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Therefore, novel TKIs effective against T674I FIP1L1-PDGFR\u03b1 are needed. Ponatinib (AP24534) is a novel orally bioavailable TKI against T315I Bcr-Abl, but it is not clear whether ponatinib is effective against T674I FIP1L1-PDGFR\u03b1. The purpose of this study was to examine the effect of ponatinib on T674I FIP1L1-PDGFR\u03b1.<\/jats:p>\n              <\/jats:sec><jats:sec>\n                <jats:title>Methods<\/jats:title>\n                <jats:p>Molecular docking analysis <jats:italic>in silico<\/jats:italic> was performed. The effects of ponatinib on PDGFR\u03b1 signaling pathways, apoptosis and cell cycling were examined in EOL-1, BaF3 cells expressing either wild type (WT) or T674I FIP1L1-PDGFR\u03b1. The in vivo antitumor activity of ponatinib was evaluated with xenografted BaF3-T674I FIP1L1-PDGFR\u03b1 cells in nude mice models.<\/jats:p>\n              <\/jats:sec><jats:sec>\n                <jats:title>Results<\/jats:title>\n                <jats:p>Molecular docking analysis revealed that ponatinib could bind to the DFG (Asp-Phe-Gly)-out state of T674I PDGFR\u03b1. Ponatinib potently inhibited the phosphorylation of WT and T674I FIP1L1-PDGFR\u03b1 and their downstream signaling molecules (e.g., Stat3, Stat5). Ponatinib strikingly inhibited the growth of both WT and T674I FIP1L1-PDGFR\u03b1-carrying CEL cells (IC<jats:sub>50<\/jats:sub>: 0.004\u20132.5 nM). It induced apoptosis in CEL cells with caspase-3-dependent cleavage of Mcl-1, and inhibited tyrosine phosphorylation of \u03b2-catenin to decrease its stability and pro-survival functions. In vivo, ponatinib abrogated the growth of xenografted BaF3-T674I FIP1L1-PDGFR\u03b1 cells in nude mice.<\/jats:p>\n              <\/jats:sec><jats:sec>\n                <jats:title>Conclusions<\/jats:title>\n                <jats:p>Ponatinib is a pan-FIP1L1-PDGFR\u03b1 inhibitor, and clinical trials are warranted to investigate its efficacy in imatinib-resistant CEL.<\/jats:p>\n              <\/jats:sec>","DOI":"10.1186\/1476-4598-13-17","type":"journal-article","created":{"date-parts":[[2014,1,28]],"date-time":"2014-01-28T16:05:41Z","timestamp":1390925141000},"update-policy":"https:\/\/doi.org\/10.1007\/springer_crossmark_policy","source":"Crossref","is-referenced-by-count":23,"title":["Ponatinib efficiently kills imatinib-resistant chronic eosinophilic leukemia cells harboring gatekeeper mutant T674I FIP1L1-PDGFR\u03b1: roles of Mcl-1 and \u03b2-catenin"],"prefix":"10.1186","volume":"13","author":[{"given":"Yanli","family":"Jin","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ke","family":"Ding","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Honglin","family":"Li","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Mengzhu","family":"Xue","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Xiaoke","family":"Shi","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Chengyan","family":"Wang","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jingxuan","family":"Pan","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"297","published-online":{"date-parts":[[2014,1,28]]},"reference":[{"key":"1240_CR1","doi-asserted-by":"publisher","first-page":"1201","DOI":"10.1056\/NEJMoa025217","volume":"348","author":"J Cools","year":"2003","unstructured":"Cools J, DeAngelo DJ, Gotlib J, Stover EH, Legare RD, Cortes J, Kutok J, Clark J, Galinsky I, Griffin JD: A tyrosine kinase created by fusion of the PDGFRA and FIP1L1 genes as a therapeutic target of imatinib in idiopathic hypereosinophilic syndrome. 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