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  1. 原著論文

In vivo optical imaging of integrin alphaV-beta3 in mice using multivalent or monovalent cRGD targeting vectors

https://repo.qst.go.jp/records/45640
https://repo.qst.go.jp/records/45640
1fe1a810-7565-47bf-b3d1-e18d261ed17d
Item type 学術雑誌論文 / Journal Article(1)
公開日 2009-09-15
タイトル
タイトル In vivo optical imaging of integrin alphaV-beta3 in mice using multivalent or monovalent cRGD targeting vectors
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

WEKO 453547

Jin, Zhao-Hui

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Coll, Jean-Luc

× Coll, Jean-Luc

WEKO 453548

Coll, Jean-Luc

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et.al

× et.al

WEKO 453549

et.al

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金 朝暉

× 金 朝暉

WEKO 453550

en 金 朝暉

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抄録
内容記述タイプ Abstract
内容記述 Background
The cRGD peptide is a promising probe for early non-invasive detection of tumors. This study aimed to demonstrate how RAFT-c(-RGDfK-)4, a molecule allowing a tetrameric presentation of cRGD, improved cRGD-targeting potential using in vivo models of alphaVbeta3-positive or negative tumors.
\nResults
We chose the human embryonic kidney cells HEK293(beta3) (high levels of alphaVbeta3) or HEK293(beta1) (alphaVbeta3-negative but expressing alphaV and beta1) engrafted subcutaneously (s.c.) in mice. Non-invasive in vivo optical imaging demonstrated that as compared to its monomeric cRGD analogue, Cy5-RAFT-c(-RGDfK-)4 injected intravenously had higher uptake, prolonged retention and markedly enhanced contrast in HEK293(beta3) than in the HEK293(beta1) tumors. Blocking studies further demonstrated the targeting specificity and competitive binding ability of the tetramer.
\nConclusion
In conclusion, we demonstrated that Cy5-RAFT-c(-RGDfK-)4 was indeed binding to the alphaVbeta3 receptor and with an improved activity as compared to its monomeric analog, confirming the interest of using multivalent ligands. Intravenous injection of Cy5-RAFT-c(-RGDfK-)4 in this novel pair of HEK293(beta3) and HEK293(beta1) tumors, provided tumor/skin ratio above 15. Such an important contrast plus the opportunity to use the HEK293(beta1) negative control cell line are major assets for the community of researchers working on the design and amelioration of RGD-targeted vectors or on RGD-antagonists.
書誌情報 Molecular Cancer (Online Only URL:http://www.molecular-cancer.com/)

巻 6, p. 41-1-41- 9, 発行日 2007-06
ISSN
収録物識別子タイプ ISSN
収録物識別子 1476-4598
DOI
識別子タイプ DOI
関連識別子 10.1186/1476-4598-6-41
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