文献类型：期刊文献

英文题名：Recent Advances in Augmenting the Therapeutic Efficacy of Peptide-Drug Conjugates

作者：Ma, Jiahui[1];Wang, Xuedan[2];Hu, Yonghua[1,3];Ma, Jianping[2];Ma, Yaping[4];Chen, Hao[1];Han, Zhijian[1]

第一作者：Ma, Jiahui

通信作者：Chen, H[1];Han, ZJ[1]

机构：[1]Lanzhou Univ, Hosp 2, Dept Tumor Ctr, Clin Med Sch 2,Gansu Prov Key Lab Environm Oncol, Lanzhou 730000, Peoples R China;[2]Lanzhou Univ Technol, Sch Life Sci & Engn, Lanzhou 730050, Peoples R China;[3]Gansu Univ Chinese Med, Lanzhou 730000, Peoples R China;[4]Shenzhen DIVBIO Pharmaceut, Shenzhen 518057, Peoples R China

第一机构：Lanzhou Univ, Hosp 2, Dept Tumor Ctr, Clin Med Sch 2,Gansu Prov Key Lab Environm Oncol, Lanzhou 730000, Peoples R China

通信机构：[1]corresponding author), Lanzhou Univ, Hosp 2, Dept Tumor Ctr, Clin Med Sch 2,Gansu Prov Key Lab Environm Oncol, Lanzhou 730000, Peoples R China.

年份：2025

卷号：68

期号：9

起止页码：9037

外文期刊名：JOURNAL OF MEDICINAL CHEMISTRY

收录：;Scopus(收录号：2-s2.0-105003427242);WOS:【SCI-EXPANDED(收录号:WOS:001473243600001)】；

基金：This work was supported by National Natural Science Foundation of China (no. 82473266, no. 82160129), Cuiying Scientific and Technological Innovation Program of Lanzhou University Second Hospital (no. CY2021-MS-B09 and no. CY2023-ZD-01), Key Talents Project of Gansu Province (no. 2019RCXM020), Science and Technology Project of Chengguan District of Lanzhou City (no. 2020JSCX0073), Gansu Provincial Department of Education Project (no. 2022B-034), Gansu Provincial Science and Technology Major Project (no. 24ZDFA011), Gansu Provincial Innovation Fund for Small and Medium-Sized Technology-based Firms (no. 24CXGA107).

语种：英文

摘要：There is an urgent need for the development of safe and effective modalities for the treatment of diseases owing to drug resistance, undesired side effects, and poor clinical outcomes. Combining cell-targeting and efficient cell-killing properties, peptide-drug conjugates (PDCs) have demonstrated superior efficacy compared with peptides and payloads alone. However, innovative molecular designs of PDCs are essential for further improving targeting precision, protease resistance and stability, cell permeability, and overall treatment efficacy. Several strategies have been developed to address these challenges, such as multivalency approaches, bispecific targeting, and long-acting PDCs. Other novel strategies, including overcoming biological barriers, conjugating novel functional payloads, and targeting macropinocytosis, have also shown promise. This perspective compiles the most recent strategies for enhancing PDC treatment efficacy, highlights key advancements in PDC, and provides insights on future directions for the development of novel PDCs.