Clicking Tc-99m SPECT Probes Together
Molecular Assembly of Multifunctional 99mTc Radiopharmaceuticals Using "Clickable" Amino Acid Derivatives
Starting from azide-functionalized biomolecules and readily available alkyne pro-chelators derived from amino acids, Mindt and colleagues assembled multifunctional conjugates by convenient one-pot procedures without the need for protecting groups. They applied this copper(I)-catalyzed alkyne–azide cycloaddition (CuAAC) methodology to the preparation of a 99mTc-labeled conjugate comprising a tumor-targeting peptide sequence (bombesin(7–14)) and a low-molecular-weight albumin binder (a pharmacological modifier that prolongs the conjugate's blood circulation lifetime).
The possibility of selectively combining two different groups with biological function and a metal chelating system in a single step is a very attractive feature for the development of metallic radiotracers and opens numerous applications with great potential, including the design of radiopharmaceuticals with improved biological characteristics, multimodality imaging probes, bivalent or bi-specific targeting agents, and conjugates useful for combination therapies.
Original publication: Thomas Mindt et al.; "Molecular Assembly of Multifunctional 99mTc Radiopharmaceuticals Using "Clickable" Amino Acid Derivatives"; ChemMedChem 2010.
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