anewclassofhiv1inhibitorsandthetargetidentificationviaproteomicprofiling
文献类型：期刊论文
| 作者 | Ge Yingzi1; Zhou Bin1; Xiao Ruoxuan1; Yuan Xiaojing1; Zhou Hu1 ; Xu Yechun1; Wainberg Mark A2; Han Yingshan2; Yue Jianmin1
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| 刊名 | sciencechinachemistry
 |
| 出版日期 | 2018 |
| 卷号 | 061期号:011页码:1430 |
| 关键词 | HIV-1 鉴定 化学结构 相互作用 类固醇 有势力 化合物 氢氧根 |
| ISSN号 | 1674-7291 |
| 英文摘要 | Anti-HIV screening with the MT-4/MTT assay on a focused library of structurally diverse natural products has led to the discovery of a group of steroids with potent activities, which include four new ergostane-type steroids, named amotsterols A-D （1-4）, together with two known analogs. Among them, the most potent amotsterol D （4） exhibited anti-HIV activity against wild- type and some clinically relevant multidrug resistant HIV-I strains. Subsequent studies on its target identification through a proteomic approach found that compound 4 might target PKM2, a rate limiting enzyme ofglycolysis, in host cells to restrict HIV replication. The docking model of compound 4 to PKM2 showed that the two hydroxyl groups of 4 form hydrogen bonds with the two parallel Y390 in each subunit of PKM2 separately, and the ring C of 4 is sandwiched between the two parallel aromatic rings ofF26. The identified hit compound may have the potential to be further developed as a novel anti-HIVagent. These results demonstrated that an integrated approach, which combines new chemical structures and phenotypic screening with a proteomic approach, could not only identify novel HIV-1 inhibitors, but also elucidate the unknown targets of compound interactions in antiviral drug discovery. |
| 语种 | 英语 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/286309]  |
| 专题 | 中国科学院上海药物研究所 |
| 作者单位 | 1.中国科学院上海药物研究所 2.麦吉尔大学 |
| 推荐引用方式 GB/T 7714 | Ge Yingzi,Zhou Bin,Xiao Ruoxuan,et al. anewclassofhiv1inhibitorsandthetargetidentificationviaproteomicprofiling[J]. sciencechinachemistry,2018,061(011):1430. |
| APA | Ge Yingzi.,Zhou Bin.,Xiao Ruoxuan.,Yuan Xiaojing.,Zhou Hu.,...&Yue Jianmin.(2018).anewclassofhiv1inhibitorsandthetargetidentificationviaproteomicprofiling.sciencechinachemistry,061(011),1430. |
| MLA | Ge Yingzi,et al."anewclassofhiv1inhibitorsandthetargetidentificationviaproteomicprofiling".sciencechinachemistry 061.011(2018):1430. |
入库方式： OAI收割
来源：上海药物研究所
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