Conjugation of 1,4,7,10-Tetraazacyclododecane-1,4,7,10-Tetracetic Acid (DOTA) and its Derivatives to Peptides: Synthesis, Applications and Future Prospects

The universal chelator 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetracetic acid (DOTA) and its bifunctional derivatives are widely used to label peptides with various metal ions for biomedical applications. Bifunctional DOTA derivatives and their conjugation to peptides has become an established strategy for constructing target-specific metal containing agents including targeted MRI contrast agents and diagnostic and therapeutic radiopharmaceuticals. This review covers the synthesis of DOTA-peptide conjugates, their potential use in biomedicine and the problems related to their applications.