Review of Small Molecule Anticancer NF-κB Inhibitors

S. Kzyrgalin, R. S. Yamidanov, K. A. Nazmieva, S. Gantsev
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Abstract

   Cancer is one of the most common diseases in the world. Th e transcription factor NF-κB plays a key role in various physiological processes including immune response, cell proliferation, cell apoptosis and inflammation. Due to participation of NF-kappa B signaling pathways in carcinogenesis, angiogenesis, and tumor resistance to chemo- and radiotherapy, the factor is considered to be the ideal target for pharmacological treatment of cancer. Th e paper presents a literature review of the RSCI, PubMed, Scopus, Web of Science, Chemical Abstracts NCCN databases and other open access data. The carcinogenesis inhibitors were selected from all NF-κB inhibitors found. Inhibitors with antitumor activity of analytical interest include Bruton tyrosine kinase (BTK) inhibitors, cellular inhibitors of apoptosis proteins (c-IAP), proteasome inhibitors, and one inhibitor of NF-κB translocation to the nucleus. Th e authors analyzed products of diff erent development stages with recorded antitumor activity to varying degrees. NF-κB inhibitors are promising drug candidates, but since NF-κB is involved in most biological processes and the broad spectrum of action can cause side eff ects, the selective action of these compounds is to be explored.
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小分子抗癌NF-κB抑制剂研究进展
癌症是世界上最常见的疾病之一。转录因子NF-κB在免疫应答、细胞增殖、细胞凋亡和炎症等多种生理过程中发挥关键作用。由于NF-kappa B信号通路参与肿瘤发生、血管生成和肿瘤对化疗和放疗的抵抗,该因子被认为是癌症药物治疗的理想靶点。本文对RSCI、PubMed、Scopus、Web of Science、Chemical Abstracts NCCN等开放获取数据库进行了文献综述。从所有发现的NF-κB抑制剂中选择致癌抑制剂。具有抗肿瘤活性的抑制剂包括布鲁顿酪氨酸激酶(BTK)抑制剂、细胞凋亡蛋白抑制剂(c-IAP)、蛋白酶体抑制剂和一种NF-κB易位到细胞核的抑制剂。作者分析了不同发育阶段的产物,记录了不同程度的抗肿瘤活性。NF-κB抑制剂是很有前途的候选药物,但由于NF-κB参与大多数生物过程,并且广谱作用可引起副作用,因此这些化合物的选择性作用有待探索。
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审稿时长
12 weeks
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