FS23 binds to the N-terminal domain of human Hsp90: A novel small inhibitor for Hsp90
文献类型：期刊论文
| 作者 | Li Jian1,2; Shi Feng3; Chen Dan-Qi3 ; Cao Hui-Ling2; Xiong Bing3; Shen Jing-Kang3; He Jian-Hua1
|
| 刊名 | NUCLEAR SCIENCE AND TECHNIQUES
 |
| 出版日期 | 2015-12 |
| 卷号 | 26期号:6 |
| 关键词 | Heat shock protein 90 N-terminal domain Inhibitor X-ray diffraction Interactions |
| ISSN号 | 1001-8042 |
| 文献子类 | Article |
| 英文摘要 | The N-terminal domain of heat shock protein 90 (Hsp90(N)) is responsible for the catalytic activity of Hsp90. The reported inhibitors of Hsp90 bind to this domain and would inhibit tumor growth and progression. Here, we synthesized FS23, a small molecule inhibitor of hsp90 and collected X-ray diffraction data of the complex crystal of Hsp90-FS23. High resolution X-ray crystallography shows that FS23 interacted with Hsp90(N) at the nucleotide binding cleft, and this suggests that FS23 may complete with nucleotides to bind to Hsp90(N). The crystal structure and the interaction between Hsp90(N) and FS23 suggest a rational basis for the design of novel antitumor drugs. |
| WOS关键词 | ESCHERICHIA-COLI HSP90 ; MOLECULAR CHAPERONE ; CRYSTAL-STRUCTURE ; ANTITUMOR AGENT ; DRUG DISCOVERY ; CANCER-CELLS ; GELDANAMYCIN ; PROTEIN ; IDENTIFICATION ; MACHINERY |
| 资助项目 | National Natural Science Foundation of China[81402850] ; Natural Science Basic Research Plan in Shaanxi Province of China[2015JM3114] ; Introduced talents Foundation of Xi'an Medical University[2015 RCYJ01] ; Doctorate Foundation of Xi'an Medical University[2015 DOC23] |
| WOS研究方向 | Nuclear Science & Technology ; Physics |
| 语种 | 英语 |
| WOS记录号 | WOS:000368964600019 |
| 出版者 | ELSEVIER SCIENCE BV |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276294]  |
| 专题 | 药物化学研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 |
| 通讯作者 | Li Jian |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Appl Phys, Shanghai 201204, Peoples R China; 2.Xian Med Univ, Inst Basic & Translat Med, Shanxi Key Lab Ischem Cardiovasc Dis, Xian 710021, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Dept Med Chem, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Li Jian,Shi Feng,Chen Dan-Qi,et al. FS23 binds to the N-terminal domain of human Hsp90: A novel small inhibitor for Hsp90[J]. NUCLEAR SCIENCE AND TECHNIQUES,2015,26(6). |
| APA | Li Jian.,Shi Feng.,Chen Dan-Qi.,Cao Hui-Ling.,Xiong Bing.,...&He Jian-Hua.(2015).FS23 binds to the N-terminal domain of human Hsp90: A novel small inhibitor for Hsp90.NUCLEAR SCIENCE AND TECHNIQUES,26(6). |
| MLA | Li Jian,et al."FS23 binds to the N-terminal domain of human Hsp90: A novel small inhibitor for Hsp90".NUCLEAR SCIENCE AND TECHNIQUES 26.6(2015). |
入库方式： OAI收割
来源：上海药物研究所
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