Enzyme-Activated Gd3+ Magnetic Resonance Imaging Contrast Agents with a Prominent Receptor-Induced Magnetization Enhancement

Angew Chem Int Ed Engl. 2001 Aug 3;40(15):2903-2906. doi: 10.1002/1521-3773(20010803)40:15<2903::AID-ANIE2903>3.0.CO;2-N.


Clinically relevant relaxivity enhancement of a magnetic resonance imaging (MRI) contrast agent has been achieved by using prodrug Gd3+ complexes (see picture, DTPA=diethylenetriaminepentaaceto). Enzymatic cleavage of lysine residues from the prodrug exposes a group that has a high affinity to human serum albumin and promotes enhanced relaxivity, thus enabling the detection of targets at submicromolar concentrations.

Keywords: MRI; chelates; inhibitors; lanthanides; peptides.