Intracellular Activation of Anticancer Therapeutics Using Polymeric Bioorthogonal Nanocatalysts. Issue 5 (13th December 2020) - Zhang, Xianzhi
Abstract: Bioorthogonal catalysis provides a promising strategy for imaging and therapeutic applications, providing controlled in situ activation of pro‐dyes and prodrugs. In this work, the use of a polymeric scaffold to encapsulate transition metal catalysts (TMCs), generating bioorthogonal "polyzymes, " is presented. These polyzymes enhance the stability of TMCs, protecting the catalytic centers from deactivation in biological media. The therapeutic potential of these polyzymes is demonstrated by the transformation of a nontoxic prodrug to an anticancer drug (mitoxantrone), leading to the cancer cell death in vitro. Abstract : Ruthenium catalysts are encapsulated into the hydrophobic pocket of polymers to provide bioorthogonal "polyzymes" with enhanced catalyst stability. These polyzymes uncage imaging and anticancer therapeutics in cells.