北京大学医学部机构知识库
Advanced  
IR@PKUHSC  > 北京大学临床肿瘤学院  > 期刊论文
学科主题: 临床医学
题名:
Prodrug AST-003 Improves the Therapeutic Index of the Multi-Targeted Tyrosine Kinase Inhibitor Sunitinib
作者: Huang, Qiang1,2; Zhou, Changhua1,2; Chen, Xiao1; Dong, Bing1,2; Chen, Siqi1,2; Zhang, Ning3; Liu, Yawei4; Li, Anrong5; Yao, Meicun1; Miao, Ji1; Li, Qing1,2; Wang, Zhong1,2
刊名: PLOS ONE
发表日期: 2015-10-29
DOI: 10.1371/journal.pone.0141395
卷: 10, 期:10
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Multidisciplinary Sciences
研究领域[WOS]: Science & Technology - Other Topics
关键词[WOS]: SIGNALING PATHWAYS ; IN-VIVO ; ANGIOGENESIS ; CARCINOMA ; APOPTOSIS ; DESIGN ; CANCER
英文摘要:

Patients have responded well to the multi-targeted tyrosine kinase inhibitor (TKI) Sunitinib in the clinic. But the severe toxic side effects associated with Sunitinib limit its therapeutic index. To improve the therapeutic index of Sunitinib, a prodrug strategy was employed to modify Sunitinib. The inactive prodrug AST-003 can be converted to Sunitinib in vitro and in vivo. Compared with Sunitinib, AST-003 has unique biochemical, cellular and pharmacokinetic properties with improved tolerability in mice and yield higher efficacy in tumor xenograft models. This prodrug strategy may constitute a novel paradigm to improve the therapeutic index of Sunitinib and other TKI or anti-angiogenesis drugs in general.

语种: 英语
所属项目编号: 2011Y038
项目资助者: Introduced Innovative R&amp ; D Team Leadership of Guangdong Province (P.R. China)
WOS记录号: WOS:000363920300035
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/62163
Appears in Collections:北京大学临床肿瘤学院_期刊论文

Files in This Item:

There are no files associated with this item.


作者单位: 1.Sun Yat Sen Univ, Sch Pharmaceut Sci, Guangzhou 510275, Guangdong, Peoples R China
2.Sun Yat Sen Univ, Ctr Cellular & Struct Biol, Guangzhou 510275, Guangdong, Peoples R China
3.Peking Univ, Canc Hosp, Beijing Inst Canc Res, Beijing 100871, Peoples R China
4.Gen Staff Dept PLA, Hlth Div, Guard Bur, Beijing, Peoples R China
5.Ascenta Pharmaceut, Guangzhou, Guangdong, Peoples R China

Recommended Citation:
Huang, Qiang,Zhou, Changhua,Chen, Xiao,et al. Prodrug AST-003 Improves the Therapeutic Index of the Multi-Targeted Tyrosine Kinase Inhibitor Sunitinib[J]. PLOS ONE,2015,10(10).
Service
Recommend this item
Sava as my favorate item
Show this item's statistics
Export Endnote File
Google Scholar
Similar articles in Google Scholar
[Huang, Qiang]'s Articles
[Zhou, Changhua]'s Articles
[Chen, Xiao]'s Articles
CSDL cross search
Similar articles in CSDL Cross Search
[Huang, Qiang]‘s Articles
[Zhou, Changhua]‘s Articles
[Chen, Xiao]‘s Articles
Related Copyright Policies
Null
Social Bookmarking
Add to CiteULike Add to Connotea Add to Del.icio.us Add to Digg Add to Reddit
所有评论 (0)
暂无评论
 
评注功能仅针对注册用户开放,请您登录
您对该条目有什么异议,请填写以下表单,管理员会尽快联系您。
内 容:
Email:  *
单位:
验证码:   刷新
您在IR的使用过程中有什么好的想法或者建议可以反馈给我们。
标 题:
 *
内 容:
Email:  *
验证码:   刷新

Items in IR are protected by copyright, with all rights reserved, unless otherwise indicated.

 

 

Valid XHTML 1.0!
Copyright © 2007-2017  北京大学医学部 - Feedback
Powered by CSpace