Design and Synthesis of Novel Myristoylated Polyarginine Peptides for In Vivo Molecular Neuroimaging
Nabuurs R, Pham W, Van Buchem M, Moore A
Massachusetts General Hospital
Clinical application of potentially useful imaging agents for the detection of neurodegenerative diseases is hampered by the limited access of probes to the BBB. Here we developed Gd-associated fatty acylated polyargine (MPAP-Gd) as a probe to cross the BBB for molecular neuroimaging using MRI. The peptide backbone was synthesized by solid phase chemistry, while a fatty acid group was incorporated using Schotten-Baumann reaction. DOTA was conjugated to the peptide selectively to a lysine side chain on solid support followed by association with gadolinium to afford the final product. Assessment of the probes in vivo using MRI is currently underway.