Anti-cancer activity of the novel 2-hydroxydiarylamide derivatives IMD-0354 and KRT1853 through suppression of cancer cell invasion, proliferation, and survival mediated by TMPRSS4

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dc.contributor.authorSolbi Kim-
dc.contributor.authorDongjoon Ko-
dc.contributor.authorYunhee Lee-
dc.contributor.authorS Jang-
dc.contributor.authorY Lee-
dc.contributor.authorI Y Lee-
dc.contributor.authorSemi Kim-
dc.date.accessioned2019-10-28T16:30:11Z-
dc.date.available2019-10-28T16:30:11Z-
dc.date.issued2019-
dc.identifier.issn20452322-
dc.identifier.uri10.1038/s41598-019-46447-7ko
dc.identifier.urihttps://oak.kribb.re.kr/handle/201005/18882-
dc.description.abstractElevated expression of transmembrane serine protease 4 (TMPRSS4) correlates with poor prognosis in non-small cell lung cancer, gastric cancer, colorectal cancer, prostate cancer, and other cancer patients. Previously, we demonstrated that TMPRSS4 mediates tumor cell invasion, migration, proliferation, and metastasis. In addition, we reported novel 2-hydroxydiarylamide derivatives, IMD-0354 and KRT1853, as TMPRSS4 serine protease inhibitors. Here, we further evaluated the effects of the representative derivatives on TMPRSS4-mediated cellular function and signaling. IMD-0354 and KRT1853 inhibited cancer cell invasion, migration, and proliferation in TMPRSS4-expressing prostate, colon, and lung cancer cells. Both compounds suppressed TMPRSS4-mediated induction of Sp1/3, AP-1, and NF-κB transcription factors. Furthermore, TMPRSS4 promoted cancer cell survival and drug resistance, and both compounds enhanced anoikis sensitivity as well as reduced bcl-2 and survivin levels. Importantly, KRT1853 efficiently reduced tumor growth in prostate and colon cancer xenograft models. These results strongly recommend KRT1853 for further development as a novel anti-cancer agent.-
dc.publisherSpringer-Nature Pub Group-
dc.titleAnti-cancer activity of the novel 2-hydroxydiarylamide derivatives IMD-0354 and KRT1853 through suppression of cancer cell invasion, proliferation, and survival mediated by TMPRSS4-
dc.title.alternativeAnti-cancer activity of the novel 2-hydroxydiarylamide derivatives IMD-0354 and KRT1853 through suppression of cancer cell invasion, proliferation, and survival mediated by TMPRSS4-
dc.typeArticle-
dc.citation.titleScientific Reports-
dc.citation.number0-
dc.citation.endPage10003-
dc.citation.startPage10003-
dc.citation.volume9-
dc.contributor.affiliatedAuthorSolbi Kim-
dc.contributor.affiliatedAuthorDongjoon Ko-
dc.contributor.affiliatedAuthorYunhee Lee-
dc.contributor.affiliatedAuthorSemi Kim-
dc.contributor.alternativeName김솔비-
dc.contributor.alternativeName고동준-
dc.contributor.alternativeName이윤희-
dc.contributor.alternativeName장성휘-
dc.contributor.alternativeName이영훈-
dc.contributor.alternativeName이일영-
dc.contributor.alternativeName김세미-
dc.identifier.bibliographicCitationScientific Reports, vol. 9, pp. 10003-10003-
dc.identifier.doi10.1038/s41598-019-46447-7-
dc.description.journalClassY-
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Division of Biomedical Research > Immunotherapy Research Center > 1. Journal Articles
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