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学科主题: 药学
题名:
Design, synthesis and biological evaluation of indolizine derivatives as HIV-1 VIF-ElonginC interaction inhibitors
作者: Jin, Hongwei1; Huang, Wenlin1; Zuo, Tao2; Liu, Zhenming1; Yang, Zhenjun1; Yu, Xianghui2,3; Zhang, Liangren1; Zhang, Lihe1
关键词: VIF-ElonginC interaction inhibition ; VEC-5 ; Anti-HIV-1 ; Indolizine derivatives ; Structure-activity relationship
刊名: MOLECULAR DIVERSITY
发表日期: 2013-05-01
DOI: 10.1007/s11030-013-9424-3
卷: 17, 期:2, 页:221-243
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Biochemistry & Molecular Biology ; Chemistry, Applied ; Chemistry, Medicinal ; Chemistry, Multidisciplinary
研究领域[WOS]: Biochemistry & Molecular Biology ; Chemistry ; Pharmacology & Pharmacy
关键词[WOS]: ANTIRETROVIRAL DRUG-RESISTANCE ; SMALL-MOLECULE INHIBITION ; E3 UBIQUITIN LIGASE ; UNITED-STATES ; THERAPY ; REPLICATION ; PREVALENCE ; PROTEIN ; DNA
英文摘要:

The HIV-1 viral infectivity factor (VIF) protein is essential for viral replication. VIF recruits cellular ElonginB/C-Cullin5 E3 ubiquitin ligase to target the host antiviral protein APOBEC3G (A3G) for proteasomal degradation. Thus, the A3G-Vif-E3 complex represents an attractive target for the development of novel anti-HIV drugs. In this study, we describe the design and synthesis of indolizine derivatives as VIF inhibitors targeting the VIF-ElonginC interaction. Many of the synthesized compounds exhibited obvious inhibition activities of VIF-mediated A3G degradation, and 5 compounds showed improvement of activity compared to the known VIF inhibitor VEC-5 (1) with IC values about 20 M. The findings described here will be useful for the development of more potent VIF inhibitors.

语种: 英语
所属项目编号: 20972009
项目资助者: National Natural Science Foundation of China
WOS记录号: WOS:000318184500002
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/49938
Appears in Collections:北京大学药学院_期刊论文

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作者单位: 1.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
2.Jilin Univ, Coll Life Sci, Natl Engn Lab AIDS Vaccine, Changchun 130012, Peoples R China
3.Jilin Univ, Coll Life Sci, Minist Educ, Key Lab Mol Enzymol & Engn, Changchun 130012, Peoples R China

Recommended Citation:
Jin, Hongwei,Huang, Wenlin,Zuo, Tao,et al. Design, synthesis and biological evaluation of indolizine derivatives as HIV-1 VIF-ElonginC interaction inhibitors[J]. MOLECULAR DIVERSITY,2013,17(2):221-243.
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