Journal
CHEMICAL COMMUNICATIONS
Volume -, Issue 5, Pages 493-512Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/b814903h
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Funding
- Molecular Insight Pharmaceuticals, Inc
- Department of Energy (DOE), Office of Health and Environmental Research [D2-FG02-99ER62791]
- National Institutes of Health
- National Institute of Allergy and Infectious Diseases [STTR 1R41 A1044080-01]
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Radiolabeled biomolecules can be used to visualize a variety of diseases through interaction with specific cell receptors. A key step is the introduction of a molecular entity that allows facile labeling with the medically useful radionuclide Tc-99m without significant alteration of the structure and function of the biomolecule. One strategy focuses on the design of single amino acid chelates (SAACs), novel bifunctional chelators constructed from derivatized amino acids or amino acid analogues. The chelating terminus of the SAAC has been designed for effective coordination to the {Tc-99m(CO)(3)}(+) core, while the other terminus allows incorporation into any position along a peptide sequence or into a variety of biomolecules. In applications to peptidic materials, the approach affords significant exibility in the choice of donors for Tc-99m coordination combined with the considerable advantages of routine solid phase synthetic techniques. The methodology allows libraries of peptidebased Tc-99m(I) and Re-186,Re-188(I) radiopharmaceuticals to prepared using conventional automated peptides synthesis. Other biomolecules, including nucleosides, carbohydrates, folic acid and vitamin B12 are also readily modified using analogous methods. The approach also allows the preparation of isostructural Tc-99m and Re complexes for the correlation of in vivo and in vitro imaging studies.
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