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

Alexander L Nivorozhkin; Andrew F Kolodziej; Peter Caravan; Matthew T Greenfield; Randall B Lauffer; Thomas J McMurry

doi:10.1002/1521-3773(20010803)40:15<2903::AID-ANIE2903>3.0.CO;2-N

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.

Authors

Alexander L Nivorozhkin¹, Andrew F Kolodziej¹, Peter Caravan¹, Matthew T Greenfield¹, Randall B Lauffer¹, Thomas J McMurry¹

Affiliation

¹ EPIX Medical, Inc. 71 Rogers Street Cambridge, MA 02142 (USA) Fax: (+1) 617-250-6128.

PMID: 29711998
DOI: 10.1002/1521-3773(20010803)40:15<2903::AID-ANIE2903>3.0.CO;2-N

Abstract

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.