Home Journals Articles Updates About
CN
image
收藏切换
Legumain-responsive functional gold nanoparticles for drug targeting delivery and treatment of subcutaneous xenograft tumor
收藏切换
PDF
Shao-bo RUAN, Qin HE, Hui-le GAO*
Acta Pharmaceutica Sinica | 2017, 52(11) : 1756 - 1762
Less
收藏切换
Acta Pharmaceutica Sinica | 2017, 52(11): 1756-1762
• ORIGINAL ARTICLES •
Legumain-responsive functional gold nanoparticles for drug targeting delivery and treatment of subcutaneous xenograft tumor
Full
Shao-bo RUAN, Qin HE, Hui-le GAO*
Affiliations
  • Key Laboratory of Drug Targeting and Drug Delivery Systems, West School of Pharmacy, Sichuan University, Chengdu 610041, China
Published: 2017-11-12 doi: 10.16438/j.0513-4870.2017-0847
Outline
收藏切换

Legumain, a kind of asparaginyl endopeptidase, is overexpressed in highly metastatic and highly aggressive tumor, which can undergo an enzymatic hydrolysis of substrates. We proposed a legumain-responsive functional gold nanoparticle (GNP) drug delivery system (GNPs-A & C), which was consist of Ala-Ala-Asn-Cys-Lys (AK) modified GNPs (GNPs-AK) and 2-cyano-6-aminobenzothiazole (CABT) modified GNPs (GNPs-CABT). In the circulation system, the GNPs-A & C could passively target to the tumor site through the enhanced permeability and retention (EPR) effect. Then the overexpressed legumain specifically cleave the peptide to exposure the 1, 2-thiolamino group, which could take place click reaction with the cyano group of CABT, leading to the aggregation of two GNPs, these aggregates of GNPs with increased size were more likely to retain within tumor site. In vivo fluorescent imaging demonstrated GNPs-A & C could acquire an enhanced accumulation in legumain-overexpressed C6 tumor. Importantly, after tethering DOX, the GNPs-DOX-A & C showed an excellent anti-tumor effect with reduced cardiotoxicity.

legumain  /  metal nanoparticle  /  click chemistry  /  aggregation  /  retention
Shao-bo RUAN, Qin HE, Hui-le GAO. Legumain-responsive functional gold nanoparticles for drug targeting delivery and treatment of subcutaneous xenograft tumor[J]. Acta Pharmaceutica Sinica, 2017 , 52 (11) : 1756 -1762 . DOI: 10.16438/j.0513-4870.2017-0847
Appendix
Less
Year 2017 volume 52 Issue 11
PDF
109
41
Cite this Article
BibTeX
Article Info
doi: 10.16438/j.0513-4870.2017-0847
  • Receive Date：2017-08-29
  • Online Date：2026-01-14
  • Published：2017-11-12
Article Data
Affiliations
History
  • Received：2017-08-29
  • Revised：2017-09-07
Funding
Affiliations
    Key Laboratory of Drug Targeting and Drug Delivery Systems, West School of Pharmacy, Sichuan University, Chengdu 610041, China
References
Share
https://castjournals.cast.org.cn/joweb/yxxb/EN/10.16438/j.0513-4870.2017-0847
Share to
QR

Scan QR to access full text

Cite this article
BibTeX
Citations
表12种不同金属材料的力学参数
科
Family		 属数
Number of
genus		 种数
Number of
species		 占总种数比例
Percentage of
total species (%)		 属
Genus		 种数
Number of
species		 占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
关闭全屏
  • BibTeX
  • EndNote
  • RefWorks
  • TxT
Links
Articles
Latest Articles
Most Read
Collections
Updates
Events
News
Multimedia
About
About Us
Contact
No. 86 Xueyuan South Road, Haidian District, Beijing
100081
010-62199257
qkjq@cast.org.cn

Copyright © 2025 China Association for Science and Technology. All rights reserved. For all open access content, the relevant licensing terms apply.
Sponsored by the Office of the Leading Group for Cybersecurity and Informatization of CAST, and supported by Science and Technology Review Publishing House