The design of a novel near-infrared fluorescent HDAC inhibitor and image of tumor cells
文献类型：期刊论文
| 作者 | Huang, Ying1; Ru, Hong-bo2; Bao, Bin1; Yu, Jia-hui1; Li, Jia2 ; Zang, Yi2; Lu, Wei1
|
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2020-09-01 |
| 卷号 | 28期号:17页码:5 |
| 关键词 | HDAC Probe NIR Tumor imaging |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2020.115639 |
| 通讯作者 | Zang, Yi(yzang@simm.ac.cn) ; Lu, Wei(wlu@chem.ecnu.edu.cn) |
| 英文摘要 | Histone deacetylases (HDACs) have been found to be biomarkers of cancers and the corresponding inhibitors have attracted much attention these years. Herein we reported a near-infrared fluorescent HDAC inhibitor based on vorinostat (SAHA) and a NIR fluorophore. This newly designed inhibitor showed similar inhibitory activity to SAHA against three HDAC isoforms (HDAC1, 3, 6). The western blot assay showed significant difference in compared with the negative group. When used as probe for further kinematic imaging, Probe 1 showed enhanced retention in tumor cells and the potential of HDAC inhibitors in drug delivery was firstly brought out. The cytotoxicity assay showed Probe 1 had some anti-proliferation activities with corresponding IC50 values of 9.20 +/- 0.96 mu M on Hela cells and 5.91 +/- 0.57 mu M on MDA-MB-231 cells. These results indicated that Probe 1 could be used as a potential NIR fluorescent in the study of HDAC inhibitors and lead compound for the development of visible drugs. |
| WOS关键词 | SELECTIVE DETECTION ; LIVING CELLS ; NAKED-EYE ; IN-VITRO ; PROBE ; DERIVATIVES ; EXPRESSION ; DISCOVERY ; CYSTEINE |
| 资助项目 | China Postdoctoral Science Foundation[2019M651435] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000557982900001 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/292355]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Zang, Yi; Lu, Wei |
| 作者单位 | 1.East China Normal Univ, Shanghai Engn Res Ctr Mol Therapeut & New Drug De, Sch Chem & Mol Engn, 3663 North Zhongshan Rd, Shanghai 200062, Peoples R China 2.Chinese Acad Sci, Natl Ctr Drug Screening, Shanghai Inst Mat Med, State Key Lab Drug Res, 189 Guo Shoujing Rd, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Huang, Ying,Ru, Hong-bo,Bao, Bin,et al. The design of a novel near-infrared fluorescent HDAC inhibitor and image of tumor cells[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2020,28(17):5. |
| APA | Huang, Ying.,Ru, Hong-bo.,Bao, Bin.,Yu, Jia-hui.,Li, Jia.,...&Lu, Wei.(2020).The design of a novel near-infrared fluorescent HDAC inhibitor and image of tumor cells.BIOORGANIC & MEDICINAL CHEMISTRY,28(17),5. |
| MLA | Huang, Ying,et al."The design of a novel near-infrared fluorescent HDAC inhibitor and image of tumor cells".BIOORGANIC & MEDICINAL CHEMISTRY 28.17(2020):5. |
入库方式： OAI收割
来源：上海药物研究所
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