期刊
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
卷 60, 期 33, 页码 18280-18288出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.202106195
关键词
modular-agent probes; small molecule scaffolds; spatial arrangements; specificity; toxicity
资金
- National Key R&D Program of China [2020YFA0211200]
- National Natural Science Foundation of China [22090050, 21974128, 21874121, 52003257, 21703210]
- Hubei Provincial Natural Science Foundation of China [2019CFA043, 2020CFA037]
Researchers focused on different spatial arrangements of modular-agent probes and designed two MAPs to compare their specificity and toxicity.
To overcome a series of challenges in tumor therapy, modular-agent probes (MAPs) comprised of various functional modules have been proposed. Researchers have tried to optimize the MAPs by exploiting the new modules or increasing the numbers of module, while neglecting the configuration of various modules. Here, we focus on the different spatial arrangements of existing modules. By utilizing a tetraphenylethylene (TPE) derivative with stereochemical structure and dual modifiable end-group sites as small molecule scaffold, two MAPs with same modular agents (module T for enhancing the internalization of MAPs by tumor cells and module M for causing mitochondrial dysfunction) but different spatial arrangements (on the one side, TM-AIE, and two sides, T-AIE-M, of the molecule scaffold) are designed. T-AIE-M with larger RGD binding angle performed higher specificity, while TM-AIE characterizing longer alpha-helix structure displayed superior toxicity.
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