Devkumar Mustafi1, Elizabeth Peng1, Sean Foxley2, Gregory S. Karczmar2, Marta Zamora2, John W. Ejnik3, Heather Martin3
1Biochemistry & Molecular Biology, The University of Chicago, Chicago, IL, USA; 2Radiology, The University of Chicago, Chicago, IL, USA; 3Chemistry, Northern Michigan University, Marquette, MI, USA
Current gadolinium-based MRI contrast agents are non-specific for cancer and quickly wash out of the blood. Non-toxic vanadyl chelates (VCs) interact with intracellular glycolytic enzymes and, therefore, selectively accumulate in highly glycolytic cancer cells. They bind to serum proteins; this increases their blood half-life and results in selective leakage from hyperpermeable tumor vasculature. We have characterized the binding interactions between a VC and albumin. In vitro measurements of VC uptake by tumor and muscle tissues, and in vivo MRI studies, demonstrate that VC is a blood-pool agent that accumulates within cancer cells, thereby preferentially enhancing MR images of rodent tumors.