A Bivalent Inhibitor of Prostate Specific Membrane Antigen Radiolabeled with Copper-64 with High Tumor Uptake and Retention.
Angew Chem Int Ed Engl
; 58(42): 14991-14994, 2019 10 14.
Article
in En
| MEDLINE
| ID: mdl-31437347
ABSTRACT
Molecules containing lysine-ureido-glutamate functional groups bind to the active site of prostate specific membrane antigen, which is overexpressed in prostate cancer. To prepare copper radiopharmaceuticals for the diagnosis and therapy of prostate cancer, macrobicyclic sarcophagine ligands tethered to either one or two lysine-ureido-glutamate functional groups through an appropriate linker have been prepared. Sarcophagine ligands can be readily radiolabeled with positron-emitting copper-64 at room temperature. The bivalent agent, in which two targeting groups are tethered to a single copper complex, dramatically outperforms the monomeric agent with respect to tumor uptake and retention. The high tumor uptake, low background, and prolonged tumor retention, even at 24â
hours post injection, suggest the bivalent agent is a promising diagnostic for prostate cancer and could be used for prospective dosimetry for therapy with a copper-67 variant.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Prostatic Neoplasms
/
Copper Radioisotopes
/
Radiopharmaceuticals
/
Glutamate Carboxypeptidase II
/
Dipeptides
/
Glutamates
Limits:
Animals
/
Humans
/
Male
Language:
En
Journal:
Angew Chem Int Ed Engl
Year:
2019
Type:
Article
Affiliation country:
Australia