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Development of the Fibronectin-Mimetic Peptide KSSPHSRN(SG)5RGDSP as a Novel Radioprobe for Molecular Imaging of the Cancer Biomarker α5β1 Integrin.
https://repo.qst.go.jp/records/47409
https://repo.qst.go.jp/records/474093fcf0bbd-0260-4608-bc28-23f38692e260
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2016-05-18 | |||||
| タイトル | ||||||
| タイトル | Development of the Fibronectin-Mimetic Peptide KSSPHSRN(SG)5RGDSP as a Novel Radioprobe for Molecular Imaging of the Cancer Biomarker α5β1 Integrin. | |||||
| 言語 | ||||||
| 言語 | eng | |||||
| 資源タイプ | ||||||
| 資源タイプ識別子 | http://purl.org/coar/resource_type/c_6501 | |||||
| 資源タイプ | journal article | |||||
| アクセス権 | ||||||
| アクセス権 | metadata only access | |||||
| アクセス権URI | http://purl.org/coar/access_right/c_14cb | |||||
| 著者 |
Jin, Zhao-Hui
× Jin, Zhao-Hui× Furukawa, Takako× Kumata, Katsushi× Xie, Lin× Yui, Joji× Wakizaka, Hidekatsu× Fujibayashi, Yasuhisa× Zhang, Ming-Rong× Saga, Tsuneo× 金 朝暉× 古川 高子× 熊田 勝志× 謝 琳× 由井 譲二× 脇坂 秀克× 藤林 康久× 張 明栄× 佐賀 恒夫 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | α5β1 Integrin, a fibronectin receptor, is becoming a pertinent therapeutic target and a promising prognostic biomarker for cancer patients. The aim of this study was to functionalize an α5β1-specific fibronectin-mimetic peptide sequence KSSPHSRN(SG)5RGDSP (called PR_b) as a positron emission tomography (PET) probe. PR_b was modified by addition of a β-alanine residue, conjugated with 2-S-(4-isothiocyanatobenzyl)-1,4,7-triazacyclononane-1,4,7-triacetic acid (p-SCN-Bn-NOTA), and radiolabeled with (18)F based on the chelation of (18)F-aluminum fluoride. A control probe was produced by glycine to alanine substitution in the RGD motif of PR_b. Cell binding and blocking assays, autoradiographic evaluation of tissue binding and blocking, dynamic PET scans, and a biodistribution study were conducted using cell lines and murine tumor models with determined expression levels of α5β1 and other related integrins. (18)F-PR_b was produced with a labeling yield of 22.3±1.9% based on (18)F-F(-), a radiochemical purity of >99%, and a specific activity of 30-70 GBq/µmol; it exhibited α5β1-binding activity and specificity in vitro, ex vivo, and in vivo, and had a rapid blood clearance and a predominant renal excretion pathway. In vivo α5β1-positive tumors could be clearly visualized by (18)F-PR_b PET imaging. Both imaging and biodistribution studies suggested higher uptake of (18)F-PR_b in α5β1-positive tumors than in α5β1-negative tumors and higher α5β1-positive tumor uptake of (18)F-PR_b than the control probe. In contrast, there was no significant difference seen in the contralateral muscle uptake. A PET radioprobe, (18)F-PR_b, was developed de novo and potentially can be used for noninvasive detection of α5β1 expression in tumors. | |||||
| 書誌情報 |
Biological & pharmaceutical bulletin 巻 38, 号 11, p. 1722-1731, 発行日 2015-01 |
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| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0918-6158 | |||||
| PubMed番号 | ||||||
| 識別子タイプ | PMID | |||||
| 関連識別子 | 26277991 | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.1248/bpb.b15-00344 | |||||
