koiso, T.; Ishibashi, O.; Harada, K.; Nakayama, H.; Sugii, A.; Yahara, S.; Arano, Y. Separation of Ga-68 from Ge-68 using a macroporous organic polymer containing N-methylglucamine groups. Anal. Chim. Acta., 2002, 453, 135-141. (Pubitemid 34117553)
43. 68Ga in dilute HCl. Int. J. Appl. Radiat. Isot., 1981, 32, 31-36.
44. 68Ga-bioconjugates with high specific radioactivity. Bioconjug. Chem., 2004, 15, 554-560. (Pubitemid 38657861)
45. McQuade, P.; Rowland, D. J.; Lewis, J. S.; Welch, M. J. Positronemitting isotopes produced on biomedical cyclotrons. Curr. Med. Chem., 2005, 12, 807-818. (Pubitemid 40394332)
46. Sanchez-Crespo, A.; Andreo, P.; Larsson, S. A. Positron flight in human tissues and its influence on PET image spatial resolution. Eur. J. Nucl. Med. Mol. Imag., 2004, 31, 44-51. (Pubitemid 38133540)
47. de Jong, H.; Perk, L.; Visser, G. W. M.; Boellaard, R.; van Dongen, G.; Lammertsma, A. A.: High resolution PET imaging characteristics of Ga-68, I-124 and Zr-89 compared to F-18. in Yu B (ed): 2005 IEEE Nuclear Science Symposium Conference Record, Vols 1-5. Ieee Nuclear Science Symposium - Conference Record. 2005, 1624-1627. (Pubitemid 46172054)
48. Dymov, A. M.; Savostin, A. P.: Analytical chemistry of gallium. Moscow, Ann Arbor: Ann Arbor Science Publihers, 1968.
49. Harris, W. R.; Messori, L. A comparative study of aluminum (III), gallium (III), indium (III), and thallium (III) binding to human serum transferrin. Coordination Chem. Rev., 2002, 228, 237-262.
50. Pearson, R. G. Hard and soft acids and bases. JACS., 1963, 85, 3533-3539.
51. Luyt, L. G.; Katzenellenbogen, J. A. A trithiolate tripodal bifunctional ligand for the radiolabeling of peptides with gallium (III). Bioconjug. Chem., 2002, 13, 1140-1145.
52. Zhernosekov, K. P.; Filosofov, D. V.; Baum, R. P.; Aschoff, P.; Bihl, H.; Razbash, A. A.; Jahn, M.; Jennewein, M.; Rosch, F. Processing of Generator-Produced 68Ga for Medical Application. J. Nucl. Med., 2007, 48, 1741-1748. (Pubitemid 47572722)
53. Velikyan, I.; Långström, B.; Beyer, G. Method of obtaining gallium-68 and use thereof and device for carrying out said method. WO/2004/089517 A1, October 21, 2004.
54. Asti, M.; De Pietri, G.; Fraternali, A.; Grassi, E.; Sghedoni, R.; Floroni, F.; Roesch, F.; Versari, A.; Salvo, D. Validation of Ge-68/Ga-68 generator processing by chemical purification for routine clinical application of Ga-68-DOTATOC. Nucl. Med. Biol., 2008, 35, 721-724.
55. Kraus, K. A.; Nelson, F.: Anion exchange studies of the fission products. In Conference on peaceful uses of atomic energy. United Nations, 1956:113-125.
56. 68Ga-Labelled Macromolecules; http://urn. kb.se/resolve?urn=urn:nbn: se:uu:diva-5876. Doctoral Thesis from the Faculty of Sciences and Technology, Uppsala University, Sweden, 2005.
57. Nelson, F.; Murase, T.; Kraus, K. A. Ion exchange procedures: I. Cation exchange in concentration HCl and HClO4 solutions. J. Chromatograph. A, 1964, 13, 503-535.
58. Gebhardt, P.; Opfermann, T.; Saluz, H. P. Computer controlled Ga-68 milking and concentration system. Appl. Rad. Isotop., 2010, 68, 1057-1059.
59. 68Ga generator eluate from Fe (III) intended to improve specific radioactivity of 68Ga-based radiopharmaceuticals. WO/2009/102378 A2 2007.
60. Breeman, W. A.; de Jong, M.; de Blois, E.; Bernard, B. F.; Konijnenberg, M.; Krenning, E. P. Radiolabelling DOTA-peptides with (68) Ga. Eur. J. Nucl. Med. Mol. Imag., 2005, 32, 478-485.
61. Velikyan, I.; Beyer, G. J.; Bergstrom-Pettermann, E.; Johansen, P.; Bergstrom, M.; Langstrom, B. The importance of high specific radioactivity in the performance of (68) Ga-labeled peptide. Nucl. Med. Biol., 2008, 35, 529-536. (Pubitemid 351853426)
62. 68Ga]-DOTATOC to somatostatin receptors in neuroendocrine tumours-impact of peptide mass. Nucl. Med. Biol., 2010, 37, 265-275.
63. Bergstrom, S. K.; Edenwall, N.; Laven, M.; Velikyan, I.; Langstrom, B.; Markides, K. E. Polyamine Deactivation of Integrated Poly (dimethylsiloxane) Structures Investigated by Radionuclide Imaging and Capillary Electrophoresis Experiments. Anal. Chem., 2005, 77, 938-942. (Pubitemid 40194159)
64. Blom, E.; Langstrom, B.; Velikyan, I. (68)Ga-Labeling of Biotin Analogues and their Characterization. Bioconjug. Chem., 2009, 20, 1146-1151.
65. Lavén, M.; Wallenborg, S.; Velikyan, I.; Bergstrom, S.; Djodjic, M.; Ljung, J.; Berglund, O.; Edenwall, N.; Markides, K. E.; Langstrom, B. Radionuclide imaging of miniaturized chemical analysis systems. Anal. Chem., 2004, 76, 7102-7108. (Pubitemid 39600886)
66. Laven, M.; Velikyan, I.; Djodjic, M.; Ljung, J.; Berglund, O.; Markides, K.; Langstrom, B.; Wallenborg, S. Imaging of peptide adsorption to microfluidic channels in a plastic compact disc using a positron emitting radionuclide. Lab on a Chip, 2005, 5, 756-763. (Pubitemid 40980104)
67. Lendvai, G.; Monazzam, A.; Velikyan, I.; Eriksson, B.; Josephsson, R.; Langstrom, B.; Bergstrom, M.; Estrada, S. Non-Hybridization Saturable Mechanisms Play a Role in the Uptake of (68) Ga-Labeled LNA-DNA Mixmer Antisense Oligonucleotides in Rats. Oligonucleotides, 2009, 19, 223-232.
68. Lendvai, G.; Velikyan, I.; Bergstrom, M.; Estrada, S.; Laryea, D.; Valila, M.; Salomaki, S.; Langstrom, B.; Roivainen, A. Biodistribution of 68Ga-labelled phosphodiester, phosphorothioate, and 2'-O-methyl phosphodiester oligonucleotides in normal rats. Eur. J. Pharm. Sci., 2005, 26, 26-38. (Pubitemid 41097258)
69. Lendvai, G.; Velikyan, I.; Estrada, S.; Eriksson, B.; Langstrom, B.; Bergstrom, M. Biodistribution of (68) Ga-Labeled LNA-DNA Mixmer Antisense Oligonucleotides for Rat Chromogranin-A. Oligonucleotides., 2008, 18, 33-49.
70. Roivainen, A.; Tolvanen, T.; Salomaki, S.; Lendvai, G.; Velikyan, I.; Numminen, P.; Valila, M.; Sipila, H.; Bergstrom, M.; Harkonen, P.; Lonnberg, H.; Langstrom, B. 68Ga-labeled oligonucleotides for in vivo imaging with PET. J. Nucl. Med., 2004, 45, 347-355. (Pubitemid 47618660)
71. 68Galabelling of oligonucleotides. J. Lab. Comp. Radiopharm., 2004, 47, 79-89.
72. Långström, B.; Velikyan, I.; Bergström, M.; Lindhe, Ö. Galabeled peptide-based radiopharmaceuticals. WO/2008/026040, 2008.
73. Velikyan, I.; Långström, B. Microwave method for preparing radiolabelled gallium complexes. WO/2004/089425, 2004.
74. Velikyan, I.; Sundberg, A. L.; Lindhe, O.; Hoglund, A. U.; Eriksson, O.; Werner, E.; Carlsson, J.; Bergstrom, M.; Langstrom, B.; Tolmachev, V. Preparation and evaluation of (68) Ga-DOTA-hEGF for visualization of EGFR expression in malignant tumors. J. Nucl. Med., 2005, 46, 1881-1888. (Pubitemid 46196651)
75. Tolmachev, V.; Velikyan, I.; Sandstrom, M.; Orlova, A. A HER2-binding Affibody molecule labelled with 68Ga for PET imaging: direct in vivo comparison with the 111In-labelled analogue. Eur. J. Nucl. Med. Mol. Imag., 2010, 37, 1356-1367.
76. Velikyan, I.; Maecke, H.; Langstrom, B. Convenient preparation of 68Ga-based PET-radiopharmaceuticals at room temperature. Bioconjug. Chem., 2008, 19, 569-573. (Pubitemid 351294931)
77. 68Ga-Labeling of a Free and Macromolecule Conjugated Macrocyclic Chelator at Room Temperature WO/2008/026051, 2006.
78. Riss, P. J.; Kroll, C.; Nagel, V.; Rosch, F. NODAPA-OH and NODAPA-(NCS) n: synthesis, 68Ga-radiolabelling and in vitro characterisation of novel versatile bifunctional chelators for molecular imaging. Bioorg. Med. Chem. Lett., 2008, 18, 5364-5367.
79. MacGillivray, R. T.; Moore, S. A.; Chen, J.; Anderson, B. F.; Baker, H.; Luo, Y.; Bewley, M.; Smith, C. A.; Murphy, M. E.; Wang, Y.; Mason, A. B.; Woodworth, R. C.; Brayer, G. D.; Baker, E. N. Two high-resolution crystal structures of the recombinant N-lobe of human transferrin reveal a structural change implicated in iron release. Biochemistry, 1998, 37, 7919-7928. (Pubitemid 28307052)
80. Broan, C. J.; Cox, J. P. L.; Craig, A. S.; Kataky, R.; Parker, D.; Harrison, A.; Randall, A. M.; Ferguson, G. Structure and solution stability of indium and gallium complexes of 1, 4, 7, - triazacyclononanetriacetate and yttrium complexes of 1, 4, 7, 10-tetraazacyclododecanetetraacetate and related ligands: kinetically stable complexes for use in imaging and radioimmunotherapy. X-ray molecular structure of the indium and gallium complexes of 1, 4, 7,-triazacyclononane-1, 4, 7-triacetic acid. J. Chem. Soc. Perkin Trans. 2, 1991, 1, 87-99.
81. Arslantas, E.; Smith-Jones, P. M.; Ritter, G.; Schmidt, R. R. TAME-Hex A - A novel bifunctional chelating agent for radioimmunoimaging. Eur. J. Org. Chem., 2004, 3979-3984.
82. Chaves, S.; Mendonca, A. C.; Marques, S. M.; Prata, M. I.; Santos, A. C.; Martins, A. F.; Geraldes, C. F.; Santos, M. A. A gallium complex with a new tripodal tris-hydroxypyridinone for potential nuclear diagnostic imaging: solution and in vivo studies of 67Galabeled species. J. Inorg. Biochem., 2011, 105, 31-38.
83. Hancock, R. Molecular mechanics calculations and metal ion recognition. Acc. Chem. Res., 1990, 23, 253-257.
84. Umetani, S.; Le, Q.; Matsui, M. Molecular design of chelating ligands with highly selective recognition and separation functions for group 13 metal ions. ICR Annual Report, 1996, 3, 14-15.
85. Kaden, T. A. Reactivity and function of macrocyclic metal complexes. Chimia, 2000, 54, 574-578.
86. Clarke, E. T.; Martell, A. E. Stabilities of the Fe (III), Ga (III) and In (III) Chelates of N, N', N"-Triazacyclononanetriacetic Acid. Inorganica Chimica Acta., 1991, 181, 273-280.
87. Clarke, T. E., Martell, A. E. Stabilities of trivalent metal ion complexes of the tetraacetate derivatives of 12-, 13-and 14-membered tetraazamacrocyles. Inorganic Chimica Acta., 1991, 190, 37-46.
88. Heppeler, A.; Froidevaux, S.; Macke, H. R.; Jermann, E.; Behe, M.; Powell, P.; Hennig, M. Radiometal-labelled macrocyclic chelatorderivatised somatostatin analogue with superb tumour-targeting properties and potential for receptor-mediated internal radiotherapy. Chem-a Eur. J., 1999, 5, 1974-1981. (Pubitemid 129502685)
89. De Leon-Rodriguez, L. M.; Kovacs, Z. The synthesis and chelation chemistry of DOTA-peptide conjugates. Bioconjug. Chem., 2008, 19, 391-402. (Pubitemid 351294908)
90. Schuhmacher, J.; Zhang, H.; Doll, J.; Macke, H. R.; Matys, R.; Hauser, H.; Henze, M.; Haberkorn, U.; Eisenhut, M. GRP Receptor-Targeted PET of a Rat Pancreas Carcinoma Xenograft in Nude Mice with a 68Ga-Labeled Bombesin (6-14) Analog. J. Nucl. Med., 2005, 46, 691-699. (Pubitemid 41721868)
91. Yang, C. T.; Sreerama, S. G.; Hsieh, W. Y.; Liu, S. Synthesis and characterization of a novel macrocyclic chelator with 3-hydroxy-4-pyrone chelating arms and its complexes with medicinally important metals. Inorg. Chem., 2008, 47, 2719-2727.
92. Craig, A. S.; Parker, D.; Adams, H.; Bailey, N. A. Stability, Ga-71 Nmr, and Crystal-Structure of a Neutral Gallium (iii) Complex of 1, 4, 7-Triazacyclononanetriacetate - a Potential Radiopharmaceutical. J. Chem. Society-Chem. Commun., 1989, 1793-1794. (Pubitemid 20061566)
93. Moore, D. A.; Fanwick, P. E.; Welch, M. J. A novel hexachelating amino thiol ligand and its complex with gallium (III). Inorg. Chem., 1990, 29, 672-676.
94. Ma, R.; Welch, M. J.; Reibenspies, J.; Martell, A. E. Stability of Metal-Ion Complexes of 1, 4, 7-Tris (2-Mercaptoethyl)-1, 4, 7-Triazacyclononane (Tacn-Tm) and Molecular-Structure of in (C12h24n3s3). Inorg. Chim. Acta., 1995, 236, 75-82.
95. Andre, J. P.; Maecke, H. R.; Zehnder, M.; Macko, L.; Akyel, K. G. 1, 4, 7-Triazacyclononane-1-succinic acid-4, 7-diacetic acid (NODASA): A new bifunctional chelator for radio galliumlabelling of biomolecules. Chem. Commun., 1998, 1301-1302. (Pubitemid 128675619)
96. Prata, M. I.; Santos, A. C.; Geraldes, C. F.; de Lima, J. J. Characterisation of 67Ga3+ complexes of triaza macrocyclic ligands: biodistribution and clearance studies. Nucl. Med. Biol., 1999, 26, 707-710. (Pubitemid 29424159)
97. Prata, M. I.; Santos, A. C.; Geraldes, C. F.; de Lima, J. J. Structural and in vivo studies of metal chelates of Ga (III) relevant to biomedical imaging. J. Inorg. Biochem., 2000, 79, 359-363. (Pubitemid 30628754)
98. Notni, J.; Hermann, P.; Havlickova, J.; Kotek, J.; Kubicek, V.; Plutnar, J.; Loktionova, N.; Riss, P. J.; Rosch, F.; Lukes, I. A triazacyclononane-based bifunctional phosphinate ligand for the preparation of multimeric 68Ga tracers for positron emission tomography. Chemistry, 2010, 16, 7174-7185.
99. Jones-Wilson, T. M.; Motekaitis, R. J.; Sun, Y.; Anderson, C. J.; Martell, A. E.; Welch, M. J. New hydroxybenzyl and hydroxypyridylmethyl substituted triazacyclononane ligands for use with gallium (III) and indium (III). Nucl. Med. Biol., 1995, 22, 859-868.
100. Moore, D. A.; Fanwick, P. E.; Welch, M. J. Synthesis, characterization, and solid-state structure of a new hexachelating ligand and its complex with gallium (iii). Inorg. Chem. 1989, 28, 1504-1506.
101. de Sa, A.; Prata, M. I. M.; Geraldes, C.; Andre, J. P. Triaza-based amphiphilic chelators: Synthetic route, in vitro characterization and in vivo studies of their Ga (III) and Al (III) chelates. J. Inorg. Biochem., 2010, 104, 1051-1062.
102. Yang, C. T.; Li, Y. X.; Liu, S. A. Synthesis and structural characterization of complexes of a DO3A-conjugated triphenylphosphonium cation with diagnostically important metal ions. Inorg. Chem., 2007, 46, 8988-8997.
103. Ferreira, C. L.; Lamsa, E.; Woods, M.; Duan, Y.; Fernando, P.; Bensimon, C.; Kordos, M.; Guenther, K.; Jurek, P.; Kiefer, G. E. Evaluation of Bifunctional Chelates for the Development of Gallium-Based Radiopharmaceuticals. Bioconjug. Chem., 2010, 21, 531-536.
104. Jeong, J. M.; Hong, M. K.; Chang, Y. S.; Lee, Y. S.; Kim, Y. J.; Cheon, G. J.; Lee, D. S.; Chung, J. K.; Lee, M. C. Preparation of a promising angiogenesis PET imaging agent: Ga-68-labeled c (RGDyK)-isothiocyanatobenzyl-1, 4, 7-triazacyclononane-1, 4, 7-triacetic acid and feasibility studies in mice. J. Nucl. Med., 2008, 49, 830-836.
105. Smith-Jones, P. M.; Stolz, B.; Burns, C.; Albert, R.; Reist, H. W.; Fridrich, R.; Mäcke, H. M. Gallium-67/Gallium-68-[DFO]-Octreotide-A Potential Radiopharmaceutical for PET Imaging of Somatostatin Receptor-Positive Tumors: Synthesis and Radiolabeling In Vitro and Preliminary In Vivo Studies. J. Nucl. Med., 1994, 35, 317-325. (Pubitemid 24048322)
106. Eder, M.; Krivoshein, A. V.; Backer, M.; Backer, J. M.; Haberkorn, U.; Eisenhut, 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. Nucl. Med. Biol., 2010, 37, 405-412.
107. Caraco, C.; Aloj, L.; Eckelman, W. C. The gallium-deferoxamine complex: Stability with different deferoxamine concentrations and incubation conditions. Appl. Rad. Isotopes, 1998, 49, 1477-1479. (Pubitemid 28383956)
108. Boros, E.; Ferreira, C. L.; Cawthray, J. F.; Price, E. W.; Patrick, B. O.; Wester, D. W.; Adam, M. J.; Orvig, C. Acyclic Chelate with Ideal Properties for Ga-68 PET Imaging Agent Elaboration. J. Am. Chem. Soc., 2010, 132, 15726-15733.
109. Kung, H. F.; Liu, B. L.; Mankoff, D.; Kung, M. P.; Billings, J. J.; Francesconi, L.; Alavi, A. A new myocardial imaging agent - synthesis, characterization, and biodistribution of gallium-68-battech. J. Nucl. Med., 1990, 31, 1635-1640. (Pubitemid 20347045)
110. Anderson, C. J.; John, C. S.; Li, Y. J.; Hancock, R. D.; McCarthy, T. J.; Martell, A. E.; Welch, M. J. N, N'-Ethylene-di-l-Cysteine (EC) complexes of Ga (III) and In (III): Molecular modeling, thermodynamic stability and in vivo studies. Nucl. Med. Biol., 1995, 22, 165-173.
111. Sun, Y. Z.; Anderson, C. J.; Pajeau, T. S.; Reichert, D. E.; Hancock, R. D.; Motekaitis, R. J.; Martell, A. E.; Welch, M. J. Indium (III) and gallium (III) complexes of bis (aminoethanethiol) ligands with different denticities: Stabilities, molecular modeling, and in vivo behavior. J. Med. Chem., 1996, 39, 458-470.
112. John, C. S.; Kinuya, S.; Minear, G.; Keast, R. K.; Paik, C. H. Synthesis and biological evaluation of gallium polyaminothiols (PAT). Nucl. Med. Biol., 1993, 20, 217-223. (Pubitemid 23043079)
113. Motekaitis, R. J.; Martell, A. E.; Koch, S. A.; Hwang, J. W.; Quarless, D. A.; Welch, M. J. The Gallium (III) and Indium (III) complexes of tris (2-mercaptobenzyl) amine and tris (2-hydroxybenzyl) amine. Inorg. Chem., 1998, 37, 5902-5911.
114. Riss, P. J.; Hanik, N.; Roesch, F. Studies towards the development of lipophilic bifunctional N3S3 chelators for Ga-68. Radiochimica Acta., 2010, 98, 519-523.
115. Hermanson, G. T. (ed): Bioconjugate Techniques. 1996.
116. Lewis, M. R., Raubitschek, A., Shively, J. E. A facile, watersolubale method for modification of proteins with DOTA. Use of elevated temperature and optimized pH to achieve high specific activity and high chelate stability in radiolabeled immunoconjugates. Bioconjug. Chem., 1994, 5, 565-576.
117. Mier, W.; Hoffend, J.; Kramer, S.; Schuhmacher, J.; Hull, W. E.; Eisenhut, M.; Haberkorn, U. Conjugation of DOTA using isolated phenolic active esters: the labeling and biodistribution of albumin as blood pool marker. Bioconjug. Chem., 2005, 16, 237-240. (Pubitemid 40129699)
118. Lewis, M. R., Shively, J. E. Maleimidocysteineamido-DOTA derivatives: new reagents for radiometal chelate conjugation to antibody sulfhydryl groups undergo pH-dependent cleavage reactions. Bioconjug. Chem., 1998, 9, 72-86. (Pubitemid 28052088)
119. Ahlgren, S.; Orlova, A.; Rosik, D.; Sandstrom, M.; Sjoberg, A.; Baastrup, B.; Widmark, O.; Fant, G.; Feldwisch, J.; Tolmachev, V. Evaluation of maleimide derivative of DOTA for site-specific labeling of recombinant affibody molecules. Bioconjug. Chem., 2008, 19, 235-243. (Pubitemid 351213855)
120. Geoghegan, K. F.; Stroh, J. G. Site-directed conjugation of nonpeptide groups to peptides and proteins via periodate-oxidation of a 2-amino alcohol - application to modification at n-terminal serine. Bioconjug. Chem., 1992, 3, 138-146.
121. Mindt, T. L.; Jungi, V.; Wyss, S.; Friedli, A.; Pla, G.; Novak-Hofer, I.; Grunberg, J.; Schibli, R. Modification of different IgG1 antibodies via glutamine and lysine using bacterial and human tissue transglutaminase. Bioconjug. Chem., 2008, 19, 271-278. (Pubitemid 351213859)
122. De Leon-Rodriguez, L. M.; Kovacs, Z.; Dieckmann, G. R.; Sherry, A. D. Solid-phase synthesis of DOTA-peptides. Chemistry-a Eur. J., 2004, 10, 1149-1155.
123. Guerin, B.; Ait-Mohand, S.; Tremblay, M. C.; Dumulon-Perreault, V.; Fournier, P.; Benard, F. Total Solid-Phase Synthesis of NOTA-Functionalized Peptides for PET Imaging. Org. Lett., 2010, 12, 280-283.
124. Tanaka, K.; Masuyama, T.; Hasegawa, K.; Tahara, T.; Mizuma, H.; Wada, Y.; Watanabe, Y.; Fukase, K. A submicrogram-scale protocol for biomolecule-based PET imaging by rapid 6 piazaelectrocyclization: Visualization of sialic acid dependent circulatory residence of glycoproteins. Angewandte Chemie-International Edition, 2008, 47, 102-105.
125. Knor, S.; Modlinger, A.; Poethko, T.; Schottelius, M.; Wester, H. J.; Kessler, H. Synthesis of novel 1, 4, 7, 10-tetraazacyclodecane-1, 4, 7, 10-tetraacetic acid (DOTA) derivatives for chemoselective attachment to unprotected polyfunctionalized compounds. Chemistry-a Eur. J., 2007, 13, 6082-6090.
126. Dijkgraaf, I.; Rijnders, A. Y.; Soede, A.; Dechesne, A. C.; van Esse, G. W.; Brouwer, A. J.; Corstens, F. H.; Boerman, O. C.; Rijkers, D. T.; Liskamp, R. M. Synthesis of DOTA-conjugated multivalent cyclic-RGD peptide dendrimers via 1, 3-dipolar cycloaddition and their biological evaluation: implications for tumor targeting and tumor imaging purposes. Org. Biomol. Chem., 2007, 5, 935-944. (Pubitemid 46375649)
127. Welch, M. J.; Redvanly, C. S.: Handbook of Radiopharmaceuticals. John Wiley & Sons, Ltd, 2003.
128. Reubi, J. C.; Macke, H. R.; Krenning, E. P. Candidates for peptide receptor radiotherapy today and in the future. J. Nucl. Med., 2005, 46 Suppl 1, 67S-75S. (Pubitemid 47619021)
129. Heppeler, A., Froidevaux, S., Eberle, A. N., Maecke, H. R. Receptor targeting for tumor localisation and therapy with radiopeptides. Curr. Med. Chem., 2000, 971-994.
130. Eisenwiener, K. P.; Prata, M. I.; Buschmann, I.; Zhang, H. W.; Santos, A. C.; Wenger, S.; Reubi, J. C.; Macke, H. R. NODAGATOC, a new chelator-coupled somatostatin analogue labeled with [67/68Ga] and [111In] for SPECT, PET, and targeted therapeutic applications of somatostatin receptor (hsst2) expressing tumors. Bioconjug. Chem., 2002, 13, 530-541. (Pubitemid 34535940)
131. Liu, S.; Edwards, D. S. Tc-99m-Labeled small peptides as diagnostic radiopharmaceuticals. Chem. Rev., 1999, 99, 2235-2268.
132. Thakur, M. L. Radiolabelled peptides: now and the future. Nucl. Med. Commun., 1995, 16, 724-732.
133. Behr, T. M.; Behe, M.; Becker, W. Diagnostic applications of radiolabeled peptides in nuclear endocrinology. Q. J. Nucl. Med., 1999, 43, 268-280. (Pubitemid 29500583)
134. Otte, A.; Jermann, E.; Behe, M.; Goetze, M.; Bucher, H. C.; Roser, H. W.; Heppeler, A.; Mueller-Brand, J.; Maecke, H. R. DOTATOC: a powerful new tool for receptor-mediated radionuclide therapy. Eur. J. Nucl. Med., 1997, 24, 792-795. (Pubitemid 27356860)
135. de Jong, M.; Bakker, W. H.; Krenning, E. P.; Breeman, W. A.; van der Pluijm, M. E.; Bernard, B. F.; Visser, T. J.; Jermann, E.; Behe, M.; Powell, P.; Macke, H. R. Yttrium-90 and indium-111 labelling, receptor binding and biodistribution of [DOTA0, d-Phe1, Tyr3]octreotide, a promising somatostatin analogue for radionuclide therapy. Eur. J. Nucl. Med., 1997, 24, 368-371. (Pubitemid 27183039)
136. Schmitt, A.; Bernhardt, P.; Nilsson, O.; Ahlman, H.; Kolby, L.; Maecke, H. R.; Forssell-Aronsson, E. Radiation therapy of small cell lung cancer with 177Lu-DOTA-Tyr3-octreotate in an animal model. J. Nucl. Med., 2004, 45, 1542-1548. (Pubitemid 47618508)
137. Pless, M.; Waldherr, C.; Maecke, H.; Buitrago, C.; Herrmann, R.; Mueller-Brand, J. Targeted radiotherapy for small cell lung cancer using 90Yttrium-DOTATOC, an Yttrium-labelled somatostatin analogue: a pilot trial. Lung Cancer, 2004, 45, 365-371. (Pubitemid 39037718)
138. Meier, G.; Waldherr, C.; Herrmann, R.; Maecke, H.; Mueller-Brand, J.; Pless, M. Successful targeted radiotherapy with 90Y-DOTATOC in a patient with Merkel cell carcinoma. A Case Report. Oncology, 2004, 66, 160-163. (Pubitemid 38608384)
139. Mutic, S.; Malyapa, R. S.; Grigsby, P. W.; Dehdashti, F.; Miller, T. R.; Zoberi, I.; Bosch, W. R.; Esthappan, J.; Low, D. A. PET-guided IMRT for cervical carcinoma with positive para-aortic lymph nodes-a dose-escalation treatment planning study. Int. J. Radiat. Oncol. Biol. Phys., 2003, 55, 28-35. (Pubitemid 36020341)
140. Kowalski, J.; Henze, M.; Schuhmacher, J.; Macke, H. R.; Hofmann, M.; Haberkorn, U. Evaluation of positron emission tomography imaging using [68Ga]-DOTA-D Phe (1)-Tyr (3)-Octreotide in comparison to [111In]-DTPAOC SPECT. First results in patients with neuroendocrine tumors. Mol. Imaging Biol., 2003, 5, 42-48. (Pubitemid 36596544)
141. Eary, J. F. PET imaging for planning cancer therapy. J. Nucl. Med., 2001, 42, 770-771.
142. Barone, R.; Borson-Chazot, F.; Valkema, R.; Walrand, S.; Chauvin, F.; Gogou, L.; Kvols, L. K.; Krenning, E. P.; Jamar, F.; Pauwels, S. Patient-specific dosimetry in predicting renal toxicity with (90) Y-DOTATOC: relevance of kidney volume and dose rate in finding a dose-effect relationship. J. Nucl. Med., 2005, 46 Suppl 1, 99S-106S. (Pubitemid 47619025)
143. Gambhir, S. S. Molecular imaging of cancer with positron emission tomography. Nat. Rev. Cancer, 2002, 2, 683-693. (Pubitemid 37328919)
144. Carlsson, J.; Forssell-Aronsson, E.; Glimelius, B.; Mattsson, S. Therapy with radiopharmaceuticals. Acta. Oncol., 2002, 41, 623-628. (Pubitemid 36106205)
145. Tofilon, P. J.; Saxman, S.; Coleman, C. N. Molecular targets for radiation therapy: bringing preclinical data into clinical trials. Clin. Cancer Res., 2003, 9, 3518-3520. (Pubitemid 37169213)
146. Carlsson, J.; Forssell Aronsson, E.; Hietala, S. O.; Stigbrand, T.; Tennvall, J. Tumour therapy with radionuclides: assessment of progress and problems. Radiother. Oncol., 2003, 66, 107-117. (Pubitemid 36321806)
147. Forssell-Aronsson, E.; Kjellen, E.; Mattsson, S.; Hellstrom, M. Medical imaging for improved tumour characterization, delineation and treatment verification. Acta Oncol., 2002, 41, 604-614. (Pubitemid 36109157)
148. Reubi, J. C. Somatostatin receptor sst1-sst5 expression in normal and neoplastic human tissues using receptor autoradiography with subtype-selective ligands. 2001, 28, 836-846.
149. Rivier, J. E.; Kirby, D. A.; Erchegyi, J.; Waser, B.; Eltschinger, V.; Cescato, R.; Reubi, J. C. Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides. J. Med. Chem., 2005, 48, 515-522. (Pubitemid 40139794)
150. Wild, D.; Schmitt, J. S.; Ginj, M.; Macke, H. R.; Bernard, B. F.; Krenning, E.; De Jong, M.; Wenger, S.; Reubi, J. C. DOTA-NOC, a high-affinity ligand of somatostatin receptor subtypes 2, 3 and 5 for labelling with various radiometals. Eur. J. Nucl. Med. Mol. Imaging., 2003, 30, 1338-1347. (Pubitemid 37247950)
151. Ginj, M.; Chen, J.; Walter, M. A.; Eltschinger, V.; Reubi, J. C.; Maecke, H. R. Preclinical evaluation of new and highly potent analogues of octreotide for predictive imaging and targeted radiotherapy. Clin. Cancer Res., 2005, 11, 1136-1145. (Pubitemid 40175763)
152. Hofland, L. J.; Breeman, W. A.; Krenning, E. P.; de Jong, M.; Waaijers, M.; van Koetsveld, P. M.; Macke, H. R.; Lamberts, S. W. Internalization of [DOTA degrees, 125I-Tyr3]Octreotide by somatostatin receptor-positive cells in vitro and in vivo: implications for somatostatin receptor-targeted radio-guided surgery. Proc. Assoc. Am. Physicians, 1999, 111, 63-69. (Pubitemid 29047111)
153. De Jong, M.; Bakker, W. H.; Breeman, W. A.; Bernard, B. F.; Hofland, L. J.; Visser, T. J.; Srinivasan, A.; Schmidt, M.; Behe, M.; Macke, H. R.; Krenning, E. P. Pre-clinical comparison of [DTPA0] octreotide, [DTPA0, Tyr3] octreotide and [DOTA0, Tyr3] octreotide as carriers for somatostatin receptor-targeted scintigraphy and radionuclide therapy. Int. J. Cancer, 1998, 75, 406-411. (Pubitemid 28100044)
154. Reubi, J. C.; Schär, J.-C.; Waser, B.; Wenger, S.; Heppeler, A.; Schmitt, J. S.; Mäcke, H. R. Affinity profiles for human somatostatin receptor subtypes SST1-SST5 of somatostatin radiotracers selected for scintigraphic and radiotherapeutic use. Eur. J. Nucl. Med. Mol. Imag., 2000, 27, 273-282. (Pubitemid 30167697)
155. Forrer, F.; Uusijarvi, H.; Waldherr, C.; Cremonesi, M.; Bernhardt, P.; Mueller-Brand, J.; Maecke, H. R. A comparison of (111) In-DOTATOC and (111) In-DOTATATE: biodistribution and dosimetry in the same patients with metastatic neuroendocrine tumours. Eur. J. Nucl. Med. Mol. Imag., 2004, 31, 1257-1262. (Pubitemid 39222489)
156. Schmitt, A.; Bernhardt, P.; Nilsson, O.; Ahlman, H.; Kolby, L.; Forssell-Aronsson, E. Differences in biodistribution between 99mTc-depreotide, 111In-DTPA-octreotide, and 177Lu-DOTA-Tyr3-octreotate in a small cell lung cancer animal model. Cancer Biother. Radiopharm., 2005, 20, 231-236. (Pubitemid 40696108)
157. Froidevaux, S.; Eberle, A. N.; Christe, M.; Sumanovski, L.; Heppeler, A.; Schmitt, J. S.; Eisenwiener, K.; Beglinger, C.; Macke, H. R. Neuroendocrine tumor targeting: study of novel galliumlabeled somatostatin radiopeptides in a rat pancreatic tumor model. Int. J. Cancer, 2002, 98, 930-937. (Pubitemid 34286693)
158. Henze, M.; Schuhmacher, J.; Hipp, P.; Kowalski, J.; Becker, D. W.; Doll, J.; Macke, H. R.; Hofmann, M.; Debus, J.; Haberkorn, U. PET Imaging of Somatostatin Receptors Using [68GA]DOTA-D-Phe1-Tyr3-Octreotide: First Results in Patients with Meningiomas. J. Nucl. Med., 2001, 42, 1053-1056. (Pubitemid 32595304)
159. Deshmukh, M. V.; Voll, G.; Kuhlewein, A.; Macke, H.; Schmitt, J.; Kessler, H.; Gemmecker, G. NMR studies reveal structural differences between the gallium and yttrium complexes of DOTA-D-Phe1-Tyr3-octreotide. J. Med. Chem., 2005, 48, 1506-1514. (Pubitemid 40364558)
160. Hofmann, M.; Maecke, H.; Borner, R.; Weckesser, E.; Schoffski, P.; Oei, L.; Schumacher, J.; Henze, M.; Heppeler, A.; Meyer, J.; Knapp, H. Biokinetics and imaging with the somatostatin receptor PET radioligand (68) Ga-DOTATOC: preliminary data. Eur. J. Nucl. Med., 2001, 28, 1751-1757.
161. Wild, D.; Macke, H. R.; Waser, B.; Reubi, J. C.; Ginj, M.; Rasch, H.; Muller-Brand, J.; Hofmann, M. 68Ga-DOTANOC: a first compound for PET imaging with high affinity for somatostatin receptor subtypes 2 and 5. Eur. J. Nucl. Med. Mol. Imag., 2005, 32, 724. (Pubitemid 40897499)
162. Pettinato, C.; Sarnelli, A.; Di Donna, M.; Civollani, S.; Nanni, C.; Montini, G.; Di Pierro, D.; Ferrari, M.; Marengo, M.; Bergamini, C. (68) Ga-DOTANOC: biodistribution and dosimetry in patients affected by neuroendocrine tumors. Eur. J. Nucl. Med. Mol. Imag., 2008, 35, 72-79. (Pubitemid 350234154)
163. Antunes, P.; Ginj, M.; Walter, M. A.; Chen, J.; Reubi, J. C.; Maecke, H. R. Influence of Different Spacers on the Biological Profile of a DOTA-Somatostatin Analogue. Bioconjug. Chem., 2007, 18, 84-92. (Pubitemid 46145997)
164. Erchegyi, J.; Grace, C. R.; Samant, M.; Cescato, R.; Piccand, V.; Riek, R.; Reubi, J. C.; Rivier, J. E. Ring size of somatostatin analogues (ODT-8) modulates receptor selectivity and binding affinity. J. Med. Chem., 2008, 51, 2668-2675. (Pubitemid 351620788)
165. Grace, C. R.; Erchegyi, J.; Samant, M.; Cescato, R.; Piccand, V.; Riek, R.; Reubi, J. C.; Rivier, J. E. Ring size in octreotide amide modulates differently agonist versus antagonist binding affinity and selectivity. J. Med. Chem., 2008, 51, 2676-2681. (Pubitemid 351620789)
166. Grace, C. R.; Erchegyi, J.; Reubi, J. C.; Rivier, J. E.; Riek, R. Threedimensional consensus structure of sst2-selective somatostatin (SRIF) antagonists by NMR. Biopolymers, 2008, 89, 1077-1087.
167. Cescato, R.; Erchegyi, J.; Waser, B.; Piccand, V.; Maecke, H. R.; Rivier, J. E.; Reubi, J. C. Design and in vitro characterization of highly sst2-selective somatostatin antagonists suitable for radiotargeting. J. Med. Chem., 2008, 51, 4030-4037. (Pubitemid 351956530)
168. Fani, M.; Mueller, A.; Tamma, M. L.; Nicolas, G.; Rink, H. R.; Cescato, R.; Reubi, J. C.; Maecke, H. R. Radiolabeled bicyclic somatostatin-based analogs: a novel class of potential radiotracers for SPECT/PET of neuroendocrine tumors. J. Nucl. Med., 2010, 51, 1771-1779.
169. Zhang, H.; Moroz, M. A.; Serganova, I.; Ku, T.; Huang, R.; Vider, J.; Maecke, H. R.; Larson, S. M.; Blasberg, R.; Smith-Jones, P. M. Imaging Expression of the Human Somatostatin Receptor Subtype-2 Reporter Gene with 68Ga-DOTATOC. J. Nucl. Med., 2010, jnumed.110.079004.
170. Hanin, F. X.; Pauwels, S.; Bol, A.; Breeman, W.; de Jong, M.; Jamar, F. Tumor uptake of 68Ga-DOTA-Tyr3-octreotate: animal PET studies of tumor flow and acute somatostatin receptor modulation in the CA20948 rat model. Nucl. Med. Biol., 2010, 37, 157-165.
171. Hofmann, M.; Beyer, T.; Boerner, A.; Mueller, J.; Frilling, A.; Maecke, H.; Muller, S.; Clauss, R.; Bockisch, A.; Knapp, W. Improved imaging of SMS PET (Ga-68-DOTATOC) by PET/CT in carcinoids. Eur. J. Nucl. Med. Mol. Imag., 2004, 31, S339.
172. Koukouraki, S.; Strauss, L. G.; Georgoulias, V.; Schuhmacher, J.; Haberkorn, U.; Karkavitsas, N.; Dimitrakopoulou-Strauss, A. Evaluation of the pharmacokinetics of 68Ga-DOTATOC in patients with metastatic neuroendocrine tumours scheduled for 90Y-DOTATOC therapy. Eur. J. Nucl. Med. Mol. Imaging, 2006, 33, 460-466.
173. Gabriel, M.; Decristoforo, C.; Kendler, D.; Dobrozemsky, G.; Heute, D.; Uprimny, C.; Kovacs, P.; Von Guggenberg, E.; Bale, R.; Virgolini, I. J. 68Ga-DOTA-Tyr3-octreotide PET in neuroendocrine tumors: comparison with somatostatin receptor scintigraphy and CT. J. Nucl. Med., 2007, 48, 508-518. (Pubitemid 47571404)
174. Henze, M.; Schuhmacher, J.; Dimitrakopoulou-Strauss, A.; Strauss, L. G.; Macke, H. R.; Eisenhut, M.; Haberkorn, U. Exceptional increase in somatostatin receptor expression in pancreatic neuroendocrine tumour, visualised with Ga-68-DOTATOC PET. Eur. J. Nucl. Med. Mol. Imaging, 2004, 31, 466-466.
175. Dimitrakopoulou-Strauss, A.; Georgoulias, V.; Eisenhut, M.; Herth, F.; Koukouraki, S.; Macke, H. R.; Haberkorn, U.; Strauss, L. G. Quantitative assessment of SSTR2 expression in patients with non-small cell lung cancer using Ga-68-DOTATOC PET and comparison with F-18-FDG PET. Eur. J. Nucl. Med. Mol. Imaging, 2006, 33, 823-830. (Pubitemid 43979691)
176. Koukouraki, S.; Strauss, L. G.; Georgoulias, V.; Eisenhut, M.; Haberkorn, U.; Dimitrakopoulou-Strauss, A. Comparison of the pharmacokinetics of Ga-68-DOTATOC and F-18 FDG in patients with metastatic neuroendocrine tumours scheduled for Y-90-DOTATOC therapy. Eur. J. Nucl. Med. Mol. Imaging, 2006, 33, 1115-1122. (Pubitemid 44484467)
177. Kayani, I.; Bomanji, J. B.; Groves, A.; Conway, G.; Gacinovic, S.; Win, T.; Dickson, J.; Caplin, M.; Ell, P. J. Functional imaging of neuroendocrine tumors with combined PET/CT using 68Ga-DOTATATE (DOTA-DPhe1, Tyr3-octreotate) and 18F-FDG. Cancer, 2008, 112, 2447-2455.
178. Gabriel, M.; Andergassen, U.; Putzer, D.; Kroiss, A.; Waitz, D.; Von Guggenberg, E.; Kendler, D.; Virgolini, I. J. Individualized peptide-related-radionuclide-therapy concept using different radiolabelled somatostatin analogs in advanced cancer patients. Q. J. Nucl. Med. Mol. Imaging, 2010, 54, 92-99.
179. Putzer, D.; Gabriel, M.; Kendler, D.; Henninger, B.; Knoflach, M.; Kroiss, A.; Vonguggenberg, E.; Warwitz, B.; Virgolini, I. J. Comparison of (68) Ga-DOTA-Tyr (3)-octreotide and (18) F-fluoro-L-dihydroxyphenylalanine positron emission tomography in neuroendocrine tumor patients. Q. J. Nucl. Med. Mol. Imaging, 2010, 54, 68-75.
180. Modlin, I. M.; Oberg, K.; Chung, D. C.; Jensen, R. T.; de Herder, W. W.; Thakker, R. V.; Caplin, M.; Delle Fave, G.; Kaltsas, G. A.; Krenning, E. P.; Moss, S. F.; Nilsson, O.; Rindi, G.; Salazar, R.; Ruszniewski, P.; Sundin, A. Gastroenteropancreatic neuroendocrine tumours. Lancet Oncol., 2008, 9, 61-72.
181. Virgolini, I.; Ambrosini, V.; Bomanji, J. B.; Baum, R. P.; Fanti, S.; Gabriel, M.; Papathanasiou, N. D.; Pepe, G.; Oyen, W.; De Cristoforo, C.; Chiti, A. Procedure guidelines for PET/CT tumour imaging with 68Ga-DOTA-conjugated peptides: 68Ga-DOTA-TOC, 68Ga-DOTA-NOC, 68Ga-DOTA-TATE. Eur. J. Nucl. Med. Mol. Imaging, 2010, 37, 2004-2010.
182. Janson, E. T.; Sorbye, H.; Welin, S.; Federspiel, B.; Gronbaek, H.; Hellman, P.; Mathisen, O.; Mortensen, J.; Sundin, A.; Thiis-Evensen, E.; Valimaki, M. J.; Oberg, K.; Knigge, U. Nordic Guidelines 2010 for diagnosis and treatment of gastroenteropancreatic neuroendocrine tumours. Acta Oncologica, 2010, 49, 740-756.
183. Win, Z.; Al-Nahhas, A.; Towey, D.; Todd, J. F.; Rubello, D.; Lewington, V.; Gishen, P. 68Ga-DOTATATE PET in neuroectodermal tumours: first experience. Nucl. Med. Commun., 2007, 28, 359-363. (Pubitemid 46569168)
184. Srirajaskanthan, R.; Kayani, I.; Quigley, A. M.; Soh, J.; Caplin, M. E.; Bomanji, J. The Role of 68Ga-DOTATATE PET in Patients with Neuroendocrine Tumors and Negative or Equivocal Findings on 111In-DTPA-Octreotide Scintigraphy. J. Nucl. Med., 2010, 51, 875-882.
185. Putzer, D.; Gabriel, M.; Henninger, B.; Kendler, D.; Uprimny, C.; Dobrozemsky, G.; Decristoforo, C.; Bale, R. J.; Jaschke, W.; Virgolini, I. J. Bone Metastases in Patients with Neuroendocrine Tumor: 68Ga-DOTA-Tyr3-Octreotide PET in Comparison to CT and Bone Scintigraphy. J. Nucl. Med., 2009, 50, 1214-1221.
186. Milker-Zabel, S.; Zabel-du Bois, A.; Henze, M.; Huber, P.; Schulz-Ertner, D.; Hoess, A.; Haberkorn, U.; Debus, J. Improved target volume definition for fractionated stereotactic radiotherapy in patients with intracranial meningiomas by correlation of CT, MRI, and [68Ga]-DOTATOC-PET. Int. J. Radiat. Oncol. Biol. Phys., 2006, 65, 222-227.
187. Gehler, B.; Paulsen, F.; Oksuz, M. O.; Hauser, T. K.; Eschmann, S. M.; Bares, R.; Pfannenberg, C.; Bamberg, M.; Bartenstein, P.; Belka, C.; Ganswindt, U. [68Ga]-DOTATOC-PET/CT for meningioma IMRT treatment planning. Radiat. Oncol., 2009, 4, 56.
188. Prasad, V.; Baum, R. P. Biodistribution of the Ga-68 labeled somatostatin analogue DOTA-NOC in patients with neuroendocrine tumors: characterization of uptake in normal organs and tumor lesions. Q. J. Nucl. Med. Mol. Imaging, 2010, 54, 61-67.
189. Ambrosini, V.; Nanni, C.; Zompatori, M.; Campana, D.; Tomassetti, P.; Castellucci, P.; Allegri, V.; Rubello, D.; Montini, G.; Franchi, R.; Fanti, S. Ga-68-DOTA-NOC PET/CT in comparison with CT for the detection of bone metastasis in patients with neuroendocrine tumours. Eur. J. Nucl. Med. Mol. Imag., 2010, 37, 722-727.
190. Campana, D.; Ambrosini, V.; Pezzilli, R.; Fanti, S.; Labate, A. M. M.; Santini, D.; Ceccarelli, C.; Nori, F.; Franchi, R.; Corinaldesi, R.; Tomassetti, P. Standardized Uptake Values of 68Ga-DOTANOC PET: A Promising Prognostic Tool in Neuroendocrine Tumors. J. Nucl. Med., 2010, 51, 353-359.
191. Frilling, A.; Sotiropoulos, G. C.; Radtke, A.; Malago, M.; Bockisch, A.; Kuehl, H.; Li, J.; Broelsch, C. E. The impact of 68Ga-DOTATOC positron emission tomography/computed tomography on the multimodal management of patients with neuroendocrine tumors. Ann. Surg., 2010, 252, 850-856.
192. Versari, A.; Camellini, L.; Carlinfante, G.; Frasoldati, A.; Nicoli, F.; Grassi, E.; Gallo, C.; Giunta, F. P.; Fraternali, A.; Salvo, D.; Asti, M.; Azzolini, F.; Iori, V.; Sassatelli, R. Ga-68 DOTATOC PET, endoscopic ultrasonography, and multidetector CT in the diagnosis of duodenopancreatic neuroendocrine tumors: a singlecentre retrospective study. Clin. Nucl. Med., 2010, 35, 321-328.
193. Van Riet, J.; Rattat, D.; Verbruggen, A.; Mortelmans, L.; Mottaghy, F. M. Ga-68 DOTATOC PET/CT changed the therapeutic course of a patient with the sudden onset of vision problems. Clin. Nucl. Med., 2009, 34, 27-28.
194. Ambrosini, V.; Tomassetti, P.; Castellucci, P.; Campana, D.; Montini, G.; Rubello, D.; Nanni, C.; Rizzello, A.; Franchi, R.; Fanti, S. Comparison between 68Ga-DOTA-NOC and 18F-DOPA PET for the detection of gastro-entero-pancreatic and lung neuroendocrine tumours. Eur. J. Nucl. Med. Mol. Imaging, 2008
195. Sainz-Esteban, A.; Prasad, V.; Baum, R. P. Pancreatic Neuroendocrine Tumor With Involvement of the Inferior Mesenteric Vein Diagnosed by Ga-68 DOTA-TATE PET/CT. Clin. Nucl. Med., 2010, 35, 40-41.
196. Ambrosini, V.; Campana, D.; Allegri, V.; Opocher, G.; Fanti, S. 68Ga-DOTA-NOC PET/CT detects somatostatin receptors expression in von hippel-lindau cerebellar disease. Clin. Nucl. Med., 2011, 36, 64-65.
197. Traub-Weidinger, T.; Von Guggenberg, E.; Dobrozemsky, G.; Kendler, D.; Eisterer, W.; Bale, R.; Putzer, D.; Gabriel, M.; Virgolini, I. Preliminary experience with Ga-68-DOTA-lanreotide positron emission tomography. Q. J. Nucl. Med. Mol. Imaging, 2010, 54, 52-60.
198. Boss, A.; Bisdas, S.; Kolb, A.; Hofmann, M.; Ernemann, U.; Claussen, C. D.; Pfannenberg, C.; Pichler, B. J.; Reimold, M.; Stegger, L. Hybrid PET/MRI of Intracranial Masses: Initial Experiences and Comparison to PET/CT. J. Nucl. Med., 2010, 51, 1198-1205.
199. Henze, M.; Dimitrakopoulou-Strauss, A.; Milker-Zabel, S.; Schuhmacher, J.; Strauss, L. G.; Doll, J.; Macke, H. R.; Eisenhut, M.; Debus, J.; Haberkorn, U. Characterization of 68Ga-DOTA-D-Phe1-Tyr3-Octreotide Kinetics in Patients with Meningiomas. J. Nucl. Med., 2005, 46, 763-769.
200. Luboldt, W.; Zophel, K.; Wunderlich, G.; Abramyuk, A.; Luboldt, H. J.; Kotzerke, J. Visualization of somatostatin receptors in prostate cancer and its bone metastases with Ga-68-DOTATOC PET/CT. Mol. Imaging Biol., 2010, 12, 78-84.
201. Tan, E. H.; Goh, S. W. Exploring new frontiers in molecular imaging: Emergence of Ga PET/CT. World J. Radiol., 2010, 2, 55-67.
202. Ambrosini, V.; Zompatori, M.; De Luca, F.; Antonia, D. E.; Allegri, V.; Nanni, C.; Malvi, D.; Tonveronachi, E.; Fasano, L.; Fabbri, M.; Fanti, S. 68Ga-DOTANOC PET/CT Allows Somatostatin Receptor Imaging in Idiopathic Pulmonary Fibrosis: Preliminary Results. J. Nucl. Med., 2010, 51, 1950-1955.
203. Conry, B. G.; Papathanasiou, N. D.; Prakash, V.; Kayani, I.; Caplin, M.; Mahmood, S.; Bomanji, J. B. Comparison of Ga-68-DOTATATE and F-18-fluorodeoxyglucose PET/CT in the detection of recurrent medullary thyroid carcinoma. Eur. J. Nucl. Med. Mol. Imaging, 2010, 37, 49-57.
204. Lincke, T.; Singer, J.; Kluge, R.; Sabri, O.; Paschke, R. Relative quantification of indium-111 pentetreotide and gallium-68 DOTATOC uptake in the thyroid gland and association with thyroid pathologies. Thyroid, 2009, 19, 381-389.
205. Rominger, A.; Saam, T.; Vogl, E.; Ubleis, C.; la Fougere, C.; Forster, S.; Haug, A.; Cumming, P.; Reiser, M. F.; Nikolaou, K.; Bartenstein, P.; Hacker, M. In Vivo Imaging of Macrophage Activity in the Coronary Arteries Using 68Ga-DOTATATE PET/CT: Correlation with Coronary Calcium Burden and Risk Factors. J. Nucl. Med., 2010, 51, 193-197.
206. Shastry, M.; Kayani, I.; Wild, D.; Caplin, M.; Visvikis, D.; Gacinovic, S.; Reubi, J. C.; Bomanji, J. B. Distribution pattern of Ga-68-DOTATATE in disease-free patients. Nucl. Med. Commun., 2010, 31, 1025-1032.
207. Cotugno, G.; Aurilio, M.; Annunziata, P.; Capalbo, A.; Faella, A.; Rinaldi, V.; Strisciuglio, C.; Tommaso, M. D.; Aloj, L.; Auricchio, A. Noninvasive Repetitive Imaging of Somatostatin Receptor 2 Gene Transfer with Positron Emission Tomography. Hum. Gene Ther., 2011
208. Yarden, Y.; Sliwkowski, M. X. Untangling the ErbB signalling network. Nat. Rev. Mol. Cell Biol., 2001, 2, 127-137. (Pubitemid 33674041)
209. Walker, R. A.; Dearing, S. J. Expression of epidermal growth factor receptor mRNA and protein in primary breast carcinomas. Breast Cancer Res. Treat, 1999, 53, 167-176. (Pubitemid 29161123)
210. Witton, C. J.; Reeves, J. R.; Going, J. J.; Cooke, T. G.; Bartlett, J. M. Expression of the HER1-4 family of receptor tyrosine kinases in breast cancer. J. Pathol., 2003, 200, 290-297. (Pubitemid 36827302)
211. Hirsch, F. R.; Varella-Garcia, M.; Bunn, P. A., Jr.; Di Maria, M. V.; Veve, R.; Bremmes, R. M.; Baron, A. E.; Zeng, C.; Franklin, W. A. Epidermal growth factor receptor in non-small-cell lung carcinomas: correlation between gene copy number and protein expression and impact on prognosis. J. Clin. Oncol., 2003, 21, 3798-3807. (Pubitemid 46606235)
212. Neal, D. E.; Mellon, K. Epidermal growth factor receptor and bladder cancer: a review. Urol. Int., 1992, 48, 365-371.
213. Vosjan, M. J.; Perk, L. R.; Roovers, R. C.; Visser, G. W.; Stigter-van Walsum, M.; van Bergen En Henegouwen, P. M.; van Dongen, G. A. Facile labelling of an anti-epidermal growth factor receptor Nanobody with (68) Ga via a novel bifunctional desferal chelate for immuno-PET. Eur. J. Nucl. Med. Mol. Imaging, 2011
214. Tolmachev, V.; Orlova, A. Update on Affibody molecules for in vivo imaging of targets for cancer therapy. Minerva Biotecnologica, 2009, 21, 21-30.
215. Ahlgren, S.; Tolmachev, V. Radionuclide molecular imaging using Affibody molecules. Curr. Pharm. Biotechnol., 2010, 11, 581-589.
216. Tolmachev, V.; Friedman, M.; Sandstrom, M.; Eriksson, T. L. J.; Rosik, D.; Hodik, M.; Stahl, S.; Frejd, F. Y.; Orlova, A. Affibody Molecules for Epidermal Growth Factor Receptor Targeting In Vivo: Aspects of Dimerization and Labeling Chemistry. J. Nucl. Med., 2009, 50, 274-283.
217. Smith-Jones, P. M.; Solit, D. B.; Akhurst, T.; Afroze, F.; Rosen, N.; Larson, S. M. Imaging the pharmacodynamics of HER2 degradation in response to Hsp90 inhibitors. Nat. Biotechnol., 2004, 22, 701-706. (Pubitemid 38702826)
218. Ren, G.; Zhang, R.; Liu, Z.; Webster, J. M.; Miao, Z.; Gambhir, S. S.; Syud, F. A.; Cheng, Z. A 2-Helix Small Protein Labeled with 68Ga for PET Imaging of HER2 Expression. J. Nucl. Med., 2009, 50, 1492-1499.
219. Theeraladanon, C.; Takahashi, N.; Shiina, M.; Hamada, K.; Takada, Y.; Endo, H.; Tateishi, U.; Oka, T.; Ogata, K.; Inoue, T. Rational Approach to the Synthesis, Evaluation, and 68Ga Labeling of a Novel 4-Anilinoquinoline Epidermal Growth Factor Receptor Inhibitor as a New Imaging Agent That Selectively Targets the Epidermal Growth Factor Receptor Tyrosine Kinase. Cancer Biother. Radiopharm., 2010, 25, 479-485.
220. Campbell, I. D.; Cooke, R. M.; Baron, M.; Harvey, T. S.; Tappin, M. J. The solution structures of epidermal growth factor and transforming growth factor alpha. Prog. Growth Factor Res., 1989, 1, 13-22.
221. Carpenter, G.; Cohen, S. Epidermal growth factor. J. Biol. Chem., 1990, 265, 7709-7712. (Pubitemid 20158927)
222. 68Ga] DOTA hEGF for non-invasive measurement of EGFR expression in tumors using PET. WO/2006/090232, 2006.
223. Baum, R. P.; Prasad, V.; Muller, D.; Schuchardt, C.; Orlova, A.; Wennborg, A.; Tolmachev, V.; Feldwisch, J. Molecular Imaging of HER2-Expressing Malignant Tumors in Breast Cancer Patients Using Synthetic 111In-or 68Ga-Labeled Affibody Molecules. J. Nucl. Med., 2010, 51, 892-897.
224. Smith-Jones, P. M.; Solit, D.; Afroze, F.; Rosen, N.; Larson, S. M. Early Tumor Response to Hsp90 Therapy Using HER2 PET: Comparison with 18F-FDG PET. J. Nucl. Med., 2006, 47, 793-796. (Pubitemid 46768442)
225. Zhang, H. W.; Schuhmacher, J.; Waser, B.; Wild, D.; Eisenhut, M.; Reubi, J. C.; Maecke, H. R. DOTA-PESIN, a DOTA-conjugated bombesin derivative designed for the imaging and targeted radionuclide treatment of bombesin receptor-positive tumours. Eur. J. Nucl. Med. Mol. Imaging, 2007, 34, 1198-1208. (Pubitemid 47296770)
226. Dimitrakopoulou-Strauss, A.; Hohenberger, P.; Haberkorn, U.; Macke, H. R.; Eisenhut, M.; Strauss, L. G. Ga-68-Labeled bombesin studies in patients with gastrointestinal stromal tumors: Comparison with F-18-FDG. J. Nucl. Med., 2007, 48, 1245-1250. (Pubitemid 47242788)
227. Hofmann, M.; Machtens, S.; Stief, C.; Langer, F.; Boerner, A. R.; Maecke, H.; Knapp, W. H. Feasibility of Ga-68-DOTABOM PET in prostate carcinoma patients. Eur. J. Nucl. Med. Mol. Imag., 2004, 31, S253-S253.
228. Baum, R. P.; Prasad, V.; Frischknecht, M.; Maecke, H.; Reubi, J. Bombesin receptor imaging in various tumors: First results of Ga-68 AMBA PET/CT. Eur. J. Nucl. Med. Mol. Imaging, 2007, 34, S193-S193.
229. Mansi, R.; Wang, X.; Forrer, F.; Waser, B.; Cescato, R.; Graham, K.; Borkowski, S.; Reubi, J. C.; Maecke, H. R. Development of a potent DOTA-conjugated bombesin antagonist for targeting GRPrpositive tumours. Eur. J. Nucl. Med. Mol. Imaging, 2011, 38, 97-107.
230. Froidevaux, S.; Calame-Christe, M.; Schuhmacher, J.; Tanner, H.; Saffrich, R.; Henze, M.; Eberle, A. N. A Gallium-Labeled DOTA-{alpha}- Melanocyte-Stimulating Hormone Analog for PET Imaging of Melanoma Metastases. J. Nucl. Med., 2004, 45, 116-123. (Pubitemid 47611617)
231. Cantorias, M. V.; Figueroa, S. D.; Quinn, T. P.; Lever, J. R.; Hoffman, T. J.; Watkinson, L. D.; Carmack, T. L.; Cutler, C. S. Development of high-specific-activity Ga-68-labeled DOTA-rhenium-cyclized alpha-MSH peptide analog to target MC1 receptors overexpressed by melanoma tumors. Nucl. Med. Biol., 2009, 36, 505-513.
232. Wei, L.; Miao, Y.; Gallazzi, F.; Quinn, T. P.; Welch, M. J.; Vavere, A. L.; Lewis, J. S. Gallium-68-labeled DOTA-rhenium-cyclized alpha-melanocyte- stimulating hormone analog for imaging of malignant melanoma. Nucl. Med. Biol., 2007, 34, 945-953. (Pubitemid 350061168)
233. Schmidt, K.; Hoffend, J.; Altmann, A.; Strauss, L. G.; Dimitrakopoulou-Strauss, A.; Engelhardt, B.; Koczan, D.; Peter, J.; Dengler, T. J.; Mier, W.; Eisenhut, M.; Haberkorn, U.; Kinscherf, R. Angiostatin Overexpression in Morris Hepatoma Results in Decreased Tumor Growth but Increased Perfusion and Vascularization. J. Nucl. Med., 2006, 47, 543-551. (Pubitemid 46768498)
234. Hoffend, J.; Mier, W.; Schuhmacher, J.; Schmidt, K.; Dimitrakopoulou- Strauss, A.; Strauss, L. G.; Eisenhut, M.; Kinscherf, R.; Haberkorn, U. Gallium-68-DOTA-albumin as a PET blood-pool marker: experimental evaluation in vivo. Nucl. Med. Biol., 2005, 32, 287-292. (Pubitemid 40488386)
235. Backer, M. V.; Levashova, Z.; Patel, V.; Jehning, B. T.; Claffey, K.; Blankenberg, F. G.; Backer, J. M. Molecular imaging of VEGF receptors in angiogenic vasculature with single-chain VEGF-based probes. Nat. Med., 2007, 13, 504-509. (Pubitemid 46559824)
236. Backer, M. V.; Levashova, Z.; Levenson, R.; Blankenberg, F. G.; Backer, J. M. Cysteine-containing fusion tag for site-specific conjugation of therapeutic and imaging agents to targeting proteins. Methods Mol. Biol, 2008, 494, 275-294.
237. Dijkgraaf, I.; Boerman, O. C. Radionuclide imaging of tumor angiogenesis. Cancer Biother. Radiopharm., 2009, 24, 637-647.
238. Bergstrom, M.; Grahnen, A.; Langstrom, B. Positron emission tomography microdosing: a new concept with application in tracer and early clinical drug development. Eur. J. Clin. Pharmacol., 2003, 59, 357-366. (Pubitemid 37214939)
239. Garner, R. C.; Lappin, G. The phase 0 microdosing concept. Br. J. Clin. Pharmacol., 2006, 61, 367-370.
240. Chen, X.; Park, R.; Shahinian, A. H.; Bading, J. R.; Conti, P. S. Pharmacokinetics and tumor retention of 125I-labeled RGD peptide are improved by PEGylation. Nucl. Med. Biol., 2004, 31, 11-19. (Pubitemid 38115121)
241. Haubner, R.; Kuhnast, B.; Mang, C.; Weber, W. A.; Kessler, H.; Wester, H. J.; Schwaiger, M. [18F]Galacto-RGD: synthesis, radiolabeling, metabolic stability, and radiation dose estimates. Bioconjug. Chem., 2004, 15, 61-69. (Pubitemid 38165981)
242. Janssen, M.; Oyen, W. J.; Massuger, L. F.; Frielink, C.; Dijkgraaf, I.; Edwards, D. S.; Radjopadhye, M.; Corstens, F. H.; Boerman, O. C. Comparison of a monomeric and dimeric radiolabeled RGD-peptide for tumor targeting. Cancer Biother. Radiopharm., 2002, 17, 641-646. (Pubitemid 36025945)
243. Liu, S. Radiolabeled multimeric cyclic RGD peptides as integrin alphavbeta3 targeted radiotracers for tumor imaging. Mol. Pharm., 2006, 3, 472-487. (Pubitemid 44639125)
244. Decristoforo, C.; Hernandez Gonzalez, I.; Carlsen, J.; Rupprich, M.; Huisman, M.; Virgolini, I.; Wester, H. J.; Haubner, R. 68Gaand 111In-labelled DOTA-RGD peptides for imaging of alphavbeta3 integrin expression. Eur. J. Nucl. Med. Mol. Imaging., 2008, 35, 1507-1515.
245. Indrevoll, B.; Kindberg, G. M.; Solbakken, M.; Bjurgert, E.; Johansen, J. H.; Karlsen, H.; Mendizabal, M.; Cuthbertson, A. NC-100717: a versatile RGD peptide scaffold for angiogenesis imaging. Bioorg. Med. Chem. Lett., 2006, 16, 6190-6193. (Pubitemid 44709917)
246. Haukkala, J.; Laitinen, I.; Luoto, P.; Iveson, P.; Wilson, I.; Karlsen, H.; Cuthbertson, A.; Laine, J.; Leppanen, P.; Yla-Herttula, S.; Knuuti, J.; Roivainen, A. (68) Ga-DOTA-RGD peptide: biodistribution and binding into atherosclerotic plaques in mice. Eur. J. Nucl. Med. Mol. Imaging, 2009
247. Liu, Z.; Niu, G.; Shi, J.; Liu, S.; Wang, F.; Chen, X. (68) Ga-labeled cyclic RGD dimers with Gly3 and PEG4 linkers: promising agents for tumor integrin alphavbeta3 PET imaging. Eur. J. Nucl. Med. Mol. Imaging, 2009, 36, 947-957.
248. Li, Z. B.; Chen, K.; Chen, X. (68) Ga-labeled multimeric RGD peptides for microPET imaging of integrin alpha (v) beta (3) expression. Eur. J. Nucl. Med. Mol. Imaging, 2008, 35, 1100-1108.
249. Dijkgraaf, I.; Yim, C. B.; Franssen, G. M.; Schuit, R. C.; Luurtsema, G.; Liu, S.; Oyen, W. J.; Boerman, O. C. PET imaging of alphavbeta integrin expression in tumours with Ga-labelled mono-, di-and tetrameric RGD peptides. Eur. J. Nucl. Med. Mol. Imaging, 2011, 38, 128-137.
250. Ujula, T.; Huttunen, M.; Luoto, P.; Perakyla, H.; Simpura, I.; Wilson, I.; Bergman, M.; Roivainen, A. Matrix Metalloproteinase 9 Targeting Peptides: Syntheses, Ga-68-labeling, and Preliminary Evaluation in a Rat Melanoma Xenograft Model. Bioconjug. Chem., 2010, 21, 1612-1621.
251. Hong, H.; Sun, J.; Cai, W. Radionuclide-based cancer imaging targeting the carcinoembryonic antigen. Biomark Insights, 2008, 3, 435-451.
252. Frangioni, J. V. The problem is background, not signal. Mol. Imaging, 2009, 8, 303-304.
253. Eder, M.; Knackmuss, S.; Le Gall, F.; Reusch, U.; Rybin, V.; Little, M.; Haberkorn, U.; Mier, W.; Eisenhut, M. 68Ga-labelled recombinant antibody variants for immuno-PET imaging of solid tumours. Eur. J. Nucl. Med. Mol. Imaging., 2010, 37, 1397-1407.
254. Chang, C.-H.; Sharkey, R. M.; Rossi, E. A.; Karacay, H.; McBride, W.; Hansen, H. J.; Chatal, J.-F.; Barbet, J.; Goldenberg, D. M. Molecular Advances in Pretargeting Radioimunotherapy with Bispecific Antibodies 1 Supported in part by USPHS Grant R01-CA-84379 from the NIH and Department of Energy Grant DE-FG01-00NE22941 (both to R. M. S.).1. Mol. Cancer Ther., 2002, 1, 553-563.
255. Sharkey, R. M.; Rossi, E. A.; McBride, W. J.; Chang, C. H.; Goldenberg, D. M. Recombinant bispecific monoclonal antibodies prepared by the dock-and-lock strategy for pretargeted radioimmunotherapy. Semin. Nucl. Med., 2010, 40, 190-203.
256. Sharkey, R. M.; Rossi, E. A.; Chang, C. H.; Goldenberg, D. M. Improved cancer therapy and molecular imaging with multivalent, multispecific antibodies. Cancer Biother. Radiopharm., 2010, 25, 1-12.
257. Goldenberg, D. M.; Sharkey, R. M.; Paganelli, G.; Barbet, J.; Chatal, J. F. Antibody pretargeting advances cancer radioimmunodetection and radioimmunotherapy. J. Clin. Oncol., 2006, 24, 823-834. (Pubitemid 46671186)
258. Boerman, O. C.; van Schaijk, F. G.; Oyen, W. J. G.; Corstens, F. H. M. Pretargeted Radioimmunotherapy of Cancer: Progress Step by Step. J. Nucl. Med., 2003, 44, 400-411. (Pubitemid 39586017)
259. Schuhmacher, J.; Kaul, S.; Klivenyi, G.; Junkermann, H.; Magener, A.; Henze, M.; Doll, J.; Haberkorn, U.; Amelung, F.; Bastert, G. Immunoscintigraphy with positron emission tomography: gallium-68 chelate imaging of breast cancer pretargeted with bispecific anti-MUC1/anti-Ga chelate antibodies. Cancer Res, 2001, 61, 3712-3717. (Pubitemid 32694984)
260. Schuhmacher, J.; Klivenyi, G.; Kaul, S.; Henze, M.; Matys, R.; Hauser, H.; Clorius, J. Pretargeting of human mammary carcinoma xenografts with bispecific anti-MUC1/anti-Ga chelate antibodies and immunoscintigraphy with PET. Nucl. Med. Biol., 2001, 28, 821-828. (Pubitemid 32900640)
261. Somasundaram, C.; Matzku, S.; Schuhmacher, J.; Zöller, M. Development of a bispecific monoclonal antibody against a gallium-67 chelate and the human melanoma-associated antigen p97 for potential use in pretargeted immunoscintigraphy. Cancer Immunol. Immunother., 1993, 36, 337-345. (Pubitemid 23106004)
262. Rossi, E. A.; Rossi, D. L.; Stein, R.; Goldenberg, D. M.; Chang, C. H. A bispecific antibody-IFNalpha2b immunocytokine targeting CD20 and HLA-DR is highly toxic to human lymphoma and multiple myeloma cells. Cancer Res., 2010, 70, 7600-7609.
263. Sharkey, R. M.; Karacay, H.; Litwin, S.; Rossi, E. A.; McBride, W. J.; Chang, C. H.; Goldenberg, D. M. Improved therapeutic results by pretargeted radioimmunotherapy of non-Hodgkin's lymphoma with a new recombinant, trivalent, anti-CD20, bispecific antibody. Cancer Res., 2008, 68, 5282-5290.
264. Griffiths, G. L.; Chang, C. H.; McBride, W. J.; Rossi, E. A.; Sheerin, A.; Tejada, G. R.; Karacay, H.; Sharkey, R. M.; Horak, I. D.; Hansen, H. J.; Goldenberg, D. M. Reagents and methods for PET using bispecific antibody pretargeting and 68Ga-radiolabeled bivalent hapten-peptide-chelate conjugates. J. Nucl. Med., 2004, 45, 30-39. (Pubitemid 47611605)
265. Watine, J.; Miedouge, M.; Friedberg, B. Carcinoembryonic antigen as an independent prognostic factor of recurrence and survival in patients resected for colorectal liver metastases: a systematic review. Dis. Colon Rectum., 2001, 44, 1791-1799. (Pubitemid 34031435)
266. Goldstein, M. J.; Mitchell, E. P. Carcinoembryonic antigen in the staging and follow-up of patients with colorectal cancer. Cancer Invest., 2005, 23, 338-351. (Pubitemid 41656973)
267. Gold, D. V.; Goldenberg, D. M.; Karacay, H.; Rossi, E. A.; Chang, C. H.; Cardillo, T. M.; McBride, W. J.; Sharkey, R. M. A novel bispecific, trivalent antibody construct for targeting pancreatic carcinoma. Cancer Res., 2008, 68, 4819-4826.
268. Forster, G. J.; Santos, E. B.; Smith-Jones, P. M.; Zanzonico, P.; Larson, S. M. Pretargeted Radioimmunotherapy with a Single-Chain Antibody/Streptavidin Construct and Radiolabeled DOTA-Biotin: Strategies for Reduction of the Renal Dose. J. Nucl. Med., 2006, 47, 140-149. (Pubitemid 46768523)
269. Schuhmacher, J.; Klivényi, G.; Matys, R.; Stadler, M.; Regiert, T.; Hauser, H.; Doll, J.; Maier-Borst, W.; Zöller, M. Multistep Tumor Targeting in Nude Mice Using Bispecific Antibodies and a Gallium Chelate Suitable for Immunoscintigraphy with Positron Emission Tomography. Cancer Res., 1995, 55, 115-123.
270. Klivenyi, G.; Schuhmacher, J.; Patzelt, E.; Hauser, H.; Matys, R.; Moock, M.; Regiert, T.; Maier-Borst, W. Gallium-68 Chelate Imaging of Human Colon Carcinoma Xenografts Pretargeted with Bispecific Anti-CD44V6/Anti-Gallium Chelate Antibodies. J. Nucl. Med., 1998, 39, 1769-1776. (Pubitemid 28473528)
271. Zoller, M.; Schuhmacher, J.; Reed, J.; Maier-Borst, W.; Matzku, S. Establishment and Characterization of Monoclonal Antibodies Against an Octahedral Gallium Chelate Suitable for Immunoscintigraphy with PET. J. Nucl. Med., 1992, 33, 1366-1372.
272. Sharkey, R. M.; Cardillo, T. M.; Rossi, E. A.; Chang, C. H.; Karacay, H.; McBride, W. J.; Hansen, H. J.; Horak, I. D.; Goldenberg, D. M. Signal amplification in molecular imaging by pretargeting a multivalent, bispecific antibody. Nat. Med., 2005, 11, 1250-1255. (Pubitemid 43093674)
273. Goldenberg, D. M.; Sharkey, R. M. Novel radiolabeled antibody conjugates. Oncogene, 2007, 26, 3734-3744. (Pubitemid 46842708)
274. Goldenberg, D. M.; Rossi, E. A.; Sharkey, R. M.; McBride, W. J.; Chang, C. H. Multifunctional antibodies by the Dock-and-Lock method for improved cancer imaging and therapy by pretargeting. J. Nucl. Med., 2008, 49, 158-163.
275. Schoffelen, R.; Sharkey, R. M.; Goldenberg, D. M.; Franssen, G.; McBride, W. J.; Rossi, E. A.; Chang, C. H.; Laverman, P.; Disselhorst, J. A.; Eek, A.; van der Graaf, W. T.; Oyen, W. J.; Boerman, O. C. Pretargeted immuno-positron emission tomography imaging of carcinoembryonic antigen-expressing tumors with a bispecific antibody and a 68Ga-and 18F-labeled hapten peptide in mice with human tumor xenografts. Mol. Cancer Ther., 2010, 9, 1019-1027.
276. Kumaresan, P. R.; Natarajan, A.; Song, A. M.; Wang, X. B.; Liu, R. W.; DeNardo, G.; DeNardo, S.; Lam, K. S. Development of tissue plasminogen activator specific "on demand cleavable" (ODC) linkers for radioimmunotherapy by screening one-bead-onecompound combinatorial peptide libraries. Bioconjug. Chem., 2007, 18, 175-182. (Pubitemid 46146008)
277. Chapman, J. D.; Baer, K.; Lee, J. Characteristics of the metabolisminduced binding of misonidazole to hypoxic mammalian-cells. Cancer Res., 1983, 43, 1523-1528. (Pubitemid 13122542)
278. Hoigebazar, L.; Jeong, J. M.; Choi, S. Y.; Choi, J. Y.; Shetty, D.; Lee, Y. S.; Lee, D. S.; Chung, J. K.; Lee, M. C.; Chung, Y. K. Synthesis and characterization of nitroimidazole derivatives for 68Ga-labeling and testing in tumor xenografted mice. J. Med. Chem., 2010, 53, 6378-6385.
279. Mukai, T.; Suwada, J.; Sano, K.; Okada, M.; Yamamoto, F.; Maeda, M. Design of Ga-DOTA-based bifunctional radiopharmaceuticals: Two functional moieties can be conjugated to radiogallium-DOTA without reducing the complex stability. Bioorg. Med. Chem., 2009, 17, 4285-4289.
280. Yang, B. Y.; Jeong, J. M.; Kim, Y. J.; Choi, J. Y.; Lee, Y. S.; Lee, D. S.; Chung, J. K.; Lee, M. C. Formulation of 68Ga BAPEN kit for myocardial positron emission tomography imaging and biodistribution study. Nucl. Med. Biol., 2010, 37, 149-155.
281. Tsang, B. W.; Mathias, C. J.; Green, M. A. A gallium-68 radiopharmaceutical that is retained in myocardium: 68Ga[(4, 6-MeO2sal) 2BAPEN]+. J. Nucl. Med., 1993, 34, 1127-1131. (Pubitemid 23191329)
282. Hsiao, Y. M.; Mathias, C. J.; Wey, S. P.; Fanwick, P. E.; Green, M. A. Synthesis and biodistribution of lipophilic and monocationic gallium radiopharmaceuticals derived from N, N'-bis (3-aminopropyl)-N, N'-dimethylethylenediamine: potential agents for PET myocardial imaging with Ga-68. Nucl. Med. Biol., 2009, 36, 39-45.
283. Plossl, K.; Chandra, R.; Qua, W. C.; Lieberman, B. P.; Kung, M. P.; Zhou, R.; Huang, B.; Kung, H. F. A novel gallium bisaminothiolate complex as a myocardial perfusion imaging agent. Nucl. Med. Biol., 2008, 35, 83-90. (Pubitemid 350298244)
284. Cutler, C. S.; Giron, M. C.; Reichert, D. E.; Snyder, A. Z.; Herrero, P.; Anderson, C. J.; Quarless, D. A.; Koch, S. A.; Welch, M. J. Evaluation of gallium-68 tris (2-mercaptobenzyl) amine: a complex with brain and myocardial uptake. Nucl. Med. Biol., 1999, 26, 305-316. (Pubitemid 29179874)
285. Zhang, Z.; Lyster, D. M.; Webb, G. A.; Orvig, C. Potential 67Ga radiopharmaceuticals for myocardial imaging: tris (1-aryl-3-hydroxy-2-methyl-4- pyridinonato) gallium (III) complexes. Int. J. Rad. Appl. Instrum. B, 1992, 19, 327-335.
286. Fellner, M.; Baum, R. P.; Kubicek, V.; Hermann, P.; Lukes, I.; Prasad, V.; Rosch, F. PET/CT imaging of osteoblastic bone metastases with Ga-68-bisphosphonates: first human study. Eur. J. Nucl. Med. Mol. Imaging, 2010, 37, 834-834.
287. Toegel, S.; Wadsak, W.; Mien, L. K.; Viernstein, H.; Kluger, R.; Eidherr, H.; Haeusler, D.; Kletter, K.; Dudczak, R.; Mitterhauser, M. Preparation and pre-vivo evaluation of no-carrier-added, carrier-added and cross-complexed Ga-68-EDTMP formulations. Eur. J. Pharm. Biopharm., 2008, 68, 406-412.
288. Mitterhauser, M.; Toegel, S.; Wadsak, W.; Lanzenberger, R. R.; Mien, L. K.; Kuntner, C.; Wanek, T.; Eidherr, H.; Ettlinger, D. E.; Viernstein, H.; Kluger, R.; Dudczak, R.; Kletter, K. Pre vivo, ex vivo and in vivo evaluations of Ga-68-EDTMP. Nucl. Med. Biol., 2007, 34, 391-397.
289. Shetty, D.; Jeong, J. M.; Ju, C. H.; Lee, Y. S.; Jeong, S. Y.; Choi, J. Y.; Yang, B. Y.; Lee, D. S.; Chung, J. K.; Lee, M. C. Synthesis of novel 68Ga-labeled amino acid derivatives for positron emission tomography of cancer cells. Nucl. Med. Biol., 2010, 37, 893-902.
290. Shetty, D.; Jeong, J. M.; Ju, C. H.; Kim, Y. J.; Lee, J. Y.; Lee, Y. S.; Lee, D. S.; Chung, J. K.; Lee, M. C. Synthesis and evaluation of macrocyclic amino acid derivatives for tumor imaging by gallium-68 positron emission tomography. Bioorg. Med. Chem., 2010, 18, 7338-7347.
291. Burchardt, C.; Riss, P. J.; Zoller, F.; Maschauer, S.; Prante, O.; Kuwert, T.; Roesch, F. Ga-68 Ga-DO (2) A-(OBu-L-tyr) (2): Synthesis, Ga-68-radiolabeling and in vitro studies of a novel Ga-68-DO (2) A-tyrosine conjugate as potential tumor tracer for PET. Bioorg. Med. Chem. Lett., 2009, 19, 3498-3501.
292. Ito, M.; Yang, D. J.; Mawlawi, O.; Mendez, R.; Oh, C. S.; Azhdarinia, A.; Greenwell, A. C.; Yu, D. F.; Kim, E. E. PET and planar imaging of tumor hypoxia with labeled metronidazole. Acad Radiol., 2006, 13, 598-609.
293. Yang, D. J.; Kim, E. E. Tracer development and hybrid imaging. Eur. J. Nucl. Med. Mol. Imaging, 2005, 32, 1001-1002. (Pubitemid 41339273)
294. Yang, D. J.; Azhdarinia, A.; Kim, E. E. Tumor Specific Imaging Using Tc-99m and Ga-68 Labeled Radiopharmaceuticals. Curr. Med. Imag. Rev., 2005, 1, 25-34.
295. Tavitian, B. Oligonucleotides as radiopharmaceuticals. Ernst Schering Res Found Workshop, 2005, 1-34.
296. Lendvai, G.; Estrada, S.; Bergstrom, M. Radiolabelled oligonucleotides for imaging of gene expression with PET. Curr. Med. Chem., 2009, 16, 4445-4461.
297. Schuster, D. P. The evaluation of lung function with PET. Sem. Nucl. Med., 1998, 28, 341-351. (Pubitemid 28478047)
298. Wagner, S. J.; Welch, M. J. Gallium-68 labeling of albumin and albumin microspheres. J. Nucl. Med., 1979, 20, 428-433.
299. Yvert, J. P.; Maziere, B.; Verhas, M.; Comar, D. Simple, fast preparation of gallium-68-labeled human-serum albumin microspheres. Eur. J. Nucl. Med., 1979, 4, 95-99. (Pubitemid 9218284)
300. Hayes, R. L.; Carlton, J. E.; Kuniyasu, Y. A new method for labeling microspheres with 68Ga. Eur. J. Nucl. Med., 1981, 6, 531-533. (Pubitemid 12238114)
301. Steinling, M.; Baron, J. C.; Maziere, B.; Lasjaunias, P.; Loc'h, C.; Cabanis, E. A.; Guillon, B. Tomographic measurement of cerebral blood flow by the 68Ga-labelledmicrosphere and continuous- C15O2-inhalation methods. Eur. J. Nucl. Med. Mol. Imaging, 1985, 11, 29-32. (Pubitemid 15005162)
302. Chesler, D. A.; Hales, C.; Hnatowich, D. J.; Hoop, B. 3-dimensional reconstruction of lung perfusion image with positron detection. J. N. Med., 1975, 16, 80-82.
303. Mintun, M. A.; Terpogossian, M. M.; Green, M. A.; Lich, L. L.; Schuster, D. P. Quantitative measurement of regional pulmonary blood-flow with positron emission tomography. J. Appl. Physiol., 1986, 60, 317-326. (Pubitemid 16024052)
304. Even, G. A.; Green, M. A. Gallium-68-labeled macroaggregated human serum albumin, 68Ga-MAA. Int. J. Rad. Appl. Instrum. Part B. Nucl. Med. Biol., 1989, 16, 319-321. (Pubitemid 19094766)
305. Mathias, C. J.; Green, M. A. A convenient route to Ga-68 Ga-MAA for use as a particulate PET perfusion tracer. Appl. Rad. Isot., 2008, 66, 1910-1912.
306. Maziere, B.; Loc'h, C.; Steinling, M.; Comar, D. Stable labelling of serum albumin microspheres with gallium-68. Int. J. Rad. Appl. Instrum. A, 1986, 37, 360-361. (Pubitemid 16099408)
307. Maus, S.; Buchholz, H.-G.; Ament, S.; Brochhausen, C.; Bausbacher, N.; Schreckenberger, M. Labelling of commercially available human serum albumin kits with 68Ga as surrogates for 99mTc-MAA microspheres. Appl. Rad. Isotopes, 2011, 69, 171-175.
308. Wunderlich, G.; Schiller, E.; Bergmann, R.; Pietzsch, H.-J. Comparison of the stability of Y-90-, Lu-177-and Ga-68-labeled human serum albumin microspheres (DOTA-HSAM). Nucl. Med. Biol., 2010, 37, 861-867.
309. Schiller, E.; Bergmann, R.; Pietzsch, J.; Noll, B.; Sterger, A.; Johannsen, B.; Wunderlich, G.; Pietzsch, H. J. Yttrium-86-labelled human serum albumin microspheres: relation of surface structure with in vivo stability. Nucl. Med. Biol., 2008, 35, 227-232.
310. Richter, T.; Bergmann, R.; Pietzsch, J.; Kozle, I.; Hofheinz, F.; Schiller, E.; Ragaller, M.; van den Hoff, J. Effects of posture on regional pulmonary blood flow in rats as measured by PET. J. Appl. Phys., 2010, 108, 422-429.
311. Schuster, D. P.; Kaplan, J. D.; Gauvain, K.; Welch, M. J.; Markham, J. Measurement of regional pulmonary blood-flow with PET. J. Nucl. Med., 1995, 36, 371-377.
312. Beller, G. A.; Alton, W. J.; Cochavi, S.; Hnatowich, D.; Brownell, G. L. Assessment of regional myocardial perfusion by positron emission tomography after intra-coronary administration of ga-68 labeled albumin microspheres. J. Comput. Assist. Tomograp., 1979, 3, 447-452. (Pubitemid 9218359)
313. Jain, R.; Dandekar, P.; Patravale, V. Diagnostic nanocarriers for sentinel lymph node imaging. J. Cont. Release, 2009, 138, 90-102.
314. Hwang, D. W.; Ko, H. Y.; Lee, J. H.; Kang, H.; Ryu, S. H.; Song, I. C.; Lee, D. S.; Kim, S. A Nucleolin-Targeted Multimodal Nanoparticle Imaging Probe for Tracking Cancer Cells Using an Aptamer. J. Nucl. Med., 2010, 51, 98-105.
315. Borges, J. B.; Velikyan, I.; Långström, B.; Sörensen, J.; Ulin, J.; Maripuu, E.; Sandström, M.; Widström, C.; Hedenstierna, G. Ventilation distribution studies comparing Technegas and Gallgas using 68GaCl3 as the label. J. Nucl. Med., 2011, 52, 206-209.
316. Kotzerke, J.; Andreeff, M.; Wunderlich, G. PET aerosol lung scintigraphy using Galligas. Eur. J. Nucl. Med. Mol. Imaging, 2010, 37, 175-177.
317. Banerjee, S. R.; Pullambhatla, M.; Byun, Y.; Nimmagadda, S.; Green, G.; Fox, J. J.; Horti, A.; Mease, R. C.; Pomper, M. G. Ga-68-Labeled Inhibitors of Prostate-Specific Membrane Antigen (PSMA) for Imaging Prostate Cancer. J. Med. Chem., 2010, 53, 5333-5341.
318. Ujula, T.; Salomaki, S.; Autio, A.; Luoto, P.; Tolvanen, T.; Lehikoinen, P.; Viljanen, T.; Sipila, H.; Harkonen, P.; Roivainen, A. Ga-68-Chloride PET Reveals Human Pancreatic Adenocarcinoma Xenografts in Rats-Comparison with FDG. Mol. Imag. Biol., 2010, 12, 259-268.
319. Brom, M.; Oyen, W. J.; Joosten, L.; Gotthardt, M.; Boerman, O. C. 68Ga-labelled exendin-3, a new agent for the detection of insulinomas with PET. Eur. J. Nucl. Med. Mol. Imaging, 2010, 37, 1345-1355.
320. Wild, D.; Wicki, A.; Mansi, R.; Behe, M.; Keil, B.; Bernhardt, P.; Christofori, G.; Ell, P. J.; Macke, H. R. Exendin-4-Based Radiopharmaceuticals for Glucagonlike Peptide-1 Receptor PET/CT and SPECT/CT. J. Nucl. Med., 2010, 51, 1059-1067.
321. Schottelius, M.; Berger, S.; Poethko, T.; Schwaiger, M.; Wester, H. J. Development of novel Ga-68-and F-18-labeled GnRH-I analogues with high GnRHR-targeting efficiency. Bioconjug. Chem., 2008, 19, 1256-1268. (Pubitemid 351874949)
322. Demmer, O.; Dijkgraaf, I.; Schottelius, M.; Wester, H. J.; Kessler, H. Introduction of functional groups into peptides via N-alkylation. Org. Lett., 2008, 10, 2015-2018.
323. Mathias, C. J.; Lewis, M. R.; Reichert, D. E.; Laforest, R.; Sharp, T. L.; Lewis, J. S.; Yang, Z. F.; Waters, D. J.; Snyder, P. W.; Low, P. S.; Welch, M. J.; Green, M. A. Preparation of 66Ga-and 68Galabeled Ga (III)-deferoxamine- folate as potential folate-receptortargeted PET radiopharmaceuticals. Nucl. Med. Biol., 2003, 30, 725-731. (Pubitemid 37123129)
324. Fani, M.; Wang, X.; Nicolas, G.; Medina, C.; Raynal, I.; Port, M.; Maecke, H. R. Development of new folate-based PET radiotracers: preclinical evaluation of Ga-DOTA-folate conjugates. Eur. J. Nucl. Med. Mol. Imaging, 2011, 38, 108-119.
325. Maschauer, S.; Einsiedel, J.; Hocke, C.; Hubner, H.; Kuwert, T.; Gmeiner, P.; Prante, O. Synthesis of a Ga-68-Labeled Peptoid-Peptide Hybrid for Imaging of Neurotensin Receptor Expression in Vivo. Acs Med. Chem. Lett., 2010, 1, 224-228.
326. Prinsen, K.; Li, J. J.; Vanbilloen, H.; Vermaelen, P.; Devos, E.; Mortelmans, L.; Bormans, G.; Ni, Y. C.; Verbruggen, A. Development and evaluation of a Ga-68 labeled pamoic acid derivative for in vivo visualization of necrosis using positron emission tomography. Bioorg. Med. Chem., 2010, 18, 5274-5281.
327. Liu, Z. F.; Yan, Y. J.; Liu, S. L.; Wang, F.; Chen, X. Y. F-18, Cu-64, and Ga-68 Labeled RGD-Bombesin Heterodimeric Peptides for PET Imaging of Breast Cancer. Bioconjug. Chem., 2009, 20, 1016-1025.
328. Liu, Z.; Niu, G.; Wang, F.; Chen, X. (68) Ga-labeled NOTA-RGD-BBN peptide for dual integrin and GRPR-targeted tumor imaging. Eur. J. Nucl. Med. Mol. Imaging, 2009, 36, 1483-1494.
329. Sharma, V.; Prior, J. L.; Belinsky, M. G.; Kruh, G. D.; Piwnica-Worms, D. Characterization of a 67Ga/68Ga radiopharmaceutical for SPECT and PET of MDR1 P-glycoprotein transport activity in vivo: validation in multidrug-resistant tumors and at the bloodbrain barrier. J. Nucl. Med., 2005, 46, 354-364. (Pubitemid 43073447)
330. Thews, O.; Dillenburg, W.; Fellner, M.; Buchholz, H. G.; Bausbacher, N.; Schreckenberger, M.; Rosch, F. Activation of P-glycoprotein (Pgp)-mediated drug efflux by extracellular acidosis: in vivo imaging with Ga-68-labelled PET tracer. Eur. J. Nucl. Med. Mol. Imaging, 2010, 37, 1935-1942.
331. Lankinen, P.; Maekinen, T. J.; Poeyhoenen, T. A.; Virsu, P.; Salomaeki, S.; Hakanen, A. J.; Jalkanen, S.; Aro, H. T.; Roivainen, A. Ga-68-DOTAVAP-P1 PET imaging capable of demonstrating the phase of inflammation in healing bones and the progress of infection in osteomyelitic bones. Eur. J. Nucl. Med. Mol. Imaging, 2008, 35, 352-364.
332. Autio, A.; Ujula, T.; Luoto, P.; Salomaki, S.; Jalkanen, S.; Roivainen, A. PET imaging of inflammation and adenocarcinoma xenografts using vascular adhesion protein 1 targeting peptide 68Ga-DOTAVAP-P1: comparison with 18F-FDG. Eur. J. Nucl. Med. Mol. Imaging, 2010, 37, 1918-1925.
333. Silvola, J.; Autio, A.; Luoto, P.; Jalkanen, S.; Roivainen, A. Preliminary evaluation of novel 68Ga-DOTAVAP-PEG-P2 peptide targeting vascular adhesion protein-1. Clin. Physiol. Funct. Imaging, 2010, 30, 75-78.
334. Ujula, T.; Salomaki, S.; Virsu, P.; Lankinen, P.; Makinen, T. J.; Autio, A.; Yegutkin, G. G.; Knuuti, J.; Jalkanen, S.; Roivainen, A. Synthesis, Ga-68 labeling and preliminary evaluation of DOTA peptide binding vascular adhesion protein-1: a potential PET imaging agent for diagnosing osteomyelitis. Nucl. Med. Biol., 2009, 36, 631-641.
335. Makinen, T. J.; Lankinen, P.; Poyhonen, T.; Jalava, J.; Aro, H. T.; Roivainen, A. Comparison of F-18-FDG and Ga-68 PET imaging in the assessment of experimental osteomyelitis due to Staphylococcus aureus. Eur. J. Nucl. Med. Mol. Imaging, 2005, 32, 1259-1268. (Pubitemid 41598716)
336. Petrik, M.; Haas, H.; Dobrozemsky, G.; Lass-Florl, C.; Helbok, A.; Blatzer, M.; Dietrich, H.; Decristoforo, C. 68Ga-Siderophores for PET Imaging of Invasive Pulmonary Aspergillosis: Proof of Principle. J. Nucl. Med., 2010, 51, 639-645.
337. Nanni, C.; Errani, C.; Boriani, L.; Fantini, L.; Ambrosini, V.; Boschi, S.; Rubello, D.; Pettinato, C.; Mercuri, M.; Gasbarrini, A.; Fanti, S. 68Ga-Citrate PET/CT for Evaluating Patients with Infections of the Bone: Preliminary Results. J. Nucl. Med., 2010, 51, 1932-1936.
338. Welch, M. J.; Thakur, M. L.; Coleman, R. E.; Patel, M.; Siegel, B. A.; Ter-Pogossian, M. M. Gallium-68 Labeled Red Cells and Platelets New Agents for Positron Tomography. J. Nucl. Med., 1977, 18, 558-562. (Pubitemid 8128897)
339. Yano, Y.; Budinger, T. F.; Ebbe, S. N.; Mathis, C. A.; Singh, M.; Brennan, K. M.; Moyer, B. R. Gallium-68 Lipophilic Complexes for Labeling Platelets. J. Nucl. Med., 1985, 26, 1429-1437. (Pubitemid 16063026)
340. Mintun, M. A.; Dennis, D. R.; Welch, M. J.; Mathias, C. J.; Schuster, D. P. Measurements of Pulmonary Vascular Permeability with PET and Gallium-68 Transferrin. J. Nucl. Med., 1987, 28, 1704-1716. (Pubitemid 17160289)
341. Schuster, D. P.; Stark, T.; Stephenson, J.; Royal, H. Detecting lung injury in patients with pulmonary edema. Intensive Care Med., 2002, 28, 1246-1253. (Pubitemid 35025041)
342. Schuhmacher, J.; Maier-Borst, W.; Wellman, H. N. Liver and Kidney Imaging with Ga-68-Labeled Dihydroxyanthraquinones. J. Nucl. Med., 1980, 21, 983-987. (Pubitemid 10010847)
343. Szabo, Z.; Xia, J.; Mathews, W. B. Radiopharmaceuticals for renal positron emission tomography imaging. Semin. Nucl. Med., 2008, 38, 20-31. (Pubitemid 350256719)
344. Schuhmacher, J.; Matys, R.; Hauser, H.; Clorius, J. H.; Maier-Borst, W. A Ga-68-labeled tetrabromophthalein (Ga-68 BP-IDA) for positron imaging of hepatobiliary function: concise communication. J. Nucl. Med., 1983, 24, 593-602. (Pubitemid 13049711)
345. Moerlein, S. M.; Daugherty, A.; Sobel, B. E.; Welch, M. J. Metabolic Imaging with Gallium-68-and Indium-111-Labeled Low-Density Lipoprotein. J. Nucl. Med., 1991, 32, 300-307.
346. Stoll, H.-P.; Hutchins, G. D.; Winkle, W. L.; Nguyen, A. T.; Appledorn, C. R.; Janzen, I.; Seifert, H.; Rube, C.; Schieffer, H.; March, K. L. Advantages of Short-Lived Positron-Emitting Radioisotopes for Intracoronary Radiation Therapy with Liquid-Filled Balloons to Prevent Restenosis. J. Nucl. Med., 2001, 42, 1375-1383. (Pubitemid 32852614)
347. de Jong, M.; Breeman, W. A.; Bernard, B. F.; van Gameren, A.; de Bruin, E.; Bakker, W. H.; van der Pluijm, M. E.; Visser, T. J.; Macke, H. R.; Krenning, E. P. Tumour uptake of the radiolabelled somatostatin analogue [DOTA0, TYR3]octreotide is dependent on the peptide amount. Eur. J. Nucl. Med., 1999, 26, 693-698. (Pubitemid 29338656)
348. Bernhardt, P.; Kolby, L.; Johanson, V.; Nilsson, O.; Ahlman, H.; Forssell-Aronsson, E. Biodistribution of 111in-DTPA-D-Phe1-octreotide in tumor-bearing nude mice: influence of amount injected and route of administration. Nucl. Med. Biol., 2003, 30, 253-260. (Pubitemid 36556240)
349. Lappin, G.; Kuhnz, W.; Jochemsen, R.; Kneer, J.; Chaudhary, A.; Oosterhuis, B.; Drijfhout, W. J.; Rowland, M.; Garner, R. C. Use of microdosing to predict pharmacokinetics at the therapeutic dose: Experience with 5 drugs. Clin. Pharmacol. Ther., 2006, 80, 203-215. (Pubitemid 44313903)
350. Marchetti, S.; Schellens, J. H. M. The impact of FDA and EMEA guidelines on drug development in relation to Phase 0 trials. Br. J. Cancer, 2007, 97, 577-581. (Pubitemid 47339894)
351. Deutsch, E. Clinical PET: Its Time Has Come? J. Nucl. Med., 1993, 34, 1132-1133. (Pubitemid 23191330)