Double-Edged Swords as Cancer Therapeutics: Novel, Orally Active, Small Molecules Simultaneously Inhibit p53–MDM2 Interaction and the NF-κB Pathway

…, Z Miao, Y Wu, Z Guo, J Li, J Yao, C Xing…

Index: Zhuang, Chunlin; Miao, Zhenyuan; Wu, Yuelin; Guo, Zizhao; Li, Jin; Yao, Jianzhong; Xing, Chengguo; Sheng, Chunquan; Zhang, Wannian Journal of Medicinal Chemistry, 2014 , vol. 57, # 3 p. 567 - 577

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Citation Number: 15

Abstract

Simultaneous inactivation of p53 and hyperactivation of nuclear factor-κB (NF-κB) is a common occurrence in human cancer. Currently, antitumor agents are being designed to selectively activate p53 or inhibit NF-κB. However, there is no concerted effort yet to deliberately design inhibitors that can simultaneously do both. This paper provided a proof- of-concept study that p53–MDM2 interaction and NF-κB pathway can be simultaneously ...