文献类型：期刊文献

英文题名：Antibody-drug conjugates for targeted cancer therapy: Recent advances in potential payloads

作者：Xi, Meiyang[1,2];Zhu, Jingjing[3];Zhang, Fengxia[3];Shen, Hualiang[1,2];Chen, Jianhui[2];Xiao, Ziyan[2];Huangfu, Yanping[2];Wu, Chunlei[1,2];Sun, Haopeng[4];Xia, Gang[3]

机构：[1]Shaoxing Univ, Zhejiang Engn Res Ctr Fat Soluble Vitamin, Shaoxing 312000, Peoples R China;[2]Shaoxing Univ, Coll Chem & Chem Engn, Shaoxing 312000, Peoples R China;[3]NovoCodex Biopharmaceut Co Ltd, Shaoxing 312090, Peoples R China;[4]China Pharmaceut Univ, Dept Med Chem, Nanjing 210009, Peoples R China

年份：2024

卷号：276

外文期刊名：EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

收录：SCI-EXPANDED(收录号：WOS:001283909900001)、、Scopus(收录号：2-s2.0-85199495851)、WOS

基金：The authors greatly acknowledge the support from the National Natural Science Foundation of China (No. 22278270) .

语种：英文

外文关键词：Payload; Antibody-drug conjugate (ADC); Cancer therapy

外文摘要：Antibody-drug conjugates (ADCs) represent a promising cancer therapy modality which specifically delivers highly toxic payloads to cancer cells through antigen-specific monoclonal antibodies (mAbs). To date, 15 ADCs have been approved and more than 100 ADC candidates have advanced to clinical trials for the treatment of various cancers. Among these ADCs, microtubule-targeting and DNA-damaging agents are at the forefront of payload development. However, several challenges including toxicity and drug resistance limit the potential of this modality. To tackle these issues, multiple innovative payloads such as immunomodulators and proteolysis targeting chimeras (PROTACs) are incorporated into ADCs to enable multimodal cancer therapy. In this review, we describe the mechanism of ADCs, highlight the importance of ADC payloads and summarize recent progresses of conventional and unconventional ADC payloads, trying to provide an insight into payload diversification as a key step in future ADC development.