Tumor-Triggered Disassembly of a Multiple-Agent-Therapy Probe for Efficient Cellular Internalization.
Angew Chem Int Ed Engl
; 59(46): 20405-20410, 2020 11 09.
Article
em En
| MEDLINE
| ID: mdl-32720727
ABSTRACT
Integration of multiple agent therapy (MAT) into one probe is promising for improving therapeutic efficiency for cancer treatment. However, MAT probe, if entering the cell as a whole, may not be optimal for each therapeutic agent (with different physicochemical properties), to achieve their best performance, hindering strategy optimization. A peptide-conjugated-AIEgen (FC-PyTPA) is presented upon loading with siRNA, it self-assembles into FCsiRNA -PyTPA. When approaching the region near tumor cells, FCsiRNA -PyTPA responds to extracellular MMP-2 and is cleaved into FCsiRNA and PyTPA. The former enters cells mainly by macropinocytosis and the latter is internalized into cells mainly through caveolae-mediated endocytosis. This two-part strategy greatly improves the internalization efficiency of each individual therapeutic agent. Inside the cell, self-assembly of nanofiber precursor F, gene interference of CsiRNA , and ROS production of PyTPA are activated to inhibit tumor growth.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Sondas Moleculares
/
Endocitose
/
Neoplasias
/
Antineoplásicos
Limite:
Humans
Idioma:
En
Revista:
Angew Chem Int Ed Engl
Ano de publicação:
2020
Tipo de documento:
Article
País de afiliação:
China