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Design, synthesis and biological evaluation of indolizine derivatives as HIV-1 VIF-ElonginC interaction inhibitors
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
2013-05-01
DOI10.1007/s11030-013-9424-3
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
WOS记录号WOS:000318184500002
引用统计
被引频次:21[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/49938
专题北京大学药学院
北京大学药学院_天然药物与仿生药物国家重点实验室
北京大学药学院_药物化学系
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
推荐引用方式
GB/T 7714
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.
APA Jin, Hongwei.,Huang, Wenlin.,Zuo, Tao.,Liu, Zhenming.,Yang, Zhenjun.,...&Zhang, Lihe.(2013).Design, synthesis and biological evaluation of indolizine derivatives as HIV-1 VIF-ElonginC interaction inhibitors.MOLECULAR DIVERSITY,17(2),221-243.
MLA Jin, Hongwei,et al."Design, synthesis and biological evaluation of indolizine derivatives as HIV-1 VIF-ElonginC interaction inhibitors".MOLECULAR DIVERSITY 17.2(2013):221-243.
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