Studies on gambogic acid (IV): Exploring structure–activity relationship with IκB kinase-beta (IKKβ)

…, F Chen, X Wang, Z Liu, Q Yang, X Zhang, J Zhu…

Index: Sun, Haopeng; Chen, Feihong; Wang, Xiaojian; Liu, Zongliang; Yang, Qian; Zhang, Xiaojin; Zhu, Jia; Qiang, Lei; Guo, Qinglong; You, Qidong European Journal of Medicinal Chemistry, 2012 , vol. 51, p. 110 - 123

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Citation Number: 11

Abstract

Previously we have reported a series of gambogic acid's analogs and have identified a compound that possessed comparable in vitro growth inhibitory effect as gambogic acid. However, their target protein as well as the key pharmacophoric motifs on the target have not been identified yet. Herein we report that gambogic acid and its analogs inhibit the activity of IκB Kinase-beta (IKKβ) through suppressing the activation of TNFα/NF-κB ...