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Mitochondria-targeting Drug Conjugates for Cytotoxic, Anti-Oxidizing and Sensing Purposes: Current Strategies and Future Perspectives

Mitochondria-targeting Drug Conjugates for Cytotoxic, Anti-Oxidizing and Sensing Purposes: Current Strategies and Future Perspectives

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

Acta Pharm Sin B. 2018 Oct;8(6):862-880.

PMID: 30505656

Abstract:

Mitochondrial targeting is a promising approach for solving current issues in clinical application of chemotherapy and diagnosis of several disorders. Here, we discuss direct conjugation of 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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP1334850995	MitoTEMPO		1334850-99-5	Price
AP7790398	Platinum(II) iodide		7790-39-8	Price

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