| Autor: |
John F. Valliant, Alla Darwish, John W. Babich, Stephanie M. Rathmann, Shawn Hillier, Shannon Czorny, Megan Blacker, John Joyal, Nancy Janzen |
| Rok vydání: |
2012 |
| Předmět: |
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| Zdroj: |
ACS Medicinal Chemistry Letters. 3:313-316 |
| ISSN: |
1948-5875 |
| DOI: |
10.1021/ml300003v |
| Popis: |
A new prosthetic group referred to as the triazole appending agent (TAAG) was developed as a means to prepare targeted radioiodine-based molecular imaging and therapy agents. Tributyltin-TAAG and the fluorous analogue were synthesized in high yield using simple click chemistry and the products labeled in greater than 95% RCY with (123)I. A TAAG derivative of an inhibitor of prostate-specific membrane antigen was prepared and radiolabeled with (123)I in 85% yield where biodistribution studies in LNCap prostate cancer tumor models showed rapid clearance of the agent from nontarget tissues and tumor accumulation of 20% injected dose g(-1) at 1 h. The results presented demonstrate that the TAAG group promotes minimal nonspecific binding and that labeled conjugates can achieve high tumor uptake and exquisite target-to-nontarget ratios. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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