当前位置: X-MOL 学术Bioconjugate Chem. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Synthesis of High Relaxivity Gadolinium AAZTA Tetramers as Building Blocks for Bioconjugation
Bioconjugate Chemistry ( IF 4.0 ) Pub Date : 2018-02-22 00:00:00 , DOI: 10.1021/acs.bioconjchem.8b00120
Martina Tripepi 1 , Federico Capuana 1 , Eliana Gianolio 1 , Flávio Vinicius Crizóstomo Kock 2 , Amerigo Pagoto 1 , Rachele Stefania 1 , Giuseppe Digilio 3 , Silvio Aime 1
Affiliation  

Molecular imaging requires the specific accumulation of contrast agents at the target. To exploit the superb resolution of MRI for applications in molecular imaging, gadolinium chelates, as the MRI contrast agents (CA), have to be conjugated to a specific vector able to recognize the epitope of interest. Several Gd(III)-chelates can be chemically linked to the same binding vector in order to deliver multiple copies of the CA (multimers) in a single targeting event thus increasing the sensitivity of the molecular probe. Herein three novel bifunctional agents, carrying one functional group for the bioconjugation to targeting vectors and four Gd(III)-AAZTA chelate functions for MRI contrast enhancement (AAZTA = 6-amino-6-methylperhydro-1,4-diazepinetetraacetic acid), are reported. The relaxivity in the tetrameric derivatives is 16.4 ± 0.2 mMGd–1 s–1 at 21.5 MHz and 25 °C, being 2.4-fold higher than that of parent, monomeric Gd(III)-AAZTA. These compounds can be used as versatile building blocks to insert preformed, high relaxivity, and high density Gd-centers to biological targeting vectors. As an example, we describe the use of these bifunctional Gd(III)-chelates to label a fibrin-targeting peptide.

中文翻译:

高弛豫Relax AAZTA四聚体的合成作为生物共轭的基础。

分子成像需要造影剂在靶标处的特定积累。为了利用MRI的卓越分辨率,将其应用于MRI分子成像,必须将g螯合物作为MRI造影剂(CA),与能够识别目标抗原决定簇的特定载体偶联。几个Gd(III)螯合物可以化学连接到相同的结合载体上,以便在单个靶向事件中递送CA(多聚体)的多个副本,从而提高分子探针的灵敏度。在本文中,三种新颖的双功能剂是带有一个用于与靶载体生物缀合的功能基团和​​四个用于MRI对比增强的Gd(III)-AAZTA螯合物功能(AAZTA = 6-氨基-6-甲基过氢-1,4-二氮杂四乙酸)。报告。四聚体衍生物的弛豫度为16.4±0.2 mMGd –1 s –1在21.5 MHz和25°C下,比母体单体Gd(III)-AAZTA高2.4倍。这些化合物可用作通用构建基块,以将预先形成的,高弛豫性和高密度Gd中心插入生物靶向载体。例如,我们描述了使用这些双功能的Gd(III)-螯合物来标记靶向血纤蛋白的肽。
更新日期:2018-02-22
down
wechat
bug