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fmc.12.31.pdf | 667.84 kB | Adobe PDF | 見る/開く |
タイトル: | Development and application of fluorescent SDF-1 derivatives. |
著者: | Masuda, Ryo Oishi, Shinya https://orcid.org/0000-0002-2833-2539 (unconfirmed) Tanahara, Noriko Ohno, Hiroaki https://orcid.org/0000-0002-3246-4809 (unconfirmed) Hirasawa, Akira https://orcid.org/0000-0001-5692-805X (unconfirmed) Tsujimoto, Gozoh Kodama, Eiichi Matsuoka, Masao Fujii, Nobutaka |
著者名の別形: | 大石, 真也 |
発行日: | May-2012 |
出版者: | Future Science Ltd. |
誌名: | Future medicinal chemistry |
巻: | 4 |
号: | 7 |
開始ページ: | 837 |
終了ページ: | 844 |
抄録: | Background: SDF-1/CXCR4 signaling plays key roles in directed cell migration under physiological and pathological conditions. To develop agonist-based CXCR4 probes for detection of CXCR4 expression on cell lines and metastatic tumors, SAR analyses of fluorescent SDF-1 derivatives were carried out. Results: Several SDF-1 derivatives with a single fluorescent label were designed and synthesized. Modification of the SDF-1 C-terminus with AlexaFluor® 488 or tetramethylrhodamine provided potent CXCR4 probes. Using a potent probe, a novel binding inhibition assay was established for biological evaluation of potential CXCR4 ligands. Conclusion: SDF-1 derivatives with C-terminal modification exhibit equipotent binding with CXCR4 and an alternative SDF-1 receptor CXCR7 to unlabeled SDF-1. The SDF-1 derivatives are applicable to flow cytometry to detect the receptor expression and identify binding compounds for CXCR4. |
著作権等: | © 2012 Future Science Ltd. This is not the published version. Please cite only the published version. この論文は出版社版でありません。引用の際には出版社版をご確認ご利用ください。 |
URI: | http://hdl.handle.net/2433/174342 |
DOI(出版社版): | 10.4155/fmc.12.31 |
PubMed ID: | 22571609 |
出現コレクション: | 学術雑誌掲載論文等 |
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