Recent advances in peptide-drug conjugates as anticancer agents
Yanyan Feng1, Tong Li1, Shijia Li1
1School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, 210023, China.
European Journal of Medicinal Chemistry
|December 19, 2025
Summary
Peptide-drug conjugates (PDCs) offer targeted cancer therapy by delivering drugs directly to tumors, minimizing side effects. This review explores PDC design, applications, and future directions, including PROTAC-based PDCs.
Area of Science:
- Oncology
- Pharmacology
- Drug Delivery
Background:
- Conventional chemotherapy faces challenges due to non-specificity and severe adverse effects.
- Peptide-drug conjugates (PDCs) represent a targeted therapeutic approach to enhance oncology treatment.
- PDCs aim to improve drug delivery to tumor sites, increasing efficacy and reducing toxicity.
Purpose of the Study:
- To review the structure, components, and functions of Peptide-drug conjugates (PDCs).
- To summarize recent advancements in PDC development, including target selection, design, and anticancer applications.
- To introduce PROTAC-based PDCs and discuss future challenges and solutions in PDC development.
Main Methods:
- Literature review of Peptide-drug conjugates (PDCs) in oncology.
- Analysis of PDC structure: tumor-homing peptide, chemical linker, and payload.
- Exploration of emerging technologies like PROTAC-based PDCs.
Main Results:
- PDCs enable targeted drug delivery, enhancing antitumor efficacy and minimizing damage to healthy tissues.
- Recent advances show progress in target selection, design strategies, and anticancer applications of PDCs.
- PROTAC-based PDCs represent an innovative approach in targeted protein degradation.
Conclusions:
- PDCs are a promising strategy for targeted cancer therapy, overcoming limitations of conventional chemotherapy.
- Continued research in PDC design and target selection is crucial for clinical success.
- Addressing current challenges will pave the way for the future development and application of PDCs in oncology.
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