A Review on the Current State and Future Perspectives of [Tc]Tc-Housed PSMA-i in Prostate Cancer.

Recently, prostate-specific membrane antigen (PSMA) has gained momentum in tumor nuclear molecular imaging as an excellent target for both the diagnosis and therapy of prostate cancer. Since 2008, after years of preclinical research efforts, a plentitude of radiolabeled compounds mainly based on low molecular weight PSMA inhibitors (PSMA-i) have been described for imaging and theranostic applications, and some of them have been transferred to the clinic. Most of these compounds include radiometals (e.

Water-Soluble [Tc(N)(PNP)] Moiety for Room-Temperature Tc Labeling of Sensitive Target Vectors.

The incorporation of bioactive molecules into a water-soluble [Tc][Tc(N)(PNP)]-based mixed compound is described. The method, which exploits the chemical properties of the new [Tc][Tc(N)(PNP3OH)] synthon [PNP3OH = ,-bis(di-hydroxymethylenphosphinoethyl)methoxyethylamine], was successfully applied to the labeling of small, medium (cysteine-functionalized biotin and c-RGDfK pentapeptide), and large molecules. Apomyoglobin was chosen as a model protein and derivatized site-specific enzymatic reaction catalyzed by transglutaminase (TGase) with the H-Cys-Gly-Lys-Gly-OH tetrapeptide for the insertion in the protein sequence of a reactive N-terminal Cys for Tc chelation.