Chiral Gd-DOTA as a Versatile Platform for Hepatobiliary and Tumor Targeting MRI Contrast Agents

The leakage of gadolinium ions (Gd3+) from commercial Gd3+-based contrast agents (GBCAs) in patients is currently the major safety concern in clinical magnetic resonance imaging (MRI) scans, and the lack of task-specific GBCAs limits its usage in the early detection of disease and imaging of specifi...

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Veröffentlicht in:Journal of medicinal chemistry 2023-11, Vol.66 (21), p.14669-14682
Hauptverfasser: Xu, Weiyuan, Ye, Xinjian, Wu, Min, Jiang, Xin, Hugo TSE, Lik Hang, Gu, Yanjuan, Shu, Kun, Xu, Liuhui, Jian, Yong, Mo, Gengshen, Xu, Jiao, Ding, Yinghui, Gao, Ruonan, Shen, Jianliang, Ye, Fangfu, Yan, Zhihan, Dai, Lixiong
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Sprache:eng
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Zusammenfassung:The leakage of gadolinium ions (Gd3+) from commercial Gd3+-based contrast agents (GBCAs) in patients is currently the major safety concern in clinical magnetic resonance imaging (MRI) scans, and the lack of task-specific GBCAs limits its usage in the early detection of disease and imaging of specific biological regions. Herein, ultrastable GBCAs were constructed via decorating chiral Gd-DOTA with a phenylic analogue to one of the pendent arms, and the stability constant was determined as high as 27.08, accompanied by negligible decomplexation in 1 M of HCl over 2 years. A hepatic-specific chiral Gd-DOTA was screened out as a potential alternative to commercial Gd-EOB-DTPA, while combination with functional molecules favored chiral Gd-DOTA as tumor targeting probes. Therefore, the novel chiral Gd-DOTA is believed to be an ideal platform for designing the next generation of GBCAs for various clinical purposes due to its outstanding inert nature.
ISSN:0022-2623
1520-4804
DOI:10.1021/acs.jmedchem.3c01183