Recent Update on Development of Small-Molecule STAT3 Inhibitors for Cancer Therapy: From Phosphorylation Inhibition to Protein Degradation
文献类型：期刊论文
| 作者 | Dong, Jinyun1,2; Cheng, Xiang-Dong1,2; Zhang, Wei-Dong3; Qin, Jiang-Jiang1,2 |
| 刊名 | JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2021-07-08 |
| 卷号 | 64 |
| ISSN号 | 0022-2623 |
| DOI | 10.1021/acs.jmedchem.1c00629 |
| 通讯作者 | Qin, Jiang-Jiang(jqin@ucas.ac.cn) |
| 英文摘要 | Signal transducer and activator of transcription 3 (STAT3) is a transcription factor that regulates various biological processes, including proliferation, metastasis, angiogenesis, immune response, and chemoresistance. In normal cells, STAT3 is tightly regulated to maintain a transiently active state, while persistent STAT3 activation occurs frequently in cancers, associating with a poor prognosis and tumor progression. Targeting the STAT3 protein is a potentially promising therapeutic strategy for tumors. Although none of the STAT3 inhibitors has been marketed yet, a few of them have succeeded in entering clinical trials. This Review aims to systematically summarize the progress of the last 5 years in the discovery of directive STAT3 small-molecule inhibitors and degraders, focusing primarily on their structural features, design strategies, and bioactivities. We hope this Review will shed light on future drug design and inhibitor optimization to accelerate the discovery process of STAT3 inhibitors or degraders. |
| WOS关键词 | TRANSCRIPTION 3 STAT3 ; DNA-BINDING ACTIVITY ; SIGNAL TRANSDUCER ; INDOLEAMINE 2,3-DIOXYGENASE ; TARGETING STAT3 ; BIOLOGICAL EVALUATION ; TUMOR-GROWTH ; IN-VITRO ; DERIVATIVES ; ACTIVATION |
| 资助项目 | Program of Zhejiang Provincial TCM Sci-tech Plan[2020ZZ005] ; Zhejiang Provincial Natural Science Foundation of China[LQ21B020003] ; Zhejiang Provincial Natural Science Foundation of China[LR21H280001] ; National Natural Science Foundation of China[81903842] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000672729800003 |
| 出版者 | AMER CHEMICAL SOC |
| 资助机构 | Program of Zhejiang Provincial TCM Sci-tech Plan ; Zhejiang Provincial Natural Science Foundation of China ; National Natural Science Foundation of China |
| 源URL | [http://ir.hfcas.ac.cn:8080/handle/334002/123598]  |
| 专题 | 中国科学院合肥物质科学研究院 |
| 通讯作者 | Qin, Jiang-Jiang |
| 作者单位 | 1.Univ Chinese Acad Sci, Canc Hosp, Zhejiang Canc Hosp, Hangzhou 310022, Zhejiang, Peoples R China 2.Chinese Acad Sci, Inst Basic Med & Canc IBMC, Hangzhou 310018, Zhejiang, Peoples R China 3.Naval Med Univ, Sch Pharm, Shanghai 200433, Peoples R China |
| 推荐引用方式 GB/T 7714 | Dong, Jinyun,Cheng, Xiang-Dong,Zhang, Wei-Dong,et al. Recent Update on Development of Small-Molecule STAT3 Inhibitors for Cancer Therapy: From Phosphorylation Inhibition to Protein Degradation[J]. JOURNAL OF MEDICINAL CHEMISTRY,2021,64. |
| APA | Dong, Jinyun,Cheng, Xiang-Dong,Zhang, Wei-Dong,&Qin, Jiang-Jiang.(2021).Recent Update on Development of Small-Molecule STAT3 Inhibitors for Cancer Therapy: From Phosphorylation Inhibition to Protein Degradation.JOURNAL OF MEDICINAL CHEMISTRY,64. |
| MLA | Dong, Jinyun,et al."Recent Update on Development of Small-Molecule STAT3 Inhibitors for Cancer Therapy: From Phosphorylation Inhibition to Protein Degradation".JOURNAL OF MEDICINAL CHEMISTRY 64(2021). |
入库方式： OAI收割
来源：合肥物质科学研究院
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