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A BRD4 PROTAC nanodrug for glioma therapy
- Source :
- Acta pharmaceutica Sinica. B. 12(6)
- Publication Year :
- 2021
-
Abstract
- Glioma is a primary aggressive brain tumor with high recurrence rate. The poor efficiency of chemotherapeutic drugs crossing the blood‒brain barrier (BBB) is well-known as one of the main challenges for anti-glioma therapy. Moreover, massive infiltrated tumor-associated macrophages (TAMs) in glioma further thwart the drug efficacy. Herein, a therapeutic nanosystem (SPP-ARV-825) is constructed by incorporating the BRD4-degrading proteolytic targeting chimera (PROTAC) ARV-825 into the complex micelle (SPP) composed of substance P (SP) peptide-modified poly(ethylene glycol)-poly(d,l-lactic acid)(SP-PEG-PDLLA) and methoxy poly(ethylene glycol)-poly(d,l-lactic acid) (mPEG-PDLLA, PP), which could penetrate BBB and target brain tumor. Subsequently, released drug engenders antitumor effect
Details
- ISSN :
- 22113835
- Volume :
- 12
- Issue :
- 6
- Database :
- OpenAIRE
- Journal :
- Acta pharmaceutica Sinica. B
- Accession number :
- edsair.pmid..........836c7dd29dd935c1ee97979f2ea9c529