Arepalli Sateesh Kumar, Choi Minho, Jung Jae-Kyung, Lee Heesoon
Chungbuk National University, College of Pharmacy , Cheongju 362-763 , Republic of Korea +82 43 261 2811 ;
Expert Opin Ther Pat. 2015 Mar;25(3):319-34. doi: 10.1517/13543776.2014.998199. Epub 2015 Jan 2.
The NF-κB family of transcription factors has a vital role in coordinating the expression of a wide variety of genes that control immune responses. The dysfunction of NF-κB has been associated with diseases ranging from inflammation to cancer.
In this review, authors provided information on the role of NF-κB in human health and on recently developed inhibitors from patents granted in 2011 - 2014. The reader will gain an understanding of the mechanisms of NF-κB function as well as the structures and biological activities of recently developed NF-κB inhibitors.
Constitutive NF-κB activation is likely involved in the pathogenesis of several diseases. Researchers need to consider the specific mechanism of each invented NF-κB inhibitor, as well as the properties of the cellular, in vitro and in vivo assays and targeted diseases. For new drug development, they need various biological tests to assess the potential side effects and optimization of the biological activity.
转录因子NF-κB家族在协调控制免疫反应的多种基因的表达中起着至关重要的作用。NF-κB功能障碍与从炎症到癌症等一系列疾病相关。
在本综述中,作者提供了关于NF-κB在人类健康中的作用以及2011年至2014年授予专利的最近开发的抑制剂的信息。读者将了解NF-κB功能的机制以及最近开发的NF-κB抑制剂的结构和生物活性。
NF-κB的组成性激活可能参与多种疾病的发病机制。研究人员需要考虑每种发明的NF-κB抑制剂的具体机制,以及细胞、体外和体内试验的特性和靶向疾病。对于新药开发,他们需要各种生物学测试来评估潜在的副作用并优化生物活性。