期刊
PLOS ONE
卷 13, 期 8, 页码 -出版社
PUBLIC LIBRARY SCIENCE
DOI: 10.1371/journal.pone.0202263
关键词
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资金
- Fundacao de Amparo a Pesquisa do Estado de Sao Paulo [14/15307-7]
- Research Resettlement Fund for the new faculty, the Research Institute for Veterinary Science
- BK21 PLUS Program for Creative Veterinary Science Research Center, Seoul National University
- National Research Foundation of Korea (NRF) grant - Korea government (MSIT) [2018R1A2B2002923]
- CAPES Foundationan agency under the Ministry of Education of Brazil [BEX 3159/14-0]
Naturally-occurring chalcones and synthetic chalcone analogues have been demonstrated to have many biological effects, including anti-inflammatory, anti-malarial, anti-fungal, and anti-oxidant/anti-cancerous activities. Compared to other chalcones, trans-chalcone exhibits superior inhibitory activity in cancer cell growth as shown via in vitro assays, and exerts anti-cancerous effects via the activation of the p53 tumor suppressor protein. Thus, characterization of the specific mechanisms, by which trans-chalcone activates p53, can aid development of new chemotherapeutic drugs that can be used individually or synergistically with other drugs. In this report, we found that trans-chalcone modulates many p53 target genes, HSP40 being the most induced gene in the RNA-Seq data using trans-chalcone-treated cells. CRM1 is also inhibited by trans-chalcone, resulting in the accumulation of p53 and other tumor suppressor proteins in the nucleus. Similar effects were seen using trans-chalcone derivatives. Overall, trans-chalcone could provide a strong foundation for the development of chalcone-based anti-cancer drugs.
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