Novel Approach to Prepare {sup 99m}Tc-Based Multivalent RGD Peptides [electronic resource].
- Published:
- Washington, D.C. : United States. Dept. of Energy, 2012.
Oak Ridge, Tenn. : Distributed by the Office of Scientific and Technical Information, U.S. Dept. of Energy. - Additional Creators:
- Purdue University
United States. Department of Energy
United States. Department of Energy. Office of Scientific and Technical Information - Access Online:
- www.osti.gov
- Summary:
- This project presents a novel approach to prepare the {sup 99m}Tc-bridged multivalent RGD (arginine-glycine-aspartate) peptides. This project will focus on fundamentals of {sup 99m}Tc radiochemistry. The main objective of this project is to demonstrate the proof-of-principle for the proposed radiotracers. Once a kit formulation is developed for preparation of the {sup 99m}Tc-bridged multivalent RGD peptides, various tumor-bearing animal models will be used to evaluate their potential for SPECT (single photon-emission computed tomography) imaging of cancer. We have demonstrated that (1) multimerization of cyclic RGD peptides enhances the integrin α{sub v}β₃ bonding affinity and radiotracer tumor uptake; (2) addition of G₃ or PEG₄ linkers makes it possible for two RGD motifs in 3P-RGD₂ and 3G-RGD₂ to achieve simultaneous integrin α{sub v}β₃ binding; and (3) multimers are actually bivalent (not multivalent), the presence of extra RGD motifs can enhance the tumor retention time of the radiotracer.
- Subject(s):
- Note:
- Published through SciTech Connect.
10/24/2012.
"er64684"
Shuang Liu. - Type of Report and Period Covered Note:
- Final;
- Funding Information:
- FG02-08ER64684
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