Trifunctional somatostatin-based derivatives designed for targeted radiotherapy using Auger electron emitters

Journal of Nuclear Medicine

Volumn 46, Issue 12, 2005, Pages 2097-2103

  Ginj, Mihaela ^a   Hinni, Karin ^a   Tschumi, Sibylle ^a   Schulz, Stefan ^b   Maecke, Helmut R ^a  

^a UNIVERSITY HOSPITAL BASEL   (Switzerland)

^b OTTO VON GUERICKE UNIVERSITY   (Germany)

Author keywords

111In; Auger electron emitter; Nuclear localization signal; Nuclear uptake

Indexed keywords

[(1,4,7,10 TETRAAZACYCLODODECANE 1,4,7,10 TETRAACETIC ACID)TYROSINE 3] OCTREOTIDE; [(1,4,7,10 TETRAAZACYCLODODECANE 1,4,7,10 TETRAACETIC ACID)TYROSINE 3] OCTREOTIDE IN 111; DNA; INDIUM 111; RADIOISOTOPE; SOMATOSTATIN DERIVATIVE; UNCLASSIFIED DRUG; VIRUS LARGE T ANTIGEN; (DOTA(0) PHE(1) TYR(3))OCTREOTIDE; (DOTA(0)-PHE(1)-TYR(3))OCTREOTIDE; DRUG DERIVATIVE; G PROTEIN COUPLED RECEPTOR; INDIUM; OCTREOTIDE; PEPTIDE; SOMATOSTATIN;

AMINO ACID SEQUENCE; AMINO TERMINAL SEQUENCE; ANIMAL CELL; ARTICLE; AUGER ELECTRON SPECTROSCOPY; BINDING AFFINITY; CARBOXY TERMINAL SEQUENCE; CELL NUCLEUS; CONJUGATION; CONTROLLED STUDY; DRUG DESIGN; DRUG SYNTHESIS; DRUG TARGETING; EMBRYO CELL; HUMAN; HUMAN CELL; IN VITRO STUDY; ISOTOPE LABELING; NONHUMAN; NUCLEAR LOCALIZATION SIGNAL; PRIORITY JOURNAL; RAT; SIMIAN VIRUS; SOLID PHASE SYNTHESIS; CELL LINE; CHEMISTRY; ELECTRON; GENETIC TRANSFECTION; KINETICS; METABOLISM; METHODOLOGY; NEOPLASM; PROTEIN TERTIARY STRUCTURE; RADIOTHERAPY; TIME;

CELL LINE; CELL NUCLEUS; ELECTRONS; HUMANS; INDIUM RADIOISOTOPES; KINETICS; NEOPLASMS; OCTREOTIDE; PEPTIDES; PROTEIN STRUCTURE, TERTIARY; RADIOISOTOPES; RADIOTHERAPY; RECEPTORS, G-PROTEIN-COUPLED; SOMATOSTATIN; TIME FACTORS; TRANSFECTION;

EID: 33644874270     PISSN: 01615505     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (34)

1. Reubi JC, Waser B, Schae JC, Laissue JA. Somatostatin receptor sst1-sst5 expression in normal and neoplastic human tissues using receptor autoradiography with subtype-selective ligands. Eur J Nucl Med. 2001;28:836-846.
2. Otte A, Mueller-Brand J, Dellas S, Nitzsche E, Herrmann R, Maecke HR. Yttrium-90-labelled somatostatin-analogue for cancer treatment. Lancet. 1998; 351:417-418.
3. 90Y-DOTATOC) in neuroendocrine tumours. Eur J Nucl Med Mol Imaging. 2004;31:38-46.
4. O'Donoghue JA, Bardies M, Wheldon TE. Relationship between tumor size and curability for uniformly targeted therapy with beta-emitting radionuclides. J Nucl Med. 1995;36:1902-1909.
5. 3]octreotide radionuclide therapy in a transplantable rat tumor model is dependent on tumor size. J Nucl Med. 2001;42:1841-1846.
6. Behr T, Behe M, Lohr M, et al. Therapeutic advantages of Auger electron- over beta-emitting radiometals or radioiodine when conjugated to internalizing antibodies. Eur J Nucl Med. 2000;27:753-765.
7. 131I-labeled CO17-1A in a human colorectal cancer model. Int J Cancer. 1998;76:738-748.
8. Michel R, Castillo ME, Andrews PM, Mattes MJ. In vitro toxicity of A-431 carcinoma cells with antibodies to epidermal growth factor receptor and epithelial glycoprotein-1 conjugated to radionuclides emitting low-energy electrons. Clin Cancer Res. 2004;10:5957-5966.
9. Michel R, Rosario AV, Andrews PM, Goldenberg DM, Mattes MJ. Therapy of small subcutaneous B-lymphoma xenografts with antibodies conjugated to radionuclides emitting low-energy electrons. Clin Cancer Res. 2005;11:777-786.
10. Michel R, Brechbiel MW, Mattes MJ. A comparison of 4 radionuclides conjugated to antibodies for single-cell kill. J Nucl Med. 2003;44:632-640.
11. Govindan S, Goldenberg DM, Elsamra SE, et al. Radionuclides linked to a CD74 antibody as therapeutic agents for B-cell lymphoma: comparison of Auger electron emitters with beta-particle emitters. J Nucl Med. 2000;41:2089-2097.
12. Valkema R, De Jong M, Bakker WH, et al. Phase 1 study of peptide receptor radionuclide therapy with [In-DTPA]octreotide: the Rotterdam experience. Semin Nucl Med. 2002;32:110-122.
13. Moll S, Nickeleit V, Mueller-Brand J, et al. A new cause of renal thrombotic microangiopathy: yttrium 90-DOTATOC internal radiotherapy. Am J Kidney Dis. 2001;37:847-851.
14. 0]octreotide. J Nucl Med. 2003;44:98-104.
15. 1-octreotide in patients with neuroendocrine tumors. J Nucl Med. 1999;41:1514-1518.
16. Mariani G, Bodei L, Adelstein SJ, Kassis AI. Emerging roles for radiometabolic therapy of tumors based on Auger electron emission. J Nucl Med. 1999;41:1519-1521.
17. Kalderon D, Roberts BL, Richardson WD, Smith AE. A short amino acid sequence able to specify nuclear location. Cell. 1984;39:499-509.
18. Yoneda Y, Hieda M, Nagoshi E, Miyamoto Y. Nucleocytoplasmic protein transport and recycling of Ran. Cell Struct Funct. 1999;24:425-433.
19. Ginj M, Maecke HR. Synthesis of trifunctional somatostatin based derivatives for improved cellular and subcellular uptake. Tetrahedron Lett. 2005;46:2821-2824.
20. Ginj M, Chen J, Walter MA, Eltschinger V, Reubi JC, Maecke HR. Preclinical evaluation of new and highly potent analogs of octreotide for predictive imaging and targeted radiotherapy. Clin Cancer Res. 2005;11:1136-1145.
21. Tulipano G, Stumm R, Pfeiffer M, Kreienkamp HJ, Hollt V, Schulz S. Differential beta-arrestin trafficking and endosomal sorting of somatostatin receptor subtypes. J Biol Chem. 2004;279:21374-21382.
22. Adelstein S, Kassis AI. Radiobiologic implications of the microscopic distribution of energy from radionuclides. Int J Rad Appl Instrum B. 1987;14:165-169.
23. 125IUdR in mammalian cells: implications of localized energy deposition by Auger processes. Radiat Res. 1987;109:78-89.
24. Walicka M, Adelstein SJ, Kassis AI. Indirect mechanisms contribute to biological effects produced by decay of DNA-incorporated iodine-125 in mammalian cells in vitro: clonogenic survival. Radiat Res. 1998;149:142-146.
25. Walicka M, Ding Y, Adelstein SJ, Kassis AI. Toxicity of DNA-incorporated iodine-125: quantifying the direct and indirect effects. Radiat Res. 2000;154:326-330.
26. Xue L, Butler NJ, Makrigiorgios GM, Adelstein SJ, Kassis AI. Bystander effect produced by radiolabeled tumor cells in vivo. Proc Natl Acad Sci USA. 2002;99:13765-13770.
27. Kassis AI. Cancer therapy with Auger electrons: are we almost there? J Nucl Med. 2003;44:1479-1481.
28. 111In-pentetreotide therapy in patients with disseminated neuroendocrine tumors. J Nucl Med. 2003;44:1-6.
29. Hornick CA, Anthony CT, Hughey S, Gebhard BM, Espenan GD, Woltering EA. Progressive nuclear translocation of somatostatin analogs. J Nucl Med. 2000;41:1256-1263.
30. Wang M, Caruano AL, Lewis MR, Meyer LA, VanderWaal RP, Anderson CJ. Subcellular localization of radiolabeled somatostatin analogues: implications for targeted radiotherapy of cancer. Cancer Res. 2003;63:6864-6869.
31. Koenig JA, Edwardson JM. Endocytosis and recycling of G-protein coupled receptors. Trends Pharmacol Sci. 1997;18:276-287.
32. Kaffman A, O'Shea EK. Regulation of nuclear localization: a key to a door. Annu Rev Cell Dev Biol. 1999;15:291-339.
33. Duncan JR, Stephenson MT, Wu HP, Anderson CJ. Indium-111- diethylentriaminepentaacetic acid-octreotide is delivered in vivo to pancreatic, tumor cell, renal, and hepatocyte lysosomes. Cancer Res. 1997;57:659-671.
34. Parker D, Dickins RS, Puschmann H, Crossland C, Howard JAK. Being excited by lanthanide coordination complexes: aqua species, chirality, excited-state chemistry, and exchange dynamics. Chem Rev. 2002;102:1977-2010.