Mitochondria-targeting drug conjugates for cytotoxic, anti-oxidizing and sensing purposes:current strategies and future perspectives

作     者：Gantumur Battogtokh Yeon Su Choi Dong Seop Kang Sang Jun Park Min Suk Shim Kang Moo Huh Yong-Yeon Cho Joo Young Lee Hye Suk Lee Han Chang Kang 

作者机构：Department of Pharmacy Integrated Research Institute of Pharmaceutical Sciences and BK21 PLUS Team for Creative Leader Program for Pharmacomics-based Future Pharmacy College of Pharmacy The Catholic University of Korea Division of Bioengineering Incheon National University Department of Polymer Science and Engineering Chungnam National University 

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

年 卷 期：2018年第8卷第6期

页      面：862-880页

核心收录：

学科分类：1007[医学-药学(可授医学、理学学位)] 1006[医学-中西医结合] 100706[医学-药理学] 100602[医学-中西医结合临床] 10[医学] 

基　　金：supported by the National Research Foundation of Korea (NRF)funded by the Korean government (MSIT) (NRF2017R1A4A1015036 and NRF-2015R1A1A05001459) the study was supported by BK21PLUS grant of NRF funded by the Korean government (ME) (22A20130012250) 

主　　题：Anticancer agents Antioxidants Direct conjugation Mitochondria-targeting Sensing agents 

摘      要：mitochondrial-targeting moieties to anticancer drugs, antioxidants and sensor molecules. Among them, the most widely applied mitochondrial targeting moiety is triphenylphosphonium(TPP), which is a delocalized cationic lipid that readily accumulates and penetrates through the mitochondrial membrane due to the highly negative mitochondrial membrane potential. Other moieties, including short peptides,dequalinium, guanidine, rhodamine, and F16, are also known to be promising mitochondrial targeting agents. Direct conjugation of mitochondrial targeting moieties to anticancer drugs, antioxidants and sensors results in increased cytotoxicity, anti-oxidizing activity and sensing activity, respectively,compared with their non-targeting counterparts, especially in drug-resistant cells. Although many mitochondria-targeted anticancer drug conjugates have been investigated in vitro and in vivo, further clinical studies are still needed. On the other hand, several mitochondria-targeting antioxidants have been analyzed in clinical phases I, II and III trials, and one conjugate has been approved for treating eye disease in Russia. There are numerous ongoing studies of mitochondria-targeted sensors.