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本文引用的文献

1
4-Hydroxy--[3,5-bis(trifluoromethyl)phenyl]-1,2,5-thiadiazole-3-carboxamide: a novel inhibitor of the canonical NF-κB cascade.4-羟基-2-[3,5-双（三氟甲基）苯基]-1,2,5-噻二唑-3-甲酰胺：一种经典核因子κB级联反应的新型抑制剂。
Medchemcomm. 2017 Aug 25;8(9):1850-1855. doi: 10.1039/c7md00278e. eCollection 2017 Sep 1.
2
The non-canonical NF-κB pathway in immunity and inflammation.免疫与炎症中的非经典NF-κB信号通路
Nat Rev Immunol. 2017 Sep;17(9):545-558. doi: 10.1038/nri.2017.52. Epub 2017 Jun 5.
3
Design, synthesis, biological evaluation and X-ray structural studies of potent human dihydroorotate dehydrogenase inhibitors based on hydroxylated azole scaffolds.基于羟基化唑类支架的高效人二氢乳清酸脱氢酶抑制剂的设计、合成、生物学评价及X射线结构研究
Eur J Med Chem. 2017 Mar 31;129:287-302. doi: 10.1016/j.ejmech.2017.02.017. Epub 2017 Feb 14.
4
Structure-Based Design of Tricyclic NF-κB Inducing Kinase (NIK) Inhibitors That Have High Selectivity over Phosphoinositide-3-kinase (PI3K).基于结构的三环核因子-κB 诱导激酶（NIK）抑制剂的设计，这些抑制剂对磷酸肌醇 3-激酶（PI3K）具有高选择性。
J Med Chem. 2017 Jan 26;60(2):627-640. doi: 10.1021/acs.jmedchem.6b01363. Epub 2017 Jan 12.
5
NF-kappaΒ-inducing kinase regulates stem cell phenotype in breast cancer.NF-κB 诱导激酶调节乳腺癌中的干细胞表型。
Sci Rep. 2016 Nov 23;6:37340. doi: 10.1038/srep37340.
6
Targeting the NF-κB Pathway as a Combination Therapy for Advanced Thyroid Cancer.靶向核因子κB通路作为晚期甲状腺癌的联合治疗方法
PLoS One. 2015 Aug 11;10(8):e0134901. doi: 10.1371/journal.pone.0134901. eCollection 2015.
7
Refining the chemical toolbox to be fit for educational and practical purpose for drug discovery in the 21st Century.优化化学工具库，使其适用于21世纪药物发现的教育和实际目的。
Drug Discov Today. 2015 Aug;20(8):1018-26. doi: 10.1016/j.drudis.2015.04.010. Epub 2015 May 7.
8
Computational design and discovery of nanomolar inhibitors of IκB kinase β.计算设计和发现 IκB 激酶 β 的纳摩尔抑制剂。
J Am Chem Soc. 2015 Jan 14;137(1):337-48. doi: 10.1021/ja510636t. Epub 2015 Jan 2.
9
Targeting the NFκB signaling pathways for breast cancer prevention and therapy.靶向NFκB信号通路用于乳腺癌的预防和治疗。
Curr Med Chem. 2015;22(2):264-89. doi: 10.2174/0929867321666141106124315.
10
Synthesis, antibacterial activity and cytotoxicity of new fused pyrazolo[1,5-a]pyrimidine and pyrazolo[5,1-c][1,2,4]triazine derivatives from new 5-aminopyrazoles.新型 5-氨基吡唑衍生的吡唑并[1,5-a]嘧啶和吡唑并[5,1-c][1,2,4]三嗪衍生物的合成、抗菌活性和细胞毒性
Eur J Med Chem. 2013 Jun;64:464-76. doi: 10.1016/j.ejmech.2013.04.029. Epub 2013 Apr 23.

-乙酰基-3-氨基吡唑通过选择性抑制NF-κB诱导激酶（NIK）来阻断非经典NF-κB信号级联反应。

-Acetyl-3-aminopyrazoles block the non-canonical NF-kB cascade by selectively inhibiting NIK.

作者信息

Pippione Agnese C, Sainas Stefano, Federico Antonella, Lupino Elisa, Piccinini Marco, Kubbutat Michael, Contreras Jean-Marie, Morice Christophe, Barge Alessandro, Ducime Alex, Boschi Donatella, Al-Karadaghi Salam, Lolli Marco L

机构信息

Department of Science and Drug Technology , University of Torino , via Pietro Giuria 9 , 10125 Torino , Italy . Email:

Department of Oncology , University of Torino , via Michelangelo 27/B , 10126 Torino , Italy.

出版信息

Medchemcomm. 2018 Apr 12;9(6):963-968. doi: 10.1039/c8md00068a. eCollection 2018 Jun 1.

DOI:10.1039/c8md00068a
PMID:30108985
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6071728/
Abstract

NF-κB-inducing kinase (NIK), an oncogenic drug target that is associated with various cancers, is a central signalling component of the non-canonical pathway. A blind screening process, which established that amino pyrazole related scaffolds have an effect on IKKbeta, led to a optimization process that identified the aminopyrazole as a low μM selective NIK inhibitor. Compound effectively inhibited the NIK-dependent activation of the NF-κB pathway in tumour cells, confirming its selective inhibitory profile.

摘要

核因子κB诱导激酶（NIK）是一种与多种癌症相关的致癌药物靶点，是非经典途径的核心信号成分。一项盲筛过程确定了氨基吡唑相关支架对IKKβ有作用，进而引发了优化过程，该过程确定氨基吡唑为低 microM 选择性 NIK 抑制剂。该化合物有效抑制肿瘤细胞中 NF-κB 途径的 NIK 依赖性激活，证实了其选择性抑制特性。