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タイトル: Concise site-specific synthesis of DTPA-peptide conjugates: application to imaging probes for the chemokine receptor CXCR4.
著者: Masuda, Ryo
Oishi, Shinya  kyouindb  KAKEN_id
Ohno, Hiroaki  kyouindb  KAKEN_id
Kimura, Hiroyuki  KAKEN_id
Saji, Hideo  kyouindb  KAKEN_id
Fujii, Nobutaka  KAKEN_id
著者名の別形: 大石, 真也
キーワード: CXCR4
DTPA
Molecular imaging
発行日: 15-May-2011
出版者: Elsevier Ltd.
誌名: Bioorganic & medicinal chemistry
巻: 19
号: 10
開始ページ: 3216
終了ページ: 3220
抄録: Diethylenetriaminepentaacetic acid (DTPA) is a useful chelating agent for radionuclides such as (68)Ga, (99m)Tc and (111)In, which are applicable to nuclear medicine imaging. In this study, we established a facile synthetic protocol for the production of mono-DTPA-conjugated peptide probes. A novel monoreactive DTPA precursor reagent was synthesized in two steps using the chemistry of the o-nitrobenzenesulfonyl (Ns) protecting group, and under mild conditions this DTPA precursor was incorporated onto an N(ε)-bromoacetylated Lys of a protected peptide resin. The site-specific DTPA conjugation was facilitated by using a highly acid-labile 4-methyltrityl (Mtt) protecting group for the target site of the bioactive peptide during the solid-phase synthesis. A combination of both techniques yielded peptides with disulfide bonds, such as octreotide and polyphemusin II-derived CXCR4 antagonists. DTPA-peptide conjugates were purified in a single step following cleavage from the resin and disulfide bond formation. This site-specific on-resin construction strategy was used for the design and synthesis of a novel In-DTPA-labeled CXCR4 antagonist, which exhibited highly potent inhibitory activity against SDF-1-CXCR4 binding.
著作権等: © 2011 Elsevier 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/2433/159701
DOI(出版社版): 10.1016/j.bmc.2011.03.059
PubMed ID: 21524584
出現コレクション:学術雑誌掲載論文等

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