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231225s2018 xx |||||o 00| ||eng c |
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|a 10.1002/adma.201704888
|2 doi
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|a pubmed24n0933.xml
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|a (NLM)29341267
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|a DE-627
|b ger
|c DE-627
|e rakwb
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|a eng
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|a Zhou, Lingyun
|e verfasserin
|4 aut
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|a Cross-Linking of Thiolated Paclitaxel-Oligo(p-phenylene vinylene) Conjugates Aggregates inside Tumor Cells Leads to "Chemical Locks" That Increase Drug Efficacy
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|c 2018
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|a Text
|b txt
|2 rdacontent
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|a ƒaComputermedien
|b c
|2 rdamedia
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|a ƒa Online-Ressource
|b cr
|2 rdacarrier
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|a Date Completed 07.03.2019
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|a Date Revised 30.09.2020
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|a published: Print-Electronic
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|a Citation Status MEDLINE
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|a © 2018 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
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|a How to reduce the resistance of certain tumor cells to paclitaxel (PTX) and related taxoid anticancer drugs is a major challenge for improving cure rates. An oligo(p-phenylenevinylene) unit with thiol groups and a PTX unit (OPV-S-PTX), which enhances drug efficacy and reverses resistance is thus designed. The mechanism involves diffusion of OPV-S-PTX into the cell, where π-π interactions lead to aggregation. Cross-linking of the aggregates via oxidation of thiol groups is favored in tumor cells because of the higher reactive oxygen species (ROS) concentration. Cross-linked aggregates "chemically lock" the multichromophore particle for a more persistent effect. The IC50 of OPV-S-PTX for tumor cell line A549 is reduced down to 0.33 × 10-9 m from that observed for PTX itself (41 × 10-9 m). Enhanced efficacy by OPV-S-PTX is proposed to proceed via acceleration of microtubule bundle formation. A549/T-inoculated xenograft mice experiments reveal suppression of tumor growth upon OPV-S-PTX treatment. Altogether, these results show that the internal cross-linking of OPV-S-PTX through ROS provides a means to discriminate between tumor and healthy cells and the formation of the chemically locked particles enhances drug efficacy and helps in reducing resistance
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|a Journal Article
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|a antitumor
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|a assembly inside cells
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|a chemical locks
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|a drug resistance
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|a supramolecular paclitaxel
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|a Antineoplastic Agents
|2 NLM
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|a Antineoplastic Agents, Phytogenic
|2 NLM
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|a Micelles
|2 NLM
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|a Polyvinyls
|2 NLM
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|a oligo(p-phenylene vinylene)
|2 NLM
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|a Paclitaxel
|2 NLM
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|a P88XT4IS4D
|2 NLM
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|a Lv, Fengting
|e verfasserin
|4 aut
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|a Liu, Libing
|e verfasserin
|4 aut
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|a Shen, Guizhi
|e verfasserin
|4 aut
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|a Yan, Xuehai
|e verfasserin
|4 aut
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|a Bazan, Guillermo C
|e verfasserin
|4 aut
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|a Wang, Shu
|e verfasserin
|4 aut
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|i Enthalten in
|t Advanced materials (Deerfield Beach, Fla.)
|d 1998
|g 30(2018), 10 vom: 17. März
|w (DE-627)NLM098206397
|x 1521-4095
|7 nnns
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|g volume:30
|g year:2018
|g number:10
|g day:17
|g month:03
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|u http://dx.doi.org/10.1002/adma.201704888
|3 Volltext
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