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Title Page
Abstract
Contents
List of Abbreviations 13
Chapter 1. Introduction 15
1. Cancer 15
A. Tumor 15
B. Cancerous Progression 16
2. Targeted Therapy of Cancer 19
3. Research Purposes 21
Chapter 2. Theoretical Background 24
1. Radiopharmaceuticals 24
2. Technetium and Rhenium in Radiopharmaceuticals 26
3. Development of Target Specific Radiopharmaceuticals 31
4. Peptide Receptors in Oncology 32
5. Design of Peptide-based Radiopharmaceuticals 37
6. Somatostatin Receptor Targeting 43
A. Lung Cancer 43
B. Somatostatin Analogue 44
C. Radiolabeled Somatostatin Analogues 47
7. Melanocortin-1 Receptor (MC1-R) Targeting 49
A. Melanoma 49
B. Melanocortin-1 Receptor (MC1-R) 53
C. Radiolabeled α-MSH Analogues 54
Chapter 3. Approaches and Experiments 57
1. Approaches 57
A. Synthesis of peptides 57
B. Characterization of peptide 61
C. Radiolabeling 62
D. Biological Evaluation 63
2. Experiments 64
A. Materials and Methods 64
B. Synthesis and Characterization of Peptides 65
C. Radiolabeling of Peptide with 99mTc and 188Re(이미지참조) 67
D. Preparation of Radiolabeled Peptides 68
E. In vitro Test 69
F. Biodistribution Studies 71
G. Radionuclide therapy of 188Re-N₂S₂-α-MSH(이미지참조) 72
H. Molecular Modeling 72
Chapter 4. Results and Discussion 74
1. Synthesis of Peptide 74
A. N₂S₂-Somatostatin 74
B. α-MSH Analogue 80
2. Radiolabeled-peptides with 99mTc and 188Re(이미지참조) 92
A. 99mTc-labeled Peptides(이미지참조) 92
B. 188Re-labeled Peptides(이미지참조) 96
3. Biodistribution Studies 110
A. 188Re-N₂S₂-Somatostatin(이미지참조) 110
B. 188Re-N₂S₂-α-MSH(이미지참조) 113
C. 188Re-N₂S₂-Glucose-α-MSH(이미지참조) 115
4. Radionuclide Therapy of 188Re-N₂S₂-α-MSH(이미지참조) 116
Tumor growth inhibition 116
Treatment Efficacy 117
Chapter 5. Conclusions 119
Somatostatin Analogue 119
α-MSH Analogues 120
References 123
초록 132
Table 1. Peptide library approached to discover tumor targeting peptides 21
Table 2. Characterization of various technetium-based pharmaceuticals with 5 coordination number 29
Table 3. Peptides for disease targeting 36
Table 4. Selected β-particle emitting radionuclides with therapeutic potential 42
Table 5. Frequency of histological types of lung cancer 43
Table 6. Presence of different somatostatin receptor (SSTR) subtypes in human tumor tissues 45
Table 7. Incidence rates of melanoma by race in the United States 50
Table 8. Death rates of melanoma by race in the United States 51
Table 9. Melanoma stages 52
Table 10. Evaluation method of radiolabeling yield and radiochemical purity of 99mTc-GH or 188Re-GH using tin layer chromatography(이미지참조) 68
Table 11. Tumour-to-blood ratio of 188Re-N₂S₂-somatostatin in Calu-6 bearing mice(이미지참조) 110
Table 12. Tumour-to-blood ratio of 188Re-N₂S₂-α-MSH in B16/F1 bearing mice(이미지참조) 113
Figure 1. Classification of tumor 15
Figure 2. Cancer, the process of growth 17
Figure 3. Schematic diagram of research processes 23
Figure 4. Imaging instrumentation for disease diagnosis 25
Figure 5. Periodic Table of the elements 28
Figure 6. Chemical formulas of selected technetium radiopharmaceuticals 30
Figure 7. Radiolabeled compounds for somatostatin receptor targeting 34
Figure 8. Concept for the development of target specific radiopharmaceuticals 39
Figure 9. Examples of covalent cyclizations 40
Figure 10. Structure of somatostatin analogues 47
Figure 11. Structure of chelator-conjugate octreotide 48
Figure 12. Melanocortin-1 receptor targeting for melanoma therapy 55
Figure 13. Structure of Re-CCMSH 56
Figure 14. Peptide synthesis using Fmoc strategy 58
Figure 15. Fmoc-solid phase peptide synthesis strategy 60
Figure 16. Scheme for N₂S₂-somatostatin synthesis using Fmoc strategy 75
Figure 17. Structure of N₂S₂-somatostatin 76
Figure 18. HPLC profile of N₂S₂-somatostatin 77
Figure 19. Mass analysis of N₂S₂-Somatostatin 78
Figure 20. Molecular modeling of N₂S₂-somatostatin 79
Figure 21. Scheme for N₂S₂-α-MSH synthesis using Fmoc strategy 81
Figure 22. Structure of N₂S₂-α-MSH 82
Figure 23. HPLC profile of N₂S₂-α-MSH 83
Figure 24. Mass analysis of N₂S₂-α-MSH 84
Figure 25. Molecular modeling of N₂S₂-α-MSH 85
Figure 26. Scheme for glucose linker synthesis 86
Figure 27. Scheme for N₂S₂-glucose-α-MSH synthesis using Fmoc strategy 88
Figure 28. Structure of N₂S₂-glucose-α-MSH 89
Figure 29. HPLC profile of N₂S₂-glucose-α-MSH 90
Figure 30. Mass analysis of N₂S₂-glucose-α-MSH 91
Figure 31. ITLC-SG pattern for 99mTc-GH Radiolabeling yield(%) ＝ 100% - % of Na99mTcO₄ - % of 99mTc-colloid(이미지참조) 93
Figure 32. HPLC profile of 99mTc-N₂S₂-somatostatin(이미지참조) 94
Figure 33. HPLC profile of 99mTc-N₂S₂-α-MSH(이미지참조) 95
Figure 34. ITLC-SG pattern for 188Re-GH (2 mg SnCl₂ · 2H₂O) Radiolabeling yield (%) ＝ 100% - % of Na188ReO₄ - % of 188Re-colloid(이미지참조) 97
Figure 35. ITLC-SG pattern for 188Re-GH (0.45 mg SnCl₂ · 2H₂O)(이미지참조) 98
Figure 36. Transchelation effect of 188Re-GH(이미지참조) 99
Figure 37. Radiolabeling of N₂S₂-somatostatin with 188Re(이미지참조) 100
Figure 38. HPLC profile of 188Re-N₂S₂-somatostatin(이미지참조) 101
Figure 39. Radiolabeling yield of 188Re-N₂S₂-Somatostatin with a different concentration(이미지참조) 102
Figure 40. Serum stability of 1188Re-N₂S₂-somatostatin(이미지참조) 103
Figure 41. Radiolabeling of N₂S₂-α-MSH with 188Re(이미지참조) 104
Figure 42. HPLC profile of 188Re-labeled α-MSH derivatives(이미지참조) 105
Figure 43. Radiolabeling yield of 188Re-N₂S₂-α-MSH with a different concentration(이미지참조) 106
Figure 44. Radiolabeling yield of 188Re-N₂S₂-glucose-α-MSH with a different concentration(이미지참조) 107
Figure 45. Serum stability of 188Re-labeled α-MSH derivatives(이미지참조) 109
Figure 46. Biodistribution of 188Re-N₂S₂-somatostatin in Calu-6 bearing mice(이미지참조) 112
Figure 47. Biodistribution of 188Re-N₂S₂-α-MSH in B16/F1 bearing mice(이미지참조) 114
Figure 48. Biodistribution of 188Re-N₂S₂-glucose-α-MSH in B16/F1 bearing mice(이미지참조) 115
Figure 49. Effects of 188Re-N₂S₂-α-MSH on the tumor growth of B16/F1 tumor bearing mice(이미지참조) 117
Figure 50. Effects of 188Re-N₂S₂-α-MSH on the survival rate of B16/F1 tumor bearing mice(이미지참조) 118
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