Peptide-based building blocks as structural elements for supramolecular Gd-containing MRI contrast agents

Magnetic resonance imaging (MRI) is one of the most important clinic diagnostic tool used to obtain high‐quality body images. The administration of low‐molecular‐weight Gd complex–based MRI contrast agents (CAs) permits to increase the 1H relaxation rate of nearby water molecules, thus modulating signal intensity and contrast enhancement. Even if highly accurate, MRI modality suffers from its low sensitivity. Moreover, low‐molecular‐weight CAs rapidly equilibrate between the intravascular and extravascular spaces after their administration. In order to improve their sensitivity and limit the extravasation phenomenon, several macromolecular and supramolecular multimeric gadolinium complexes (dendrimers, polymers, carbon nanostructures, micelles, and liposomes) have been designed until now. Because of their biocompatibility, low immunogenicity, low cost, and easy synthetic modification, peptides are attractive building blocks for the fabbrication of novel materials for biomedical applications. We report on the state of the art of supramolecular CAs obtained by self‐assembly of three different classes of building blocks containing a peptide sequence, a gadolinium complex, and, if necessary, a third functional portion achieving the organization process.