Self-assembly of enzymes and prodrugs with clickable amino acids for nucleus-targeted cancer therapy.

A nucleus-targeted nanocomposite was prepared by clickable amino acid-tuned one-step co-assembly of proteins and chemotherapeutics. The nanocomposite with favorable pharmacokinetic behavior can effectively accumulate in the nucleus, thereby significantly enhancing the anticancer therapeutic effect both in vitro and in vivo.

Research progress in nucleus-targeted tumor therapy.

The nucleus is considered the most important organelle in the cell as it plays a central role in controlling cell reproduction, metabolism, and the cell cycle. The successful delivery of drugs into the nucleus can achieve excellent therapeutic effects, which reveals the potential of nucleus-targeted therapy in precision medicine. However, the transportation of therapeutics into the nucleus remains a significant challenge due to various biological barriers. Herein, we summarize the recent progress in the nucleus-targeted drug delivery system (NDDS). The structures of the nucleus and nuclear envelope are first described in order to understand the mechanisms by which drugs cross the nuclear envelope. Then, various drug delivery strategies based on the mechanisms and their applications are discussed. Finally, the challenges and solutions in the field of nucleus-targeted drug delivery are raised for developing a more efficient NDDS and promoting its clinical transformation.

Nucleus-selective self-augmenting cascade nanoassemblies for targeted synergistic photo-chemo therapy of tumors.

A nucleus-targeted enzyme prodrug nanocomposite, assembled from ß-cyclodextrin-lysine (CL), catalase (CAT), Pt(IV) and chlorin e6 (Ce6), was developed for self-augmenting cascade photo-chemo therapy of tumors. It can effectively transport through the cytoplasm and accumulate in the nucleus, thereby significantly inhibiting tumor growth and lung metastasis.