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用于血管生成的双峰靶向造影剂的设计与合成。

Design and synthesis of a bimodal target-specific contrast agent for angiogenesis.

作者信息

Dirksen Anouk, Langereis Sander, de Waal Bas F M, van Genderen Marcel H P, Meijer E W, de Lussanet Quido G, Hackeng Tilman M

机构信息

Laboratory of Macromolecular and Organic Chemistry, Eindhoven University of Technology, P.O. Box 513, 5600 MB Eindhoven, The Netherlands.

出版信息

Org Lett. 2004 Dec 23;6(26):4857-60. doi: 10.1021/ol048084u.

Abstract

[structure: see text] A bimodal target-specific contrast agent based on a cyclic peptide containing the target-specific NGR sequence, gadolinium(III) diethylenetriaminepentaacetic acid (Gd(III)DTPA), and Oregon Green 488 (OG488) suitable for both MR imaging and optical imaging of angiogenesis is developed. The synthetic strategy for this target-specific contrast agent exploits the use of highly efficient, chemoselective reactions, such as native chemical ligation, and gives a straightforward approach for double labeling of peptides in general.

摘要

[结构:见正文] 开发了一种基于含有靶标特异性NGR序列的环肽、钆(III)二乙三胺五乙酸(Gd(III)DTPA)和俄勒冈绿488(OG488)的双峰靶标特异性造影剂,适用于血管生成的磁共振成像和光学成像。这种靶标特异性造影剂的合成策略利用了高效、化学选择性反应,如天然化学连接,并且总体上为肽的双重标记提供了一种直接的方法。

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