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Preparation of a promising angiogenesis PET imaging agent: 68Ga-labeled c(RGDyK)-isothiocyanatobenzyl-1,4,7-triazacyclononane-1,4,7-triacetic acid and feasibility studies in mice
DC Field | Value | Language |
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dc.contributor.author | Jeong, Jae Min | - |
dc.contributor.author | Hong, Mee Kyung | - |
dc.contributor.author | Chang, Young Soo | - |
dc.contributor.author | Lee, Yun-Sang | - |
dc.contributor.author | Kim, Young Joo | - |
dc.contributor.author | Cheon, Gi Jeong | - |
dc.contributor.author | Lee, Dong Soo | - |
dc.contributor.author | Chung, June-Key | - |
dc.contributor.author | Lee, Myung Chul | - |
dc.date.accessioned | 2010-06-22T04:53:36Z | - |
dc.date.available | 2010-06-22T04:53:36Z | - |
dc.date.issued | 2008-04-17 | - |
dc.identifier.citation | J Nucl Med. 2008;49(5):830-836 | en |
dc.identifier.issn | 0161-5505 (Print) | - |
dc.identifier.uri | http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=18413379 | - |
dc.identifier.uri | http://jnm.snmjournals.org/cgi/reprint/49/5/830.pdf | - |
dc.identifier.uri | https://hdl.handle.net/10371/67753 | - |
dc.description.abstract | Arg-Gly-Asp (RGD) derivatives have been labeled with various radioisotopes for the imaging of angiogenesis in ischemic tissue, in which alpha(v)beta(3) integrin plays an important role. In this study, cyclic Arg-Gly-Asp-D-Tyr-Lys [c(RGDyK)] was conjugated with 2-(p-isothiocyanatobenzyl)-1,4,7-triazacyclononane-1,4,7-triacetic acid (SCN-Bz-NOTA) and then labeled with (68)Ga. The labeled RGD so produced was subjected to an in vitro binding assay and in vivo biodistribution and PET studies. METHODS: A mixture of SCN-Bz-NOTA (660 nmol) and c(RGDyK) (600 nmol) in 0.1 M sodium carbonate buffer (pH 9.5) was allowed to react for 20 h at room temperature in the dark for thiourea bond formation. The conjugate obtained was purified by semipreparative high-performance liquid chromatography (HPLC). The purified c(RGDyK)-SCN-Bz-NOTA (NOTA-RGD) was then labeled with (68)Ga from a (68)Ge/(68)Ga generator and purified by semipreparative HPLC. A competitive binding assay for c(RGDyK) and NOTA-RGD was performed with (125)I-c(RGDyK) as a radioligand and alpha(v)beta(3) integrin-coated plates as a solid phase. (68)Ga-NOTA-RGD (0.222 MBq/100 microL) was injected, through a tail vein, into mice with hind limb ischemia and into mice bearing human colon cancer SNU-C4 xenografts. Biodistribution and imaging studies were performed at 1 and 2 h after injection. RESULTS: The labeling of NOTA-RGD with (68)Ga was straightforward. The K(i) values of c(RGDyK) and NOTA-RGD were 1.3 and 1.9 nM, respectively. In the biodistribution study, the mean +/- SD uptake of (68)Ga-NOTA-RGD by ischemic muscles was 1.6+/-0.2 percentage injected dose per gram (%ID/g); this uptake was significantly blocked by cold c(RGDyK) to 0.6+/-0.3 %ID/g (P<0.01). Tumor uptake was 5.1+/-1.0 %ID/g, and the tumor-to-blood ratio was 10.3+/-4.8. Small-animal PET revealed rapid excretion through the urine and high levels of tumor and kidney uptake. CONCLUSION: Stable (68)Ga-NOTA-RGD was obtained in a straightforward manner at a high yield and showed a high affinity for alpha(v)beta(3) integrin, specific uptake by angiogenic muscles, a high level of uptake by tumors, and rapid renal excretion. (68)Ga-NOTA-RGD was found to be a promising radioligand for the imaging of angiogenesis. | en |
dc.language.iso | en | en |
dc.publisher | The Society of Nuclear Medicine Inc | en |
dc.subject | Animals | en |
dc.subject | Anoxia/radionuclide imaging | en |
dc.subject | Feasibility Studies | en |
dc.subject | Gallium Radioisotopes | en |
dc.subject | Heterocyclic Compounds/chemical synthesis/*chemistry/*diagnostic use | en |
dc.subject | Hindlimb/blood supply/pathology | en |
dc.subject | Humans | en |
dc.subject | Ischemia/radionuclide imaging | en |
dc.subject | Isothiocyanates/chemical synthesis/*chemistry/*diagnostic use | en |
dc.subject | Male | en |
dc.subject | Mice | en |
dc.subject | Neovascularization, Pathologic/*radionuclide imaging | en |
dc.subject | Oligopeptides/*chemistry | en |
dc.subject | Positron-Emission Tomography/*methods | en |
dc.subject | Staining and Labeling | en |
dc.subject | Transplantation, Heterologous | en |
dc.title | Preparation of a promising angiogenesis PET imaging agent: 68Ga-labeled c(RGDyK)-isothiocyanatobenzyl-1,4,7-triazacyclononane-1,4,7-triacetic acid and feasibility studies in mice | en |
dc.type | Article | en |
dc.contributor.AlternativeAuthor | 정재민 | - |
dc.contributor.AlternativeAuthor | 홍미경 | - |
dc.contributor.AlternativeAuthor | 장영수 | - |
dc.contributor.AlternativeAuthor | 이윤상 | - |
dc.contributor.AlternativeAuthor | 김영주 | - |
dc.contributor.AlternativeAuthor | 천기정 | - |
dc.contributor.AlternativeAuthor | 이동수 | - |
dc.contributor.AlternativeAuthor | 정준기 | - |
dc.contributor.AlternativeAuthor | 이명철 | - |
dc.identifier.doi | 10.2967/jnumed.107.047423 | - |
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