An updated review of smac mimetics, lcl161, birinapant, and gdc-0152 in cancer treatment

Yung Chieh Chang, Chun Hei Antonio Cheung

研究成果: Review article同行評審

2 引文 斯高帕斯(Scopus)


Inhibitor of apoptosis proteins (IAPs) are suggested as therapeutic targets for cancer treatment. Smac/DIABLO is a natural IAP antagonist in cells; therefore, Smac mimetics have been developed for cancer treatment in the past decade. In this article, we review the anti-cancer potency and novel molecular targets of LCL161, birinapant, and GDC-0152. Preclinical studies demonstrated that Smac mimetics not only induce apoptosis but also arrest cell cycle, induce necroptosis, and induce immune storm in vitro and in vivo. The safety and tolerance of Smac mimetics are evaluated in phase 1 and phase 2 clinical trials. In addition, the combination of Smac mimetics and chemotherapeutic compounds was reported to improve anti-cancer effects. Interestingly, the novel anti-cancer molecular mechanism of action of Smac mimetics was reported in recent studies, suggesting that many unknown functions of Smac mimetics still need to be revealed. Exploring these currently unknown signaling pathways is important to provide hints for the modification and combination therapy of further compounds.

頁(從 - 到)1-13
期刊Applied Sciences (Switzerland)
出版狀態Published - 2021 1月 1

All Science Journal Classification (ASJC) codes

  • 材料科學(全部)
  • 儀器
  • 工程 (全部)
  • 製程化學與技術
  • 電腦科學應用
  • 流體流動和轉移過程


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