Bifunctional coupling agents for radiolabeling of biomolecules and target-specific delivery of metallic radionuclides.

摘要: Receptor-based radiopharmaceuticals are of great current interest in molecular imaging and radiotherapy cancers, provide a unique tool for target-specific delivery radionuclides to the diseased tissues. In general, radiopharmaceutical can be divided into four parts: targeting biomolecule (BM), pharmacokinetic modifying (PKM) linker, bifunctional coupling or chelating agent (BFC), radionuclide. The serves as "carrier" specific PKM linkers used modify radiotracer excretion kinetics. BFC is needed radiolabeling biomolecules with metallic Different radiometals have significant difference their coordination chemistry, require BFCs different donor atoms chelator frameworks. Since radiometal chelate impact on physical biological properties radiopharmaceutical, its kinetics altered by environment various chelators coligand, if needed. This review will focus design chemistry technetium, copper, gallium, indium, yttrium lanthanide radiometals.