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Updated: Mar 18, 2026
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Constructing Cyclic Peptides Using an On-Tether Sulfonium Center
Published on: September 28, 2022
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Peptides as multifunctional linchpins in targeted drug conjugates
Xue Li1, Yuechen Qian1, Jiongjia Cheng2
1Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University Nanjing 211198 China qianchu@cpu.edu.cn.
RSC Medicinal Chemistry
|March 16, 2026
Summary
Peptide-drug conjugates (PDCs) enhance targeted therapy by using peptides for precise drug delivery. Advances in peptide discovery and optimization aim to overcome challenges for next-generation precision medicines.
Area of Science:
- Biochemistry and Molecular Biology
- Pharmacology and Pharmaceutical Sciences
- Oncology
Background:
- Peptide-drug conjugates (PDCs) are advanced therapeutics designed for targeted drug delivery.
- They utilize peptides to enhance specificity and reduce systemic toxicity in treating complex diseases.
Purpose of the Study:
- To review strategic advances in peptide discovery, modification, and optimization for PDCs.
- To discuss overcoming clinical translation challenges and future perspectives for next-generation PDCs.
Main Methods:
- Review of current literature on peptide discovery and engineering for drug conjugates.
- Analysis of strategies to improve peptide stability, tissue penetration, and targeting selectivity.
- Exploration of peptide-based linkers for controlled drug release.
Main Results:
- Peptides serve as homing devices for selective targeting of receptors overexpressed on diseased cells.
- Engineered peptides can function as enzymatically cleavable linkers for localized drug release.
- Current challenges include peptide instability, limited tissue penetration, and insufficient targeting selectivity.
Conclusions:
- Strategic advances in peptide engineering are crucial for overcoming PDC limitations.
- Next-generation PDCs hold significant potential as highly effective precision medicines.
- Further research is needed to fully realize the therapeutic promise of PDCs.
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