Premium
Synthesis and Evaluation of Gd III ‐Based Magnetic Resonance Contrast Agents for Molecular Imaging of Prostate‐Specific Membrane Antigen
Author(s) -
Banerjee Sangeeta Ray,
Ngen Ethel J.,
Rotz Matthew W.,
Kakkad Samata,
Lisok Ala,
Pracitto Richard,
Pullambhatla Mrudula,
Chen Zhengping,
Shah Tariq,
Artemov Dmitri,
Meade Thomas J.,
Bhujwalla Zaver M.,
Pomper Martin G.
Publication year - 2015
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201503417
Subject(s) - molecular imaging , glutamate carboxypeptidase ii , magnetic resonance imaging , prostate cancer , in vivo , gadolinium , chemistry , prostate , mri contrast agent , biomarker , nuclear magnetic resonance , cancer , medicine , radiology , biochemistry , biology , physics , microbiology and biotechnology , organic chemistry
Magnetic resonance (MR) imaging is advantageous because it concurrently provides anatomic, functional, and molecular information. MR molecular imaging can combine the high spatial resolution of this established clinical modality with molecular profiling in vivo. However, as a result of the intrinsically low sensitivity of MR imaging, high local concentrations of biological targets are required to generate discernable MR contrast. We hypothesize that the prostate‐specific membrane antigen (PSMA), an attractive target for imaging and therapy of prostate cancer, could serve as a suitable biomarker for MR‐based molecular imaging. We have synthesized three new high‐affinity, low‐molecular‐weight Gd III ‐based PSMA‐targeted contrast agents containing one to three Gd III chelates per molecule. We evaluated the relaxometric properties of these agents in solution, in prostate cancer cells, and in an in vivo experimental model to demonstrate the feasibility of PSMA‐based MR molecular imaging.