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Molecules 2018, 23(1), 42; https://doi.org/10.3390/molecules23010042

Fascaplysin Sensitizes Anti-Cancer Effects of Drugs Targeting AKT and AMPK

1
Department of Biomedical Chemistry, College of Biomedical & Health Science, Konkuk University, Chungju 27478, Chungbuk, Korea
2
Severance Integrative Research Institute for Cerebral & Cardiovascular Diseases (SIRIC), Yonsei University College of Medicine, 50 Yonsei-ro, Seodaemun-gu, Seoul 03722, Korea
3
Jung-Ang Microbe Research Institute (JM), 398, Jikji-daero, Heungdeok-gu, Cheongju 28576, Chungbuk, Korea
4
Nanotechnology Research Center, Konkuk University, Chungju 27478, Korea
These authors contributed equally to this work.
*
Author to whom correspondence should be addressed.
Received: 22 November 2017 / Revised: 13 December 2017 / Accepted: 22 December 2017 / Published: 24 December 2017
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Abstract

Fascaplysin, 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
Keywords: fascaplysin; AKT; AMPK; chemoresistance; cancer fascaplysin; AKT; AMPK; chemoresistance; cancer
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).
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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.

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