The ability to delineate and understand biological processes in vivo using a non-invasive technique would greatly improve our understanding of biological developmental processes and ultimately, the diagnosis of diseases. To this end, we have developed a new generation of bio-activated, self-immolative MRI contrast agents that function as reporter probes of in vivo enzyme activity using ߖgalactosidase. This new class of agents has improved kinetics of activation allowing for detection on a biologically relevant time scale. Optimization of this generation of probes includes a back-binding coordination moiety incorporated into a linker arm to further inhibit water access to the Gd(III) ion prior to enzymatic activation. Here, we describe the characterization of this class of agents and our strategy to optimize the change in relaxivity upon activation and in vitro analysis.

New generation of enzyme-activated MRI contrast agents

247th National Meeting (2014)

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