Figure 1 | NPG Asia Materials

Figure 1

From: Nuclease-resistant synthetic drug-DNA adducts: programmable drug-DNA conjugation for targeted anticancer drug delivery

Figure 1

Schematic illustration of nuclease-resistant synthetic drug-DNA adducts as a simple, yet versatile and programmable platform for targeted anticancer drug delivery. In a simple reaction, multiple copies of drugs (e.g., doxorubicin) were specifically conjugated on deoxyguanosine of DNA, making it programmable to design DNA and drugs for drug-DNA adduct-based drug delivery. Drug fluorescence was quenched upon conjugation to DNA. Drug-DNA adducts were stable at relatively low temperature, yet the cleavable methylene linkage (heat labile) between drug moieties and DNA allows for drug release at a physiological temperature. Drug-DNA adducts were resistant to nuclease degradation and maintained the functionalities of specific cancer cell recognition by drug-aptamer adducts and hybridization-mediated formation of drug-DNA nanoadducts. Drug-aptamer adducts were further studied for targeted anticancer drug delivery in a xenograft tumor mouse model, and showed potent antitumor efficacy while significantly reducing the side effects of doxorubicin.

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