Fascaplysin Sensitizes Anti-Cancer Effects of Drugs Targeting AKT and AMPK
AbstractFascaplysin, a natural product isolated from marine sponges, is a potential candidate for the development of anti-cancer drugs. However, the mechanism underlying its therapeutic effect of strengthening anti-cancer efficacy of other drugs is poorly understood. Here, we found that fascaplysin increases phosphorylation of protein kinase B (PKB), also known as AKT, and adenosine monophosphate-activated protein kinase (AMPK), which are considered therapeutic targets for cancer treatment due to their anti-apoptotic or pro-survival functions in cancer. A cell viability assay revealed that pharmacological suppression of AKT using LY294002 enhanced the anti-cancer effect of fascaplysin in various cancer cells. Similarly, fascaplysin was observed to have improved anti-cancer effects in combination with compound C, a selective AMPK inhibitor. Another challenge showed that fascaplysin increased the efficacy of methotrexate (MTX)-mediated cancer therapy by suppressing genes related to folate and purine metabolism. Overall, these results suggest that fascaplysin may be useful for improving the anti-cancer efficacy of targeted anti-cancer drugs, such as inhibitors of phosphoinositide 3-kinase AKT signaling, and chemotherapeutic agents, such as MTX. View Full-Text
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Oh, T.-I.; Lee, J.H.; Kim, S.; Nam, T.-J.; Kim, Y.-S.; Kim, B.M.; Yim, W.J.; Lim, J.-H. Fascaplysin Sensitizes Anti-Cancer Effects of Drugs Targeting AKT and AMPK. Molecules 2018, 23, 42.
Oh T-I, Lee JH, Kim S, Nam T-J, Kim Y-S, Kim BM, Yim WJ, Lim J-H. Fascaplysin Sensitizes Anti-Cancer Effects of Drugs Targeting AKT and AMPK. Molecules. 2018; 23(1):42.Chicago/Turabian Style
Oh, Taek-In; Lee, Jun H.; Kim, Seongman; Nam, Taek-Jin; Kim, Young-Seon; Kim, Byeong M.; Yim, Woo J.; Lim, Ji-Hong. 2018. "Fascaplysin Sensitizes Anti-Cancer Effects of Drugs Targeting AKT and AMPK." Molecules 23, no. 1: 42.
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