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In the present study, we found that the widely used antimalarial drug mefloquine was a <jats:styled-content style=\"fixed-case\">NF<\/jats:styled-content>\u2010\u03baB inhibitor that blocked the activation of I\u03baB\u03b1 kinase, leading to reduction of I\u03baB\u03b1 degradation, decrease of p65 phosphorylation, and suppressed expression of <jats:styled-content style=\"fixed-case\">NF<\/jats:styled-content>\u2010\u03baB target genes in <jats:styled-content style=\"fixed-case\">CRC<\/jats:styled-content> cells. We also found that mefloquine induced growth arrest and apoptosis of <jats:styled-content style=\"fixed-case\">CRC<\/jats:styled-content> cells harboring phosphorylated p65 in culture and in mice. Furthermore, expression of constitutive active <jats:styled-content style=\"fixed-case\">IKK<\/jats:styled-content>\u03b2 kinase significantly attenuated the cytotoxic effect of the compound. These results showed that mefloquine could exert antitumor action through inhibiting the <jats:styled-content style=\"fixed-case\">NF<\/jats:styled-content>\u2010\u03baB signaling pathway, and indicated that the antimalarial drug might be repurposed for anti\u2010<jats:styled-content style=\"fixed-case\">CRC<\/jats:styled-content> therapy in the clinic as a single agent or in combination with other anticancer drugs.<\/jats:p>","DOI":"10.1111\/cas.13540","type":"journal-article","created":{"date-parts":[[2018,2,17]],"date-time":"2018-02-17T14:08:42Z","timestamp":1518876522000},"page":"1220-1229","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":59,"title":["Antimalarial drug mefloquine inhibits nuclear factor kappa B signaling and induces apoptosis in colorectal cancer cells"],"prefix":"10.1111","volume":"109","author":[{"ORCID":"https:\/\/orcid.org\/0000-0001-7713-4734","authenticated-orcid":false,"given":"Xin","family":"Xu","sequence":"first","affiliation":[{"name":"Suzhou Institute of Systems Medicine Center for Systems Medicine Chinese Academy of Medical Sciences Suzhou China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jun","family":"Wang","sequence":"additional","affiliation":[{"name":"Department of Emergency Medicine First Affiliated Hospital Soochow University Suzhou China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Kunkun","family":"Han","sequence":"additional","affiliation":[{"name":"The Asclepius Technology Company Group and Asclepius Cancer Research Center Suzhou China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Shaoyan","family":"Li","sequence":"additional","affiliation":[{"name":"Suzhou Institute of Systems Medicine Center for Systems Medicine Chinese Academy of Medical Sciences Suzhou China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Feng","family":"Xu","sequence":"additional","affiliation":[{"name":"Department of Emergency Medicine First Affiliated Hospital Soochow University Suzhou China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yili","family":"Yang","sequence":"additional","affiliation":[{"name":"Suzhou Institute of Systems Medicine Center for Systems Medicine Chinese Academy of Medical Sciences Suzhou China"},{"name":"State Key Laboratory of Innovative Natural Medicine and TCM Injections Jiangxi Qingfeng Pharmaceutical Co. 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