Poster Presentation 23rd International Society of Magnetic Resonance Conference 2023

Tumor-Targeted Para CEST Contrast Agent with 3-Phenyl Boronic Acid Attachment: A Promising Approach (#315)

Christu Rajan 1 , Jaya Seema 1 , Yu-Hsuan Yeh 1 2 , Yu-Wen Chen 1 3 , Dennis Hwang 1 3
  1. Institute of biomedical sciences, Academia Sinica, Taipei 115, Taiwan
  2. Department of Chemistry, National Taiwan Univesity, Taipei, Taiwan
  3. Biomedical Translation Research Center, Academia Sinica, Taipei 115, Taiwan

Our study presents the advancement of paramagnetic chemical exchange saturation transfer (ParaCEST) MRI as an innovative approach for imaging tumor regions. We tackled the challenge of sensitivity by creating a unique ParaCEST agent, combining 3-phenyl boronic acid (PBA) and 3,5-diamino benzoic acid-based first-generation dendrimers. The agent interacts with sialic acid diols, which are prevalent on tumor cell surfaces, thereby improving the specificity of tumor detection.

 

Our novel agent design introduces exchangeable amide protons (NH) via mono malonyl esters, which generate strong chemical exchange saturation transfer (CEST) peaks, thereby amplifying the sensitivity of ParaCEST imaging. To further enhance molecular flexibility and efficacy, we incorporated a glycine linker, facilitating optimal binding and detection of target tumor tissues.

 

In conclusion, our innovative synthesis of ParaCEST agents, incorporating dendrimers, 3-phenyl boronic acid, and glycine, represents a promising strategy for enhancing the sensitivity and effectiveness of CEST MRI in tumor imaging. This development has the potential to substantially advance tumor detection and diagnosis.