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Effect of Multimerization of a Linear Arg-Gly-Asp Peptide on Integrin Binding Affinity and Specificity
https://repo.qst.go.jp/records/45770
https://repo.qst.go.jp/records/4577093263f1f-e3bb-4222-9ba0-bbc457696220
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2010-03-24 | |||||
| タイトル | ||||||
| タイトル | Effect of Multimerization of a Linear Arg-Gly-Asp Peptide on Integrin Binding Affinity and Specificity | |||||
| 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× Waki, Atsuo× Coll, Jean-Luc× Saga, Tsuneo× Fujibayashi, Yasuhisa× et.al× 金 朝暉× 古川 高子× 佐賀 恒夫× 藤林 康久 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Multivalent interactions are frequently used to enhance ligand-receptor binding affinity. In this study, mono-, di- and trimeric Ala-Val-Thr-Gly-Arg-Gly-Asp-Ser-Tyr (AVTGRGDSY) peptides, labeled with 125I or Cy5.5, were compared in vitro and in vivo. Using human embryonic kidney HEK293 (naturally aV-positive and b 3-negative), HEK293(b 1) (b 1-transfected and aVb 3-negative), HEK293(b 3) (b 3-transfected and strongly aVb 3- positive), and human glioblastoma U87MG (naturally aVb 3-positive) cell lines we evaluated their binding affinity and specificity. In vitro, the monomeric AVTGRGDSY showed specific binding to both HEK293(b 1) and HEK293(b 3) cells. Multimerization resulted in no change toward HEK293 cells, diminished binding with HEK293(b 1) cells, but substantially enhanced binding with aVb 3-positive HEK293(b 3) and U87MG cells. Moreover, multimeric AVTGRGDSY peptides were found to be nearly comparable to the same molar concentration of a well-known aVb 3-specific cyclo(RGDfV) (c(RGDfV)) peptide in specificity and affinity for targeting aVb 3 integrin. Non-invasive in vivo optical imaging demonstrated that as compared to its monomeric analogue, the Cy5.5- labeled dimeric AVTGRGDSY peptide produced markedly enhanced tumor-to-background contrast in HEK293(b 3) tumor-bearing mice than in HEK293(b 1) tumor-bearing mice. In conclusion, the present study showed the difference of monomeric and multimeric linear Arg-Gly-Asp (RGD)-containing compound in integrin selectivity and affinity. Our data provide useful information for the design of novel RGD peptides. |
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| 書誌情報 |
Biological & Pharmaceutical Bulletin 巻 33, 号 3, p. 370-378, 発行日 2009-12 |
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| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0918-6158 | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.1248/bpb.33.370 | |||||
