Biocompatible, Biodegradable, and Enzymatic-Cleavable MRI Contrast Agents for Early Detection of Bone Metastatic Breast cancer
Final rept. 1 Apr 2011-31 Mar 2013
UTAH UNIV SALT LAKE CITY
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This concept award proposes to design and test a novel peptide-based MRI contrast agent for early detection of bone metastasis from breast cancer. The proposed imaging agent is consist of bone targeting moiety of Asp8 and MRI imaging moiety of DOTAGd with a cathepsin K cleavable peptide spacer. A solid phase peptide synthesis SPPS strategy was used to synthesize the peptide. Non-targeting and CTSK-insensitive controls were similarly prepared. The obtained imaging agent with a peptide sequence of Asp8CRPGGG has shown high binding affinity to hydroxyl apatite as well as biodegradability in the presence of cathepsin K. However, it also exhibited undesirable Gd chelation ability likely due to Asp8, resulting in its toxicity and limiting its use as a contrast agent for MRI applications.
- Medicine and Medical Research