Antibody-drug conjugates:Recent advances in payloads

作     者：Zhijia Wang Hanxuan Li Lantu Gou Wei Li Yuxi Wang 

作者机构：Department of Pulmonary and Critical Care MedicineTargeted Tracer Research and Development LaboratoryInstitute of Respiratory HealthFrontiers Science Center for Disease-related Molecular NetworkNational Clinical Research Center for GeriatricsState Key Laboratory of BiotherapyPrecision Medicine Key Laboratory of Sichuan Province&Precision Medicine Research CenterWest China HospitalSichuan UniversityChengdu 610041China Frontiers Medical CenterTianfu Jincheng LaboratoryChengdu 610212China Department of Pharmaceutical SciencesCollege of PharmacyUniversity of Tennessee Health Science CenterMemphisTN 38163USA 

出 版 物：《Acta Pharmaceutica Sinica B》 (药学学报（英文版）)

年 卷 期：2023年第13卷第10期

页      面：4025-4059页

核心收录：

学科分类：100702[医学-药剂学] 1007[医学-药学(可授医学、理学学位)] 1006[医学-中西医结合] 100602[医学-中西医结合临床] 10[医学] 

基　　金：provided by the National Natural Science Foundation of China(82073318) the Fundamental Research Funds for the Central Universities(SCU2022D025,0082604151345,China) Sichuan Science and Technology Program Projects(2019YFS0003,China)to Yuxi Wang provided by the University of Tennessee College of Pharmacy Drug Discovery Center to Wei Li 

主　　题：Antibody‒drug conjugates Dual payloads Tubulin inhibitors DNA damaging agents PROTACs RNA targeting agents 

摘      要：Antibody-drug conjugates(ADCs),which combine the advantages of monoclonal antibodies with precise targeting and payloads with efficient killing,show great clinical therapeutic *** ADCs’payloads play a key role in determining the efficacy of ADC drugs and thus have attracted great attention in the *** ideal ADC payload should possess sufficient toxicity,low immunogenicity,high stability,and modifiable functional *** ADC payloads include tubulin inhibitors and DNA damaging agents,with tubulin inhibitors accounting for more than half of the ADC drugs in clinical ***,due to clinical limitations of traditional ADC payloads,such as inadequate efficacy and the development of acquired drug resistance,novel highly efficient payloads with diverse targets and reduced side effects are being *** perspective summarizes the recent research advances of traditional and novel ADC payloads with main focuses on the structure-activity relationship studies,co-crystal structures,and designing strategies,and further discusses the future research directions of ADC *** review also aims to provide valuable references and future directions for the development of novel ADC payloads that will have high efficacy,low toxicity,adequate stability,and abilities to overcome drug resistance.