Pharmacological inhibition of NF-kappa B-inducing kinase (NIK) with small molecules for the treatment of human diseases
文献类型：期刊论文
| 作者 | Cheng, Jing1,2; Feng, Xuexin1,3; Li, Zhiqiang1,2; Zhou, Feilong1; Yang, Jin-Ming3; Zhao, Yujun1,2,4
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| 刊名 | RSC MEDICINAL CHEMISTRY
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| 出版日期 | 2021-04-01 |
| 卷号 | 12期号:4页码:552-565 |
| DOI | 10.1039/d0md00361a |
| 通讯作者 | Zhao, Yujun(yjzhao@simm.ac.cn) |
| 英文摘要 | NIK is a key kinase required for the activation of alternative NF-kappa B signaling pathways. Overactivation of NIK in patients has been observed and is implicated in the pathogenesis of inflammatory diseases, B-cell malignances, and solid tumors. Over the past decade, inhibition of NIK overactivation with small molecules has been pursued as an attractive strategy for drug discovery, where numerous potent and selective NIK inhibitors with novel pharmacophores have been identified. This review summarizes the structural features and key efficacy studies of the NIK inhibitors reported, which justify the mechanism of action of such inhibitors in animal models driven by NIK overactivation. Given the strong pathological associations between overactivation of NIK and human diseases, human clinical trials of NIK inhibitors as drug candidates are eagerly awaited. Information showcased in this review article might be helpful for the discovery and clinical development of the next generation of NIK inhibitors in the near future. |
| WOS关键词 | STRUCTURAL BASIS ; BONE-RESORPTION ; TNF FAMILY ; IKK-ALPHA ; ACTIVATION ; TRAF3 ; INFLAMMATION ; DISCOVERY ; PATHWAY ; LIVER |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| 出版者 | ROYAL SOC CHEMISTRY |
| WOS记录号 | WOS:000644972200005 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/297376]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Zhao, Yujun |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China 2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 3.Yancheng Teachers Univ, Sch Pharm, Yancheng 224051, Jiangsu, Peoples R China 4.Zhengzhou Univ, Sch Pharmaceut Sci, Zhengzhou 450001, Peoples R China |
| 推荐引用方式 GB/T 7714 | Cheng, Jing,Feng, Xuexin,Li, Zhiqiang,et al. Pharmacological inhibition of NF-kappa B-inducing kinase (NIK) with small molecules for the treatment of human diseases[J]. RSC MEDICINAL CHEMISTRY,2021,12(4):552-565. |
| APA | Cheng, Jing,Feng, Xuexin,Li, Zhiqiang,Zhou, Feilong,Yang, Jin-Ming,&Zhao, Yujun.(2021).Pharmacological inhibition of NF-kappa B-inducing kinase (NIK) with small molecules for the treatment of human diseases.RSC MEDICINAL CHEMISTRY,12(4),552-565. |
| MLA | Cheng, Jing,et al."Pharmacological inhibition of NF-kappa B-inducing kinase (NIK) with small molecules for the treatment of human diseases".RSC MEDICINAL CHEMISTRY 12.4(2021):552-565. |
入库方式： OAI收割
来源：上海药物研究所
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