A 2-Hydroxyisoquinoline-1,3-Dione Active-Site RNase H Inhibitor Binds in Multiple Modes to HIV-1 Reverse Transcriptase
文献类型：期刊论文
| 作者 | Kirby, Karen A.5,6; Myshakina, Nataliya A.9,10; Christen, Martin T.3,8; Chen, Yue-Lei2,7 ; Schmidt, Hilary A.1,6; Huber, Andrew D.6,11; Xi, Zhaoyong8; Kim, Seongmi6,11; Rao, Rohit K.5,6; Kramer, Skyler T.4,6
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| 刊名 | ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
 |
| 出版日期 | 2017-10 |
| 卷号 | 61期号:10 |
| 关键词 | RNase H human immunodeficiency virus inhibitor reverse transcriptase |
| ISSN号 | 0066-4804 |
| DOI | 10.1128/AAC.01351-17 |
| 文献子类 | Article |
| 英文摘要 | The RNase H (RNH) function of HIV -1 reverse transcriptase (RT) plays an essential part in the viral life cycle. We report the characterization of YLC2-155, a 2-hydroxyisoquinoline-1,3-dione (HID) -based active -site RNH inhibitor. YLC2-155 inhibits both polymerase (50% inhibitory concentration [IC50] 2.6 mu M) and RNH functions (IC50 = 0.65 mu M) of RT but is more effective against RNH. X-ray crystallography, nuclear magnetic resonance (NMR) analysis, and molecular modeling were used to show that YLC2-155 binds at the RNH-active site in multiple conformations. |
| WOS关键词 | RIBONUCLEASE-H ; BIOLOGICAL EVALUATIONS ; DIKETO ACID ; DESIGN ; VIRUS ; SOFTWARE ; 3-HYDROXYPYRIMIDINE-2,4-DIONES ; POTENT |
| 资助项目 | National Institutes of Health[AI100890] ; National Institutes of Health[GM105401] ; U.S. Department of Energy[DE-AC02-05CH11231] |
| WOS研究方向 | Microbiology ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000411481800057 |
| 出版者 | AMER SOC MICROBIOLOGY |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/272472]  |
| 专题 | 药物化学研究室 |
| 通讯作者 | Kirby, Karen A.; Sarafianos, Stefan G. |
| 作者单位 | 1.Univ Missouri, Dept Biol Engn, Columbia, MO USA; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai, Peoples R China 3.Swiss Natl Sci Fdn, Bern, Switzerland; 4.Univ Missouri, Dept Biochem, Columbia, MO 65211 USA; 5.Univ Missouri, Sch Med, Dept Mol Microbiol & Immunol, Columbia, MO 65212 USA; 6.Univ Missouri, Christopher S Bond Life Sci Ctr, Columbia, MO 65211 USA; 7.Univ Minnesota, Acad Hlth Ctr, Ctr Drug Design, Minneapolis, MN USA; 8.Univ Pittsburgh, Sch Med, Dept Biol Struct, Pittsburgh, PA USA; 9.Chatham Univ, Dept Nat Sci, Pittsburgh, PA USA; 10.Univ Pittsburgh, Sch Med, Dept Microbiol & Mol Genet, Pittsburgh, PA USA; |
| 推荐引用方式 GB/T 7714 | Kirby, Karen A.,Myshakina, Nataliya A.,Christen, Martin T.,et al. A 2-Hydroxyisoquinoline-1,3-Dione Active-Site RNase H Inhibitor Binds in Multiple Modes to HIV-1 Reverse Transcriptase[J]. ANTIMICROBIAL AGENTS AND CHEMOTHERAPY,2017,61(10). |
| APA | Kirby, Karen A..,Myshakina, Nataliya A..,Christen, Martin T..,Chen, Yue-Lei.,Schmidt, Hilary A..,...&Sarafianos, Stefan G..(2017).A 2-Hydroxyisoquinoline-1,3-Dione Active-Site RNase H Inhibitor Binds in Multiple Modes to HIV-1 Reverse Transcriptase.ANTIMICROBIAL AGENTS AND CHEMOTHERAPY,61(10). |
| MLA | Kirby, Karen A.,et al."A 2-Hydroxyisoquinoline-1,3-Dione Active-Site RNase H Inhibitor Binds in Multiple Modes to HIV-1 Reverse Transcriptase".ANTIMICROBIAL AGENTS AND CHEMOTHERAPY 61.10(2017). |
入库方式： OAI收割
来源：上海药物研究所
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