@article{oai:repo.qst.go.jp:00045770,
 author = {Jin, Zhao-Hui and Furukawa, Takako and Waki, Atsuo and Coll, Jean-Luc and Saga, Tsuneo and Fujibayashi, Yasuhisa and et.al and 金 朝暉 and 古川 高子 and 佐賀 恒夫 and 藤林 康久},
 issue = {3},
 journal = {Biological & Pharmaceutical Bulletin},
 month = {Dec},
 note = {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.},
 pages = {370--378},
 title = {Effect of Multimerization of a Linear Arg-Gly-Asp Peptide on Integrin Binding Affinity and Specificity},
 volume = {33},
 year = {2009}
}