dc.contributor.author | Song, Songlin | |
dc.contributor.author | Gui, Lin | |
dc.contributor.author | Feng, Qiqi | |
dc.contributor.author | Taledaohan, Ayijiang | |
dc.contributor.author | Li, Yuanming | |
dc.contributor.author | Wang, Wei | |
dc.contributor.author | Wang, Yanming | |
dc.contributor.author | Wang, Yuji | |
dc.date.accessioned | 2021-03-25T08:24:20Z | |
dc.date.available | 2021-03-25T08:24:20Z | |
dc.date.created | 2020-09-10T10:59:08Z | |
dc.date.issued | 2020 | |
dc.Published | International Journal of Nanomedicine. 2020, 15 6659-6671. | |
dc.identifier.issn | 1176-9114 | |
dc.identifier.uri | https://hdl.handle.net/11250/2735403 | |
dc.description.abstract | Purpose: Histone citrullination by peptidylarginine deiminases 4 (PAD4) regulates the gene expression of tumor suppressor. In our previously study, YW3-56 (356) was developed as a potent PAD4 inhibitor for cancer therapy with novel function in the autophagy pathway. To enhance the antitumor activity, the PAD4 inhibitor 356 was modified by the well-established cationic penetrating peptide RKKRRQRRR (peptide TAT) and gold nanoparticles to obtain 356-TAT-AuNPs which could enhance the permeability of chemical drug in solid tumor.
Methods: 356-TAT-AuNPs were prepared, and their morphology were characterized. The antitumor activity of 356-TAT-AuNPs was evaluated in vitro and in vivo.
Results: 356-TAT-AuNPs exhibited higher anticancer activity against HCT-116, MCF-7 and A549 cells than 356 and 356-AuNPs. Compared with 356 and 356-AuNPs, 356-TAT-AuNPs entered the cytoplasm and nuclear, exhibited stronger anticancer activity by increasing apoptosis, inducing autophagy and inhibiting of histone H3 citrullination, and in HCT-116 xenograft mouse model, 356-TAT-AuNPs could improve the antitumor activity.
Conclusion: The modified AuNPs with peptide TAT as drug delivery system are potent in delaying tumor growth and could be a powerful vehicle for profitable anticancer drug development. We believe that peptide TAT modification strategy may provide a simple and valuable method for improving antitumor activity of PAD4 inhibitors for clinical use. | en_US |
dc.language.iso | eng | en_US |
dc.publisher | Dove Medical Press | en_US |
dc.rights | Navngivelse-Ikkekommersiell 4.0 Internasjonal | * |
dc.rights.uri | http://creativecommons.org/licenses/by-nc/4.0/deed.no | * |
dc.title | TAT-Modified Gold Nanoparticles Enhance the Antitumor Activity of PAD4 Inhibitors | en_US |
dc.type | Journal article | en_US |
dc.type | Peer reviewed | en_US |
dc.description.version | publishedVersion | en_US |
dc.rights.holder | Copyright 2020 Song et al. | en_US |
cristin.ispublished | true | |
cristin.fulltext | original | |
cristin.qualitycode | 1 | |
dc.identifier.doi | 10.2147/IJN.S255546 | |
dc.identifier.cristin | 1828659 | |
dc.source.journal | International Journal of Nanomedicine | en_US |
dc.source.40 | 15 | |
dc.source.pagenumber | 6659–6671 | en_US |
dc.identifier.citation | International Journal of Nanomedicine. 2020, 15, 6659–6671. | en_US |
dc.source.volume | 15 | en_US |