![]() ![]() At a pole apart from surgical implantation of macroscopic objects are various strategies for molecular localization of therapeutic agents at or near the tumor site. While successful for the treatment of localized solid tumor cancers, brachytherapy has not been adapted for treatment of metastatic cancer given the challenge of identification and surgical implantation in metastases. β ραχυ′), meaning “short” or “few”, refers to the proximal location of the radionuclide-bearing seeds (typically pins or beads) to the diseased tissue. Taken together, blending biomedical strategies of enzyme prodrug therapy with materials chemistry concerning substances that undergo AIE may comprise a step forward on the long road toward molecular brachytherapy.īrachytherapy is a medical treatment where radionuclide-bearing macroscopic objects are implanted in a tumor. Altogether, 21 compounds were synthesized (18 new, 3 known via new routes). The aggregation is essential to molecular brachytherapy, whereas the induced emission of AIE is not essential but provides a convenient basis for research development. The pegylated phosphodiester-iodinated benzothiazole undergoes conversion from aqueous-soluble to aqueous-insoluble upon treatment with a phosphatase or phosphodiesterase. ![]() In particular, (1) the 2-(2-hydroxyphenyl) unit was derivatized to bear a pegylated phosphodiester that imparts water solubility yet undergoes enzymatic cleavage, and (2) a p-phenol unit was attached to the benzo moiety to provide a reactive site for final-step iodination (here examined with natural abundance iodide). Here, several 2-(2-hydroxyphenyl)benzothiazole substrates that readily aggregate in aqueous solution (and afford AIE) were elaborated in this regard. ![]() In distinct research, the advent of molecular designs for aggregation-induced emission (AIE) suggests translational use in molecular brachytherapy. Such a molecular brachytherapy has been scarcely investigated. A related strategy with radiotherapeutics entails enzymatically promoted conversion of a soluble to insoluble radiotherapeutic agent, thereby immobilizing the latter at the target site. A limitation may be the diffusion of the active drug away from the antibody target site. A targeted strategy for treating cancer is antibody-directed enzyme prodrug therapy, where the enzyme attached to the antibody causes conversion of an inactive small-molecule prodrug into an active drug. ![]()
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