Pharmaceutics, Volume 14, Issue 10
2022 October - 276 articles
Cover Story: A prodrug is bioreversible medication that is specifically converted to the active drugs by enzymes overexpressed in the tumor microenvironment, which can considerably reduce the chemotherapy-induced side effects. However, prodrug strategies usually have low antitumor efficacy compared to free drugs by delayed drug release. Herein, we propose tumor-specific monomethyl auristatin E (MMAE) prodrug nanoparticles for safe and effective chemotherapy. The cathepsin B-specific cleavable FRRG peptide and MMAE are chemically conjugated via one-step simple synthetic chemistry. The resulting FRRG-MMAE nanoparticles efficiently accumulated within tumor tissues and inhibited tubulin polymerization by releasing free MMAE in cathepsin B-overexpressing tumor cells. Collectively, this study provides a promising approach for safe and effective chemotherapy via MMAE-based prodrug nanoparticles. View this paper - Issues are regarded as officially published after their release is announced to the table of contents alert mailing list .
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