Nikita Oskolkov1,
Kannie W.Y. Chan2, Amnon Bar-Shir2, Peter C.M. van Zijl1,
3, Jeff W.M. Bulte2, 4, Assaf A. Gilad2,
4, Michael T. McMahon1, 3
1Russell
H. Morgan Department of Radiology and Radiological Science, The Johns Hopkins
University School of Medicine, Baltimore, MD, United States; 2Russell
H. Morgan Department of Radiology and Radiological Science, Johns Hopkins
University, Baltimore, MD, United States; 3F.M. Kirby Research
Center for Functional Brain Imaging, Kennedy Krieger Institute, Baltimore,
MD, United States; 4Cellular Imaging Section and Vascular Biology
Program, Institute for Cell Engineering, Baltimore, MD, United States
We have synthesized human protamine-1 (hPRM1), a compound biologically relevant for packing cellular DNA, which is rich in arginine and generates high CEST contrast associated with the exchangeable protons in the guanidyl group. We have also determined how the contrast varies upon binding of hPRM1 to nucleotides, the natural role of this protein, which is relevant to how it might perform in vivo as contrast material. This synthetic approach has resulted in a high yield and retention of the peptides ability to bind DNA, potentially enabling use of hPRM-1 as an alternative to recombinant or naturally occurring protamine.