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211At-Labeled Polymer Nanoparticles for Targeted Radionuclide Therapy of Glucose-Dependent Insulinotropic Polypeptide Receptor (GIPR)-Overexpressed Cancer
https://repo.qst.go.jp/records/85194
https://repo.qst.go.jp/records/851948ea734e5-7766-4f02-82a3-8ab1585af25c
Item type | 学術雑誌論文 / Journal Article(1) | |||||
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公開日 | 2021-07-01 | |||||
タイトル | ||||||
タイトル | 211At-Labeled Polymer Nanoparticles for Targeted Radionuclide Therapy of Glucose-Dependent Insulinotropic Polypeptide Receptor (GIPR)-Overexpressed Cancer | |||||
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 |
Shi, Xiumin
× Shi, Xiumin× Qing, Li× Lulu, Zhang× Masayuki, Hanyu× Lin, Xie× Kuan, Hu× Kotaro, Nagatsu× Chuan, Zhang× Zhengcan, Wu× WANG, Feng× Zhang, Ming-Rong× Kai, Yang× Ran, Zhu× Masayuki, Hanyu× Lin, Xie× Kuan, Hu× Kotaro, Nagatsu× WANG, Feng× Zhang, Ming-Rong |
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抄録 | ||||||
内容記述タイプ | Abstract | |||||
内容記述 | Targeted radionuclide therapy (TRT) provides new and safe opportunities for cancer treatment and management with high precision and efficiency. Here we have designed a novel semiconducting polymer nanoparticle (SPN)-based radiopharmaceutical (211At-MeATE-SPN-GIP) for TRT against glucose-dependent insulinotropic polypeptide receptor (GIPR)-positive cancers to further explore the applications of nano-engineered TRT. 211At-MeATE-SPN-GIP was engineered via nanoprecipitation, followed by its functionalization with a glucose-dependent insulinotropic polypeptide (GIP) to target GIPR and deliver 211At for α therapy. The therapeutic effect and biological safety of 211At-MeATE-SPN-GIP were investigated using GIPR-overexpressing human pancreatic cancer CFPAC-1 cells and CFPAC-1-bearing mice. In this work, 211At-MeATE-SPN-GIP was produced with a radiochemical yield of 43% and radiochemical purity of 98%, which exhibited a specifically high uptake in CFPAC-1 cells, inducing cell cycle arrest at G2/M phase and extensive DNA damage. In the CFPAC-1-bearing tumor model, 211At-MeATE-SPN-GIP exhibited high therapeutic efficiency, with no obvious side effects. The GIPR-specific binding of 211At-MeATE-SPN-GIP combined with effective inhibition of tumor growth, and fewer side effects compared to control suggest that 211At-MeATE-SPN-GIP TRT holds great potential as a novel nano-engineered TRT strategy for patients with GIPR-positive cancer. |
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書誌情報 |
Bioconjugate Chemistry 巻 32, 号 8, p. 1763-1772, 発行日 2021-07 |
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出版者 | ||||||
出版者 | ACS | |||||
ISSN | ||||||
収録物識別子タイプ | ISSN | |||||
収録物識別子 | 1043-1802 | |||||
DOI | ||||||
識別子タイプ | DOI | |||||
関連識別子 | 10.1021/acs.bioconjchem.1c00263 | |||||
関連サイト | ||||||
識別子タイプ | URI | |||||
関連識別子 | https://pubs.acs.org/doi/10.1021/acs.bioconjchem.1c00263 |