2014 Fiscal Year Final Research Report
Development of peptide-based PET probe targeting integrin alpha5beta1
| Project/Area Number |
24591827
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Multi-year Fund |
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| Section | 一般 |
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| Research Field |
Radiation science
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| Research Institution | National Institute of Radiological Sciences |
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Principal Investigator |
JIN Zhao-Hui 独立行政法人放射線医学総合研究所, 分子イメージング研究センター, 主任研究員 (70324150)
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| Co-Investigator(Kenkyū-buntansha) |
ZHANG Ming-Rong 独立行政法人放射線医学総合研究所, 分子イメージング研究センター, プログラムリーダー (80443076)
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| Co-Investigator(Renkei-kenkyūsha) |
FURUKAWA Takako 独立行政法人放射線医学総合研究所, 分子イメージング研究センター, チームリーダー (00221557)
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| Project Period (FY) |
2012-04-01 – 2015-03-31
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| Keywords | alpha5beta1 integrin / Fluorine-18 / PET imaging / Fibronectin / Radioprobe |
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| Outline of Final Research Achievements |
This study was aimed to develop a novel PET imaging probe targeting the transmembrane glycoprotein receptor, α5β1integrin, by use of the fibronectin-mimetic peptide sequence KSSPHSRNSGSGSGSGSGRGDSP (called PR_b). PR_b was modified and conjugated with the chelating agent p-SCN-Bn-NOTA, and radiolabeled with 18F based on the chelation of 18F-aluminum fluoride. 18F-PR_b was produced with a radiochemical purity of >95%; it exhibited α5β1-binding activity and specificity in cultured cells and in tumor-bearing mice, and had a rapid blood clearance and a predominant renal excretion pathway. In vivo α5β1-positive tumors could be clearly visualized by 18F-PR_b PET imaging. 18F-PR_b was developed as a promising PET imaging agent targeting the α5β1 integrin.
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| Free Research Field |
医歯薬学
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