Research advances in peptide‒drug conjugates.

Author: Liming GONG ¹ ; Heming ZHAO ¹ ; Yanhong LIU ¹ ; Hao WU ² ; Chao LIU ¹ ; Shuangyan CHANG ¹ ; Liqing CHEN ¹ ; Mingji JIN ¹ ; Qiming WANG ¹ ; Zhonggao GAO ¹ ; Wei HUANG ¹
Author Information

1. State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
2. Department of Pharmacy, Yanbian University, Yanji 133000, China.
Publication Type:Review
Keywords: Drug delivery systems; Linkers; Peptides; Peptide‒drug conjugates; Prodrug strategy
From: Acta Pharmaceutica Sinica B 2023;13(9):3659-3677
CountryChina
Language:English
Abstract: Peptide‒drug conjugates (PDCs) are drug delivery systems consisting of a drug covalently coupled to a multifunctional peptide via a cleavable linker. As an emerging prodrug strategy, PDCs not only preserve the function and bioactivity of the peptides but also release the drugs responsively with the cleavable property of the linkers. Given the ability to significantly improve the circulation stability and targeting of drugs in vivo and reduce the toxic side effects of drugs, PDCs have already been extensively applied in drug delivery. Herein, we review the types and mechanisms of peptides, linkers and drugs used to construct PDCs, and summarize the clinical applications and challenges of PDC drugs.