High-throughput screening campaigns against a PI3Kα isoform bearing the H1047R mutation identified potential inhibitors with novel scaffolds
文献类型：期刊论文
| 作者 | Jia Wang4 ; Grace Qun Gong4; Yan Zhou4; WooJeong Lee4; Christina Maree Buchanan4; William Alexander Denny4; Gordon William Rewcastle4; Jackie Diane Kendall4; James Michael Jeremy Dickson4; Jack Urquhart Flanagan4
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| 刊名 | 中国药理学报：英文版
 |
| 出版日期 | 2018 |
| 卷号 | 39.0期号:011页码:1816 |
| 关键词 | 脚手架 屏蔽 识别 产量 运动 类脂化合物 混合物 新陈代谢 |
| ISSN号 | 1671-4083 |
| 英文摘要 | The phosphatidylinositol 3-kinase （PI3K） pathway is involved in many cellular functions including cell growth, metabolism, and transformation. Hyperactivation of this pathway contributes to tumorigenesis, therefore, PI3K is a major target for anticancer drug discover. Since the PI3Ka isoform is implicated mostly in cancer, we conducted a high-throughput screening （HTS） campaign using a 3-step PI3K homogenous time-resolved fluorescence assay against this isoform bearing the H1047R mutation. A total of 288,000 synthetic and natural product-derived compounds were screened and of which, we identified 124 initial hits that were further selected by considering the predicted binding mode, relationship to known pan-assay interference compounds and previous descriptions as a lipid kinase inhibitor. A total of 24 compounds were then tested for concentration-dependent responses. These hit compounds provide novel scaffolds that can potentially be optimized to create novel PI3K inhibitors. |
| 语种 | 英语 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/294527]  |
| 专题 | 中国科学院上海药物研究所 |
| 作者单位 | 1.Auckland Cancer Society Research Centre 2.The Maurice Wilkins Centre 3.奥克兰大学 4.中国科学院上海药物研究所 |
| 推荐引用方式 GB/T 7714 | Jia Wang,Grace Qun Gong,Yan Zhou,et al. High-throughput screening campaigns against a PI3Kα isoform bearing the H1047R mutation identified potential inhibitors with novel scaffolds[J]. 中国药理学报：英文版,2018,39.0(011):1816. |
| APA | Jia Wang.,Grace Qun Gong.,Yan Zhou.,WooJeong Lee.,Christina Maree Buchanan.,...&MingWei Wang.(2018).High-throughput screening campaigns against a PI3Kα isoform bearing the H1047R mutation identified potential inhibitors with novel scaffolds.中国药理学报：英文版,39.0(011),1816. |
| MLA | Jia Wang,et al."High-throughput screening campaigns against a PI3Kα isoform bearing the H1047R mutation identified potential inhibitors with novel scaffolds".中国药理学报：英文版 39.0.011(2018):1816. |
入库方式： OAI收割
来源：上海药物研究所
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