Structure-Guided Design and Synthesis of a Mitochondria-Targeting Near-Infrared Fluorophore with Multimodal Therapeutic Activities

© 2017 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Bibliographische Detailangaben
Veröffentlicht in:Advanced materials (Deerfield Beach, Fla.). - 1998. - 29(2017), 43 vom: 05. Nov.
1. Verfasser: Tan, Xu (VerfasserIn)
Weitere Verfasser: Luo, Shenglin, Long, Lei, Wang, Yu, Wang, Dechun, Fang, Shengtao, Ouyang, Qin, Su, Yongping, Cheng, Tianmin, Shi, Chunmeng
Format: Online-Aufsatz
Sprache:English
Veröffentlicht: 2017
Zugriff auf das übergeordnete Werk:Advanced materials (Deerfield Beach, Fla.)
Schlagworte:Journal Article cancer theranostics heptamethine cyanine dyes mitochondria-targeting agents near-infrared imaging phototherapy Fluorescent Dyes Indocyanine Green IX6J1063HV
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245 1 0 |a Structure-Guided Design and Synthesis of a Mitochondria-Targeting Near-Infrared Fluorophore with Multimodal Therapeutic Activities 
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520 |a An urgent challenge for imaging-guided disease-targeted multimodal therapy is to develop the appropriate multifunctional agents to meet the requirements for potential applications. Here, a rigid cyclohexenyl substitution in the middle of a polymethine linker and two asymmetrical amphipathic N-alkyl side chains to indocyanine green (ICG) (the only FDA-approved NIR contrast agent) are introduced, and a new analog, IR-DBI, is developed with simultaneous cancer-cell mitochondrial targeting, NIR imaging, and chemo-/PDT/PTT/multimodal therapeutic activities. The asymmetrical and amphipathic structural modification renders IR-DBI a close binding to albumin protein site II to form a drug-protein complex and primarily facilitates its preferential accumulation at tumor sites via the enhanced permeability and retention (EPR) effect. The released IR-DBI dye is further actively taken up by cancer cells through organic-anion-transporting polypeptide transporters, and the lipophilic cationic property leads to its selective accumulation in the mitochondria of cancer cells. Finally, based on the high albumin-binding affinity, IR-DBI is modified into human serum albumin (HSA) via self-assembly to produce a nanosized complex, which exhibits significant improvement in the cancer targeting and multimodal cancer treatment with better biocompatibility. This finding may present a practicable strategy to develop small-molecule-based cancer theranostic agents for simultaneous cancer diagnostics and therapeutics 
650 4 |a Journal Article 
650 4 |a cancer theranostics 
650 4 |a heptamethine cyanine dyes 
650 4 |a mitochondria-targeting agents 
650 4 |a near-infrared imaging 
650 4 |a phototherapy 
650 7 |a Fluorescent Dyes  |2 NLM 
650 7 |a Indocyanine Green  |2 NLM 
650 7 |a IX6J1063HV  |2 NLM 
700 1 |a Luo, Shenglin  |e verfasserin  |4 aut 
700 1 |a Long, Lei  |e verfasserin  |4 aut 
700 1 |a Wang, Yu  |e verfasserin  |4 aut 
700 1 |a Wang, Dechun  |e verfasserin  |4 aut 
700 1 |a Fang, Shengtao  |e verfasserin  |4 aut 
700 1 |a Ouyang, Qin  |e verfasserin  |4 aut 
700 1 |a Su, Yongping  |e verfasserin  |4 aut 
700 1 |a Cheng, Tianmin  |e verfasserin  |4 aut 
700 1 |a Shi, Chunmeng  |e verfasserin  |4 aut 
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773 1 8 |g volume:29  |g year:2017  |g number:43  |g day:05  |g month:11 
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