Azide-Masked Resiquimod Activated by Hypoxia for Selective Tumor Therapy

© 2023 Wiley-VCH GmbH.

Bibliographische Detailangaben
Veröffentlicht in:Advanced materials (Deerfield Beach, Fla.). - 1998. - 35(2023), 29 vom: 03. Juli, Seite e2207733
1. Verfasser: Sun, Jiali (VerfasserIn)
Weitere Verfasser: Liu, Zhilin, Yao, Haochen, Zhang, Honglei, Zheng, Mengfei, Shen, Na, Cheng, Jianjun, Tang, Zhaohui, Chen, Xuesi
Format: Online-Aufsatz
Sprache:English
Veröffentlicht: 2023
Zugriff auf das übergeordnete Werk:Advanced materials (Deerfield Beach, Fla.)
Schlagworte:Journal Article azide-masked hypoxia activated resiquimod (R848) selective therapy resiquimod V3DMU7PVXF Azides Imidazoles Prodrugs
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520 |a Resiquimod (R848) is an immunomodulator that causes a severe systemic inflammatory reaction due to low tumor selectivity, thus hindering its use in cancer therapy. Therefore, an azide-masked prodrug (R848-N3 ) of R848 is developed, which is selectively activated to R848 in hypoxic tumors. R848-N3 significantly reduces pro-inflammatory cytokines in treated mice to 1/12 compared to R848 at the same dose. In addition, combretastatin A4 nanoparticles (CA4-NPs) are used to enhance the tumor selectivity of R848-N3 by elevating the level of tumor hypoxia. R848-N3 +CA4-NPs has higher tumor selectivity than the intratumoral injection of R848 at 1 h after administration. The concentration of the active R848 in the tumor is 21.45-fold that in the heart. Benefiting from the high tumor selectivity of R848-N3 , R848-N3 +CA4-NPs+anti-PD1 exerted 94.1% tumor suppression and 40.0% tumor cure. Therefore, this work highlights the potential of azide-masking strategy in the development of tumor-selective prodrugs with reduced toxicity 
650 4 |a Journal Article 
650 4 |a azide-masked 
650 4 |a hypoxia activated 
650 4 |a resiquimod (R848) 
650 4 |a selective therapy 
650 7 |a resiquimod  |2 NLM 
650 7 |a V3DMU7PVXF  |2 NLM 
650 7 |a Azides  |2 NLM 
650 7 |a Imidazoles  |2 NLM 
650 7 |a Prodrugs  |2 NLM 
700 1 |a Liu, Zhilin  |e verfasserin  |4 aut 
700 1 |a Yao, Haochen  |e verfasserin  |4 aut 
700 1 |a Zhang, Honglei  |e verfasserin  |4 aut 
700 1 |a Zheng, Mengfei  |e verfasserin  |4 aut 
700 1 |a Shen, Na  |e verfasserin  |4 aut 
700 1 |a Cheng, Jianjun  |e verfasserin  |4 aut 
700 1 |a Tang, Zhaohui  |e verfasserin  |4 aut 
700 1 |a Chen, Xuesi  |e verfasserin  |4 aut 
773 0 8 |i Enthalten in  |t Advanced materials (Deerfield Beach, Fla.)  |d 1998  |g 35(2023), 29 vom: 03. Juli, Seite e2207733  |w (DE-627)NLM098206397  |x 1521-4095  |7 nnas 
773 1 8 |g volume:35  |g year:2023  |g number:29  |g day:03  |g month:07  |g pages:e2207733 
856 4 0 |u http://dx.doi.org/10.1002/adma.202207733  |3 Volltext 
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