期刊
JOURNAL OF NATURAL PRODUCTS
卷 85, 期 4, 页码 1006-1017出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jnatprod.1c01154
关键词
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资金
- Swiss National Science Foundation [205321-176008]
- Swiss Cancer League [KFS-3727-08-2015]
- Swiss National Science Foundation (SNF) [205321_176008] Funding Source: Swiss National Science Foundation (SNF)
This study identified natural products that can inhibit oncogenic signaling in melanoma through a combination of techniques.
The incidence of melanoma, the most fatal dermatological cancer, has dramatically increased over the last few decades. Modern targeted therapy with kinase inhibitors induces potent clinical responses, but drug resistance quickly develops. Combination therapy improves treatment outcomes. Therefore, novel inhibitors targeting aberrant proliferative signaling in melanoma via the MAPK/ ERK and PI3K/AKT pathways are urgently needed. Biosensors were combined that report on ERK/AKT activity with image-based high-content screening and HPLC-based activity profiling. An in-house library of 2576 plant extracts was screened on two melanoma cell lines with different oncogenic mutations leading to pathological ERK/AKT activity. Out of 140 plant extract hits, 44 were selected for HPLC activity profiling. Active thymol derivatives and piperamides from Arnica montana and Piper nigrum were identified that inhibited pathological ERK and/or AKT activity. The pipeline used enabled an efficient identification of natural products targeting oncogenic signaling in melanoma.
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