Preclinical Evaluation of a Novel High-Affinity Radioligand [^99mTc]Tc-BQ0413 Targeting Prostate-Specific Membrane Antigen (PSMA).

ABSTRACT: Radionuclide imaging using radiolabeled inhibitors of prostate-specific membrane antigen (PSMA) can be used for the staging of prostate cancer. Previously, we optimized the Glu-urea-Lys binding moiety using a linker structure containing 2-napththyl-L-alanine and L-tyrosine. We have now designed a molecule that contains mercaptoacetyl-triglutamate chelator for labeling with Tc-99m (designated as BQ0413). The purpose of this study was to evaluate the imaging properties of [^99mTc]Tc-BQ0413. PSMA-transfected PC3-pip cells were used to evaluate the specificity and affinity of [^99mTc]Tc-BQ0413 binding in vitro. PC3-pip tumor-bearing BALB/C nu/nu mice were used as an in vivo model. [^99mTc]Tc-BQ0413 bound specifically to PC3-pip cells with an affinity of 33 ± 15 pM

SUBMITTER: Bezverkhniaia E 

PROVIDER: S-EPMC10743726 | biostudies-literature | 2023 Dec

REPOSITORIES: biostudies-literature