Nuclear imaging of prostate cancer with gastrin-releasing-peptide-receptor targeted radiopharmaceuticals

Current Pharmaceutical Design

Volumn 14, Issue 28, 2008, Pages 3033-3047

  Ananias, H J K ^a   de Jong, I J ^a   Dierckx, R A ^a,b   van de Wiele, C ^a,b   Helfrich, W ^a   Elsinga, P H ^a,b  

^a UNIVERSITY MEDICAL CENTER GRONINGEN   (Netherlands)

^b GHENT UNIVERSITY HOSPITAL   (Belgium)

Author keywords

Bombesin; GRPR; Nuclear imaging; PET; Prostate cancer; SPECT

Indexed keywords

1,4,7,10 TETRAAZACYCLODODECANE 1,4,7,10 TETRAACETIC ACID; BOMBESIN DERIVATIVE; COPPER 64; FLUORINE 18; GALLIUM 67; GALLIUM 68; GASTRIN RELEASING PEPTIDE RECEPTOR; INDIUM 111; LUTETIUM 177; PENTETATE TECHNETIUM TC 99M; RADIOPHARMACEUTICAL AGENT; TECHNETIUM 99M; YTTRIUM 86; BOMBESIN; BOMBESIN RECEPTOR; DIAGNOSTIC AGENT;

BILIARY EXCRETION; BINDING AFFINITY; CANCER CELL CULTURE; CANCER STAGING; DIAGNOSTIC ACCURACY; DIAGNOSTIC VALUE; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG EXCRETION; DRUG HALF LIFE; DRUG SAFETY; DRUG STABILITY; HUMAN; HYDROPHILICITY; IMAGE QUALITY; IN VIVO STUDY; ISOTOPE LABELING; MALE; NONHUMAN; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; PROSTATE CANCER; PROTEIN TARGETING; RECEPTOR BINDING; REVIEW; SINGLE PHOTON EMISSION COMPUTER TOMOGRAPHY; URINARY EXCRETION; ANIMAL; CLINICAL TRIAL; DRUG DELIVERY SYSTEM; DRUG SCREENING; METABOLISM; METHODOLOGY; PROSTATE TUMOR; SCINTISCANNING;

ANIMALS; BOMBESIN; CLINICAL TRIALS AS TOPIC; DRUG DELIVERY SYSTEMS; DRUG EVALUATION, PRECLINICAL; HUMANS; MALE; POSITRON-EMISSION TOMOGRAPHY; PROSTATIC NEOPLASMS; RADIOPHARMACEUTICALS; RECEPTORS, BOMBESIN; TOMOGRAPHY, EMISSION-COMPUTED, SINGLE-PHOTON;

EID: 58149389523     PISSN: 13816128     EISSN: None     Source Type: Journal    
DOI: 10.2174/138161208786404335     Document Type: Review

References (117)

1. Jemal A, Siegel R, Ward E, Hao Y, Xu J, Murray T, et al. Cancer statistics, 2008. CA Cancer J Clin 2008; 58: 71-96.
2. Ferlay J, Autier P, Boniol M, Heanue M, Colombet M, Boyle P. Estimates of the cancer incidence and mortality in Europe in 2006. Ann Oncol 2007; 18: 581-92.
3. Stephenson AJ, Scardino PT, Eastham JA, Bianco FJ Jr, Dotan ZA, Fearn PA, et al. Preoperative nomogram predicting the 10-year probability of prostate cancer recurrence after radical prostatectomy. J Natl Cancer Inst 2006; 98: 715-7.
4. Stephenson AJ, Eastham JA. Role of salvage radical prostatectomy for recurrent prostate cancer after radiation therapy. J Clin Oncol 2005; 23: 8198-203.
5. Landis SH, Murray T, Bolden S, Wingo PA. Cancer statistics, 1999. CA Cancer J Clin 1999; 49: 8-31.
6. Eisenberger MA, Blumenstein BA, Crawford ED, Miller G, McLeod DG, Loehrer PJ, et al. Bilateral orchiectomy with or without flutamide for metastatic prostate cancer. N Engl J Med 1998; 339: 1036-42.
7. Tannock IF, de Wit R, Berry WR, Horti J, Pluzanska A, Chi KN, et al. Docetaxel plus prednisone or mitoxantrone plus prednisone for advanced prostate cancer. N Engl J Med 2004; 35: 1502-12.
8. Berthold DR, Pond GR, Soban F, de WR, Eisenberger M, Tannock IF. Docetaxel plus prednisone or mitoxantrone plus prednisone for advanced prostate cancer: Updated survival in the TAX 327 study. J Clin Oncol 2008; 26: 242-5.
9. Petrylak DP, Tangen CM, Hussain MH, Lara PN Jr, Jones JA, Taplin ME, et al. Docetaxel and estramustine compared with mitoxantrone and prednisone for advanced refractory prostate cancer. N Engl J Med 2004; 351: 1513-20.
10. de Jong IJ, Pruim J, Elsinga PH, Vaalburg W, Mensink HJ. Preoperative staging of pelvic lymph nodes in prostate cancer by 11C-choline PET. J Nucl Med 2003; 44: 331-5.
11. de Jong IJ, Pruim J, Elsinga PH, Vaalburg W, Mensink HJ. 11C-choline positron emission tomography for the evaluation after treatment of localized prostate cancer. Eur Urol 2003; 44: 32-8.
12. Even-Sapir E, Metser U, Mishani E, Lievshitz G, Lerman H, Leibovitch I. The detection of bone metastases in patients with high-risk prostate cancer: 99mTc-MDP Planar bone scintigraphy, single- and multi-field-of-view SPECT, 18F-fluoride PET, and 18Ffluoride PET/CT. J Nucl Med 2006; 47: 287-97.
13. Liu IJ, Zafar MB, Lai YH, Segall GM, Terris MK. Fluorodeoxyglucose positron emission tomography studies in diagnosis and staging of clinically organ-confined prostate cancer. Urology 2001; 57: 108-111.
14. Manyak MJ. Indium-111 capromab pendetide in the management of recurrent prostate cancer. Expert Rev Anticancer Ther 2008; 8:175-81.
15. Nunez R, Macapinlac HA, Yeung HW, Akhurst T, Cai S, Osman I, et al. Combined 18F-FDG and 11C-methionine PET scans in patients with newly progressive metastatic prostate cancer. J Nucl Med 2002; 43: 46-55.
16. Vees H, Buchegger F, Albrecht S, Khan H, Husarik D, Zaidi H, et al. 18F-choline and/or 11C-acetate positron emission tomography: detection of residual or progressive subclinical disease at very low prostate-specific antigen values (<1 ng/mL) after radical prostatectomy. BJU Int 2007; 99: 1415-20.
17. Krenning EP, Bakker WH, Breeman WA, Koper JW, Kooij PP, Ausema L, et al. Localisation of endocrine-related tumours with radioiodinated analogue of somatostatin. Lancet 1989; 1(8632): 242-4.
18. Weiner RE, Thakur ML. Radiolabeled peptides in oncology: Role in diagnosis and treatment. BioDrugs 2005; 19: 145-63.
19. Lebl M, Hachmann J. High-throughput peptide synthesis. Methods Mol Biol 2005; 298: 167-94.
20. Reader JC. Automation in medicinal chemistry. Curr Top Med Chem 2004; 4: 671-86.
21. Erspamer V, Erpamer GF, Inselvini M. Some pharmacological actions of alytesin and bombesin. J Pharm Pharmacol 1970; 22: 875-6.
22. McDonald TJ, Jornvall H, Nilsson G, Vagne M, Ghatei M, Bloom SR, et al. Characterization of a gastrin releasing peptide from porcine non-antral gastric tissue. Biochem Biophys Res Commun 1979; 90: 227-33.
23. Garcia LJ, Pradhan TK, Weber HC, Moody TW, Jensen RT. The gastrin-releasing peptide receptor is differentially coupled to adenylate cyclase and phospholipase C in different tissues. Biochim Biophys Acta 1997; 1356: 343-54.
24. Hildebrandt JD. Role of subunit diversity in signaling by heterotrimeric G proteins. Biochem Pharmacol 1997; 54: 325-39.
25. Ohki-Hamazaki H, Iwabuchi M, Maekawa F. Development and function of bombesin-like peptides and their receptors. Int J Dev Biol 2005; 49: 293-300.
26. Selbie LA, Hill SJ. G protein-coupled-receptor cross-talk: The fine-tuning of multiple receptor-signalling pathways. Trends Pharmacol Sci 1998; 19: 87-93.
27. Aprikian AG, Cordon-Cardo C, Fair WR, Reuter VE. Characterization of neuroendocrine differentiation in human benign prostate and prostatic adenocarcinoma. Cancer 1993; 71: 3952-65.
28. Cutz E, Chan W, Track NS. Bombesin, calcitonin and leuenkephalin immunoreactivity in endocrine cells of human lung. Experientia 1981; 37: 765-7.
29. Price J, Penman E, Wass JA, Rees LH. Bombesin-like immunoreactivity in human gastrointestinal tract. Regul Pept 1984; 9: 1-10.
30. Spindel ER, Chin WW, Price J, Rees LH, Besser GM, Habener JF. Cloning and characterization of cDNAs encoding human gastrin-releasing peptide. Proc Natl Acad Sci USA 1984; 81: 5699-703.
31. Track NS, Cutz E. Bombesin-like immunoreactivity in developing human lung. Life Sci 1982; 30: 1553-6.
32. Xiao D, Wang J, Hampton LL, Weber HC. The human gastrin-releasing peptide receptor gene structure, its tissue expression and promoter. Gene 2001; 264: 95-103.
33. Bold RJ, Ishizuka J, Yao CZ, Townsend CM Jr, Thompson JC. Bombesin stimulates in vitro growth of human breast cancer independent of estrogen receptors status. Anticancer Res 1998; 18: 4051-6.
34. Bologna M, Festuccia C, Muzi P, Biordi L, Ciomei M. Bombesin stimulates growth of human prostatic cancer cells in vitro. Cancer 1989; 63: 1714-20.
35. Cuttitta F, Carney DN, Mulshine J, Moody TW, Fedorko J, Fischler A, et al. Bombesin-like peptides can function as autocrine growth factors in human small-cell lung cancer. Nature 1985; 316: 823-6.
36. Nelson J, Donnelly M, Walker B, Gray J, Shaw C, Murphy RF. Bombesin stimulates proliferation of human breast cancer cells in culture. Br J Cancer 1991; 63: 933-6.
37. Battey J, Wada E. Two distinct receptor subtypes for mammalian bombesin-like peptides. Trends Neurosci 1991; 14: 524-8.
38. Battey J, Wada E, Corjay M, Way J, Fathi Z, Shapira H, et al. Molecular genetic analysis of two distinct receptors for mammalian bombesin-like peptides. J Natl Cancer Inst Monogr 1992; 141-4.
39. Katsuno T, Pradhan TK, Ryan RR, Mantey SA, Hou W, Donohue PJ, et al. Pharmacology and cell biology of the bombesin receptor subtype 4 (BB4-R). Biochemistry 1999; 38: 7307-20.
40. Nagalla SR, Barry BJ, Creswick KC, Eden P, Taylor JT, Spindel ER. Cloning of a receptor for amphibian [Phe13]bombesin distinct from the receptor for gastrin-releasing peptide: Identification of a fourth bombesin receptor subtype (BB4). Proc Natl Acad Sci USA 1995; 92: 6205-9.
41. Bartholdi MF, Wu JM, Pu H, Troncoso P, Eden PA, Feldman RI. In situ hybridization for gastrin-releasing peptide receptor (GRP receptor) expression in prostatic carcinoma. Int J Cancer 1998; 79: 82-90.
42. Carroll RE, Matkowskyj KA, Chakrabarti S, McDonald TJ, Benya RV. Aberrant expression of gastrin-releasing peptide and its receptor by well-differentiated colon cancers in humans. Am J Physiol 1999; 276: G655-65.
43. Gugger M, Reubi JC. Gastrin-releasing peptide receptors in non-neoplastic and neoplastic human breast. Am J Pathol 1999; 155: 2067-76.
44. Markwalder R, Reubi JC. Gastrin-releasing peptide receptors in the human prostate: Relation to neoplastic transformation. Cancer Res 1999; 59: 1152-9.
45. Reubi JC, Wenger S, Schmuckli-Maurer J, Schaer JC, Gugger M. Bombesin receptor subtypes in human cancers: Detection with the universal radioligand (125)I-[D-TYR(6), beta-ALA(11), PHE(13), NLE(14) bombesin(6-14). Clin Cancer Res 2002; 8: 1139-46.
46. Reubi JC, Korner M, Waser B, Mazzucchelli L, Guillou L. High expression of peptide receptors as a novel target in gastrointestinal stromal tumours. Eur J Nucl Med Mol Imaging 2004; 31: 803-10.
47. Schulz S, Rocken C, Schulz S. Immunohistochemical detection of bombesin receptor subtypes GRP-R and BRS-3 in human tumors using novel antipeptide antibodies. Virchows Arch 2006; 449: 421-7.
48. Sun B, Schally AV, Halmos G. The presence of receptors for bombesin/GRP and mRNA for three receptor subtypes in human ovarian epithelial cancers. Regul Pept 2000; 90: 77-84.
49. Sun B, Halmos G, Schally AV, Wang X, Martinez M. Presence of receptors for bombesin/gastrin-releasing peptide and mRNA for three receptor subtypes in human prostate cancers. Prostate 2000; 42: 295-303.
50. Waser B, Eltschinger V, Linder K, Nunn A, Reubi JC. Selective in vitro targeting of GRP and NMB receptors in human tumours with the new bombesin tracer 177Lu-AMBA. Eur J Nucl Med Mol Imaging 2007; 34: 95-100.
51. Breeman WA, de Jong M, Bernard BF, Kwekkeboom DJ, Srinivasan A, van der Pluijm ME, et al. Pre-clinical evaluation of (111)In-DTPA-Pro(1), Tyr(4)bombesin, a new radioligand for bombesin-receptor scintigraphy. Int J Cancer 1999; 83: 657-63.
52. Parry JJ, Andrews R, Rogers BE. MicroPET imaging of breast cancer using radiolabeled bombesin analogs targeting the gastrin-releasing peptide receptor. Breast Cancer Res Treat 2007; 101: 175-83.
53. Schuhmacher J, Zhang H, Doll J, Macke HR, Matys R, Hauser H, et al. 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: 691-9.
54. Varvarigou AD, Scopinaro F, Leondiadis L, Corleto V, Schillaci O, De Vincentis G, et al. Synthesis, chemical, radiochemical and radiobiological evaluation of a new 99mTc-labelled bombesin-like peptide. Cancer Biother Radiopharm 2002; 17: 317-26.
55. Dimitrakopoulou-Strauss A, Hohenberger P, Haberkorn U, Macke HR, Eisenhut M, Strauss LG. 68Ga-labeled bombesin studies in patients with gastrointestinal stromal tumors: Comparison with 18FFDG. J Nucl Med 2007; 48: 1245-50.
56. Scopinaro F, Varvarigou AD, Ussof W, De Vincentis G, Sourlingas TG, Evangelatos GP, et al. Technetium labeled bombesin-like peptide: preliminary report on breast cancer uptake in patients. Cancer Biother Radiopharm 2002; 17: 327-35.
57. Scopinaro F, De Vincentis G, Corazziari E, Massa R, Osti M, Pallotta N, et al. Detection of colon cancer with 99mTc-labeled bombesin derivative (99mTc-leu13-BN1). Cancer Biother Radiopharm 2004; 19: 245-52.
58. Soluri A, Scopinaro F, De Vincentis G, Varvarigou A, Scafe R, Massa R, et al. 99MTC [13LEU] bombesin and a new gamma camera, the imaging probe, are able to guide mammotome breast biopsy. Anticancer Res 2003; 23: 2139-42.
59. Van de Wiele C, Phonteyne P, Pauwels P, Goethals I, Van den Broecke R, Cocquyt V, et al. Gastrin-releasing peptide receptor imaging in human breast carcinoma versus immunohistochemistry. J Nucl Med 2008; 49: 260-4.
60. Chen J, Zhou JH, Mokotoff M, Fanger MW, Ball ED. Lysis of small cell carcinoma of the lung (SCCL) cells by cytokine-activated monocytes and natural killer cells in the presence of bispecific immunoconjugates containing a gastrin-releasing peptide (GRP) analog or a GRP antagonist. J Hematother 1995; 4: 369-76.
61. Johnson CV, Shelton T, Smith CJ, Ma L, Perry MC, Volkert WA, et al. Evaluation of combined (177)Lu-DOTA-8-AOC-BBN (7-14)NH(2) GRP receptor-targeted radiotherapy and chemotherapy in PC-3 human prostate tumor cell xenografted SCID mice. Cancer Biother Radiopharm 2006; 21: 155-66.
62. Jungwirth A, Pinski J, Galvan G, Halmos G, Szepeshazi K, Cai RZ, et al. Inhibition of growth of androgen-independent DU-145 prostate cancer in vivo by luteinising hormone-releasing hormone antagonist Cetrorelix and bombesin antagonists RC-3940-II and RC-3950-II. Eur J Cancer 1997; 33: 1141-8.
63. Milovanovic SR, Radulovic S, Groot K, Schally AV. Inhibition of growth of PC-82 human prostate cancer line xenografts in nude mice by bombesin antagonist RC-3095 or combination of agonist [D-Trp6]-luteinizing hormone-releasing hormone and somatostatin analog RC-160. Prostate 1992; 20: 269-80.
64. Plonowski A, Nagy A, Schally AV, Sun B, Groot K, Halmos G. In vivo inhibition of PC-3 human androgen-independent prostate cancer by a targeted cytotoxic bombesin analogue, AN-215. Int J Cancer 2000; 88: 652-7.
65. Schwartsmann G, DiLeone LP, Horowitz M, Schunemann D, Cancella A, Pereira AS, et al. A phase I trial of the bombesin/ gastrin-releasing peptide (BN/GRP) antagonist RC3095 in patients with advanced solid malignancies. Invest New Drugs 2006; 24: 403-12.
66. Stangelberger A, Schally AV, Varga JL, Zarandi M, Szepeshazi K, Armatis P, et al. Inhibitory effect of antagonists of bombesin and growth hormone-releasing hormone on orthotopic and intraosseous growth and invasiveness of PC-3 human prostate cancer in nude mice. Clin Cancer Res 2005; 11: 49-57.
67. Zhou J, Chen J, Mokotoff M, Zhong R, Shultz LD, Ball ED. Bombesin/ gastrin-releasing peptide receptor: A potential target for antibody-mediated therapy of small cell lung cancer. Clin Cancer Res 2003; 9: 4953-60.
68. Zhou J, Chen J, Zhong R, Mokotoff M, Shultz LD, Ball ED. Targeting gastrin-releasing peptide receptors on small cell lung cancer cells with a bispecific molecule that activates polyclonal T lymphocytes. Clin Cancer Res 2006; 12: 2224-31.
69. Cescato R, Maina T, Nock B, Nikolopoulou A, Charalambidis D, Piccand V, et al. Bombesin receptor antagonists may be preferable to agonists for tumor targeting. J Nucl Med 2008; 49: 318-26.
70. Maina T, Nock BA, Zhang H, Nikolopoulou A, Waser B, Reubi JC, et al. Species differences of bombesin analog interactions with GRP-R define the choice of animal models in the development of GRP-R-targeting drugs. J Nucl Med 2005; 46: 823-30.
71. Garcia-Garayoa E, Schweinsberg C, Maes V, Ruegg D, Blanc A, Blauenstein P, et al. New [99mTc]bombesin analogues with improved biodistribution for targeting gastrin releasing-peptide receptor- positive tumors. Q J Nucl Med Mol Imaging 2007; 51: 42-50.
72. Garcia-Garayoa E, Ruegg D, Blauenstein P, Zwimpfer M, Khan IU, Maes V, et al. Chemical and biological characterization of new Re(CO)3/ [99mTc](CO)3 bombesin analogues. Nucl Med Biol 2007; 34: 17-28.
73. La Bella R, Garcia-Garayoa E, Bahler M, Blauenstein P, Schibli R, Conrath P, et al. A 99mTc(I)-postlabeled high affinity bombesin analogue as a potential tumor imaging agent. Bioconjug Chem 2002; 13: 599-604.
74. La Bella R, Garcia-Garayoa E, Langer M, Blauenstein P, Beck-Sickinger AG, Schubiger PA. In vitro and in vivo evaluation of a 99mTc(I)-labeled bombesin analogue for imaging of gastrin releasing peptide receptor-positive tumors. Nucl Med Biol 2002; 29: 553-60.
75. Alves S, Correia JD, Santos I, Veerendra B, Sieckman GL, Hoffman TJ, et al. Pyrazolyl conjugates of bombesin: A new tridentate ligand framework for the stabilization of fac-[M(CO)3]+ moiety. Nucl Med Biol 2006; 33: 625-34.
76. Lane SR, Veerendra B, Rold TL, Sieckman GL, Hoffman TJ, Jurisson SS, et al. (99m)Tc(CO)(3)-DTMA bombesin conjugates having high affinity for the GRP receptor. Nucl Med Biol 2008; 35: 263- 72.
77. Smith CJ, Sieckman GL, Owen NK, Hayes DL, Mazuru DG, Kannan R, et al. Radiochemical investigations of gastrin-releasing peptide receptor-specific [(99m)Tc(X)(CO)3-Dpr-Ser-Ser-Ser-Gln- Trp-Ala-Val-Gly-His-Leu-Met-(NH2)] in PC-3, tumor-bearing, rodent models: Syntheses, radiolabeling, and in vitro/in vivo studies where Dpr = 2,3-diaminopropionic acid and X = H2O or P(CH2OH)3. Cancer Res 2003; 63: 4082-8.
78. Baidoo KE, Lin KS, Zhan Y, Finley P, Scheffel U, Wagner HN Jr. Design, synthesis, and initial evaluation of high-affinity technetium bombesin analogues. Bioconjug Chem 1998; 9: 218-25.
79. Lin KS, Luu A, Baidoo KE, Hashemzadeh-Gargari H, Chen MK, Pili R, et al. A new high affinity technetium analogue of bombesin containing DTPA as a pharmacokinetic modifier. Bioconjug Chem 2004; 15: 1416-23
80. Lin KS, Luu A, Baidoo KE, Hashemzadeh-Gargari H, Chen MK, Brenneman K, et al. A new high affinity technetium-99m-bombesin analogue with low abdominal accumulation. Bioconjug Chem 2005; 16: 43-50.
81. Ferro-Flores G, Arteaga de Murphy C, Rodriguez-Cortes J, Pedraza-Lopez M, Ramirez-Iglesias MT. Preparation and evaluation of 99mTc-EDDA/ HYNIC-[Lys 3]-bombesin for imaging gastrin- releasing peptide receptor-positive tumours. Nucl Med Commun 2006; 27: 371-6.
82. Wang LH, Coy DH, Taylor JE, Jiang NY, Moreau JP, Huang SC, et al. des-Met carboxyl-terminally modified analogues of bombesin function as potent bombesin receptor antagonists, partial agonists, or agonists. J Biol Chem 1990; 265: 15695-703.
83. Nock B, Nikolopoulou A, Chiotellis E, Loudos G, Maintas D, Reubi JC, et al. [99mTc]Demobesin 1, a novel potent bombesin analogue for GRP receptor-targeted tumour imaging. Eur J Nucl Med Mol Imaging 2003; 30: 247-58.
84. Nock BA, Nikolopoulou A, Galanis A, Cordopatis P, Waser B, Reubi JC, et al. Potent bombesin-like peptides for GRP-receptor targeting of tumors with 99mTc: A preclinical study. J Med Chem 2005; 48: 100-10
85. Ferris HA, Carroll RE, Lorimer DL, Benya RV. Location and characterization of the human GRP receptor expressed by gastrointestinal epithelial cells. Peptides 1997; 18: 663-72.
86. Narayan S, Draviam E, Rajaraman S, Singh P. High-affinity binding sites for bombesin on mouse colonic mucosal membranes. Mol Cell Biochem 1991; 106: 31-9.
87. Hoffman TJ, Gali H, Smith CJ, Sieckman GL, Hayes DL, Owen NK, et al. Novel series of 111In-labeled bombesin analogs as potential radiopharmaceuticals for specific targeting of gastrin-releasing peptide receptors expressed on human prostate cancer cells. J Nucl Med 2003; 44: 823-31.
88. de Visser M, Bernard HF, Erion JL, Schmidt MA, Srinivasan A, Waser B, et al. Novel 111In-labelled bombesin analogues for molecular imaging of prostate tumours. Eur J Nucl Med Mol Imaging 2007; 34: 1228-38.
89. Zhang H, Schuhmacher J, Waser B, Wild D, Eisenhut M, Reubi JC, et al. 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.
90. Smith CJ, Gali H, Sieckman GL, Hayes DL, Owen NK, Mazuru DG, et al. Radiochemical investigations of 177Lu-DOTA-8-Aoc- BBN[7-14]NH2: an in vitro/in vivo assessment of the targeting ability of this new radiopharmaceutical for PC-3 human prostate cancer cells. Nucl Med Biol 2003; 30: 101-09.
91. Garrison JC, Rold TL, Sieckman GL, Figueroa SD, Volkert WA, Jurisson SS, et al. In vivo evaluation and small-animal PET/CT of a prostate cancer mouse model using 64Cu bombesin analogs: Side-by-side comparison of the CB-TE2A and DOTA chelation systems. J Nucl Med 2007; 48: 1327-37.
92. Rogers BE, Bigott HM, McCarthy DW, Della MD, Kim J, Sharp TL, et al. MicroPET imaging of a gastrin-releasing peptide receptor-positive tumor in a mouse model of human prostate cancer using a 64Cu-labeled bombesin analogue. Bioconjug Chem 2003; 14: 756-63.
93. Lantry LE, Cappelletti E, Maddalena ME, Fox JS, Feng W, Chen J, et al. 177Lu-AMBA: Synthesis and characterization of a selective 177Lu-labeled GRP-R agonist for systemic radiotherapy of prostate cancer. J Nucl Med 2006; 47: 1144-52.
94. Rogers BE, Anderson CJ, Connett JM, Guo LW, Edwards WB, Sherman EL, et al. Comparison of four bifunctional chelates for radiolabeling monoclonal antibodies with copper radioisotopes: Biodistribution and metabolism. Bioconjug Chem 1996; 7: 511-22.
95. Bass LA, Wang M, Welch MJ, Anderson CJ. In vivo transchelation of copper-64 from TETA-octreotide to superoxide dismutase in rat liver. Bioconjug Chem 2000; 11: 527-32.
96. Parry JJ, Kelly TS, Andrews R, Rogers BE. In vitro and in vivo evaluation of 64Cu-labeled DOTA-linker-bombesin(7-14) analogues containing different amino acid linker moieties. Bioconjug Chem 2007; 18: 1110-7.
97. Prasanphanich AF, Nanda PK, Rold TL, Ma L, Lewis MR, Garrison JC, et al. [64Cu-NOTA-8-Aoc-BBN(7-14)NH2] targeting vector for positron-emission tomography imaging of gastrin-releasing peptide receptor-expressing tissues. Proc Natl Acad Sci USA 2007; 104: 12462-7.
98. Chen X, Park R, Hou Y, Tohme M, Shahinian AH, Bading JR, et al. microPET and autoradiographic imaging of GRP receptor expression with 64Cu-DOTA-[Lys3]bombesin in human prostate pression with 64Cu-DOTA-[Lys3]bombesin in human prostate adenocarcinoma xenografts. J Nucl Med 2004; 45: 1390-7.
99. Yang YS, Zhang X, Xiong Z, Chen X. Comparative in vitro and in vivo evaluation of two 64Cu-labeled bombesin analogs in a mouse model of human prostate adenocarcinoma. Nucl Med Biol 2006; 33: 371-80.
100. Biddlecombe GB, Rogers BE, de Visser M, Parry JJ, de Jong M, Erion JL, et al. Molecular imaging of gastrin-releasing peptide receptor-positive tumors in mice using 64Cu- and 86Y-DOTA- (Pro1,Tyr4)-bombesin(1-14). Bioconjug Chem 2007; 18: 724-30.
101. Wester HJ, Hamacher K, Stocklin G. A comparative study of N.C.A. fluorine-18 labeling of proteins via acylation and photochemical conjugation. Nucl Med Biol 1996; 23: 365-72.
102. Poethko T, Schottelius M, Thumshirn G, Hersel U, Herz M, Henriksen G, et al. Two-step methodology for high-yield routine radio-halogenation of peptides: (18)F-labeled RGD and octreotide analogs. J Nucl Med 2004; 45: 892-902.
103. Zhang X, Cai W, Cao F, Schreibmann E, Wu Y, Wu JC, et al. 18F-labeled bombesin analogs for targeting GRP receptor-expressing prostate cancer. J Nucl Med 2006; 47: 492-501.
104. Li ZB, Wu Z, Chen K, Ryu EK, Chen X. 18F-labeled BBN-RGD heterodimer for prostate cancer imaging. J Nucl Med 2008; 49: 453-61.
105. Bello L, Francolini M, Marthyn P, Zhang J, Carroll RS, Nikas DC, et al. Alpha(v)beta3 and alpha(v)beta5 integrin expression in glioma periphery. Neurosurgery 2001; 49: 380-9.
106. Friedlander M, Brooks PC, Shaffer RW, Kincaid CM, Varner JA, Cheresh DA. Definition of two angiogenic pathways by distinct alpha v integrins. Science 1995; 270: 1500-2.
107. Horton MA. The alpha v beta 3 integrin "vitronectin receptor". Int J Biochem Cell Biol 1997; 29: 721-5.
108. Zhang X, Cai W, Cao F, Schreibmann E, Wu Y, Wu JC, et al. 18F-labeled bombesin analogs for targeting GRP receptor-expressing prostate cancer. J Nucl Med 2006; 47: 492-501.
109. Van de Wiele C, Dumont F, Vanden Broecke R, Oosterlinck W, Cocquyt V, Serreyn R, et al. Technetium-99m RP527, a GRP analogue for visualisation of GRP receptor-expressing malignancies: A feasibility study. Eur J Nucl Med 2000; 27: 1694-9.
110. Van de Wiele C, Dumont F, Dierckx RA, Peers SH, Thornback JR, Slegers G, et al. Biodistribution and dosimetry of (99m)Tc-RP527, a gastrin-releasing peptide (GRP) agonist for the visualization of GRP receptor-expressing malignancies. J Nucl Med 2001; 42: 1722-7.
111. De Vincentis G, Remediani S, Varvarigou AD, Di SG, Iori F, Laurenti C, et al. Role of 99mTc-bombesin scan in diagnosis and staging of prostate cancer. Cancer Biother Radiopharm 2004; 19: 81-4.
112. Scopinaro F, De Vincentis G, Varvarigou AD, Laurenti C, Iori F, Remediani S, et al. 99mTc-bombesin detects prostate cancer and invasion of pelvic lymph nodes. Eur J Nucl Med Mol Imaging 2003; 30: 1378-82.
113. de Visser M, van Weerden WM, de Ridder CM, Reneman S, Melis M, Krenning EP, et al. Androgen-dependent expression of the gastrin- releasing peptide receptor in human prostate tumor xenografts. J Nucl Med 2007; 48: 88-93.
114. Jiborn T, Bjartell A, Abrahamsson PA. Neuroendocrine differentiation in prostatic carcinoma during hormonal treatment. Urology 1998; 51: 585-9.
115. Bauer M, Wagner CC, Langer O. Microdosing studies in humans: The role of positron emission tomography. Drugs RD 2008; 9(2): 73-81.
116. Hamoudeh M, Kamleh MA, Diab R, Fessi H. Radionuclides delivery systems for nuclear imaging and radiotherapy of cancer. Adv Drug Deliv Rev 2008; 60(12): 1329-46.
117. Wagner CC, Muller M, Lappin G, Langer O. Positron emission tomography for use in microdosing studies. Curr Opin Drug Discov Devel 2008; 11(1): 104-10.