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学科主题: 药学
题名:
In vitro selection of G-rich RNA aptamers that target HIV-1 integrase
作者: Liu YingChun; Zhang Yan; Ye GuoZhu; Yang ZhenJun; Zhang LiangRen; Zhang LiHe
关键词: RNA aptamer ; HIV-1 integrase ; G-quadruplex
刊名: SCIENCE IN CHINA SERIES B-CHEMISTRY
发表日期: 2008-05-01
DOI: 10.1007/s11426-008-0056-x
卷: 51, 期:5, 页:401-413
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Chemistry, Multidisciplinary
研究领域[WOS]: Chemistry
关键词[WOS]: NUCLEIC-ACID APTAMERS ; TETRAD-FORMING OLIGONUCLEOTIDES ; G-QUARTET OLIGONUCLEOTIDES ; VIRUS TYPE-1 INTEGRASE ; DRUG DESIGN ; INHIBITORS ; DNA ; THERAPEUTICS ; LIGANDS ; BINDING
英文摘要:

Aptamers that interact with various HIV-1 proteins, such as reverse transcriptase, Rev, Tat protein, and nuclear capsule protein, have been prepared through SELEX (systematic evolution of ligands by exponential enrichment) technique. However, there are few reports about the DNA or RNA aptamers that target HIV-1 integrase. In this investigation, we selected alternative RNA aptamers specific for the HIV-1 integrase by using a different binding buffer containing 10 mmol center dot L(-1) MgCl(2) and 100 mmol center dot L(-1) KCI. Aptamer IN1, IN2, IN3 had similar and the highest Kd values from 145 to 239 nmol center dot L(-1). Structural studies showed that they formed similar stem-loop structure. Deletion of any stem structure resulted in diminished affinity. In addition, structure probing study with antisense DNA indicated that the stem-loop structure in the random region was critical for integrase binding. Although aptamer IN1 failed to form G-quartet structure, it might directly interact with the DDE motif of integrase, which is the virus DNA-binding site, because G-quadruplex T40214 competitively inhibited the interaction between IN1 and integrase. Together, this study generated a novel RNA aptamer IN1, which could be useful in basic research and anti-HIV drug screening.

语种: 英语
WOS记录号: WOS:000255985300002
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/66727
Appears in Collections:北京大学药学院_期刊论文

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作者单位: Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100083, Peoples R China

Recommended Citation:
Liu YingChun,Zhang Yan,Ye GuoZhu,et al. In vitro selection of G-rich RNA aptamers that target HIV-1 integrase[J]. SCIENCE IN CHINA SERIES B-CHEMISTRY,2008,51(5):401-413.
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