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Published on: September 3, 2013
A Sweet and Stable Strike: Multivalent Glucosylated Gd-DOTBA Conjugate with Ultrahigh Relaxivity for Targeted MRI of
Xinhui Xiao1,2, Yi Lu1, Weiyuan Xu2
1Department of Radiology, The Second Affiliated Hospital and Yuying Children's Hospital of Wenzhou Medical University, Wenzhou, Zhejiang 325027, China.
Abstract:
The early detection of aggressive malignancies remains challenging due to the limited performance of current clinical magnetic resonance imaging (MRI) contrast agents. This study developed a glucosylated gadolinium complex, Gd-DOTBA-Glc, as a high-relaxivity, target-specific MRI contrast agent. By employing an α-aryl substitution strategy, the agent achieves an enhanced longitudinal relaxation rate (r1 = 16.1 mM-1 s-1, approximately five times that of clinical Gd-DOTA). For targeting, covalently attached glucose moieties promote tumor accumulation through glucose transporters (GLUTs), particularly GLUT1, a mechanism validated by suppression of signal enhancement using the GLUT inhibitor WZB-117. In vivo, Gd-DOTBA-Glc at half the clinical dose (0.05 mmol/kg) produced tumor-specific contrast enhancement in orthotopic PDAC and subcutaneous TNBC models, outperforming nontargeted Gd-DOTBA-OH and clinical Gd-DOTA. This work demonstrates a strategy combining high relaxivity with metabolic targeting, offering a platform for early diagnosis of GLUTs-overexpressing cancers.
