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Here, we assessed the anti\u2010allergic effects of the anti\u2010cancer drug tozasertib specifically regarding regulatory effects on mast cell activation.<\/jats:p><\/jats:sec><jats:sec><jats:title>Experimental Approach<\/jats:title><jats:p>Tozasertib effects on mast cell degranulation were determined by measuring \u03b2\u2010hexosaminidase and histamine release and by assessing morphological changes in RBL\u20102H3 and mouse bone marrow\u2010derived mast cells (BMMCs) stimulated with mouse anti\u2010dinitrophenyl (DNP)\u2010IgE\/DNP\u2010human serum albumin or human LAD2 cells activated with phorbol\u201012\u2010myristate 13\u2010acetate plus calcium ionophore (PMACI). Western blots were performed to detect the expression of molecules involved in NF\u2010\u03baB, MAPK, and Aurora kinase signalling. in vivo anti\u2010allergic effects of tozasertib were determined in the murine IgE\u2010mediated passive cutaneous anaphylaxis (PCA) and ovalbumin (OVA)\u2010induced active systemic anaphylaxis (ASA) models.<\/jats:p><\/jats:sec><jats:sec><jats:title>Key Results<\/jats:title><jats:p>Tozasertib treatment decreased high\u2010affinity IgE receptor (Fc\u03b5RI) or PMACI\u2010mediated degranulation in RBL\u20102H3 cells and in BMMCs or LAD2 cells as shown by \u03b2\u2010hexosaminidase or histamine levels. Similarly, tozasertib prevented morphological changes in mast cells, such as particle release and F\u2010actin reorganization. In addition, tozasertib markedly decreased expression of phosphorylated (p)\u2010NF\u2010\u03baB p65, p\u2010Erk1\/2, p\u2010p38, and p\u2010Aurora A\/B, indicating that tozasertib can inhibit the signalling pathway mediating mast cell activation. Tozasertib attenuated IgE\/Ag\u2010induced PCA dose\u2010dependently, as shown by reduced Evans blue staining. Similarly, tozasertib reduced body temperature levels and serum histamine levels in OVA\u2010challenged ASA mice.<\/jats:p><\/jats:sec><jats:sec><jats:title>Conclusion and Implications<\/jats:title><jats:p>The Aurora kinase inhibitor tozasertib suppressed mast cell activation in vitro and in vivo. Tozasertib may be a potential drug, targeting mast cell activation, to treat allergic diseases or mastocytosis.<\/jats:p><\/jats:sec>","DOI":"10.1111\/bph.15012","type":"journal-article","created":{"date-parts":[[2020,2,4]],"date-time":"2020-02-04T08:37:10Z","timestamp":1580805430000},"page":"2848-2859","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":23,"title":["Aurora kinase inhibitor tozasertib suppresses mast cell activation <i>in vitro<\/i> and <i>in vivo<\/i>"],"prefix":"10.1111","volume":"177","author":[{"ORCID":"https:\/\/orcid.org\/0000-0003-4837-3810","authenticated-orcid":false,"given":"Li\u2010Na","family":"Zhang","sequence":"first","affiliation":[{"name":"Department of Biochemistry and Molecular Biology, School of Medicine Shenzhen University  Shenzhen China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-5754-8697","authenticated-orcid":false,"given":"Kunmei","family":"Ji","sequence":"additional","affiliation":[{"name":"Department of Biochemistry and Molecular Biology, School of Medicine Shenzhen University  Shenzhen China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-6691-1283","authenticated-orcid":false,"given":"Yue\u2010Tong","family":"Sun","sequence":"additional","affiliation":[{"name":"Department of Biochemistry and Molecular Biology, School of Medicine Shenzhen University  Shenzhen China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-5582-5243","authenticated-orcid":false,"given":"Yi\u2010Bo","family":"Hou","sequence":"additional","affiliation":[{"name":"Department of Biochemistry and Molecular Biology, School of Medicine Shenzhen University  Shenzhen China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-1372-8450","authenticated-orcid":false,"given":"Jia\u2010Jie","family":"Chen","sequence":"additional","affiliation":[{"name":"Department of Biochemistry and Molecular Biology, School of Medicine Shenzhen University  Shenzhen China"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2020,4,6]]},"reference":[{"key":"e_1_2_12_2_1","doi-asserted-by":"publisher","DOI":"10.1111\/bph.14748"},{"key":"e_1_2_12_3_1","doi-asserted-by":"publisher","DOI":"10.1111\/bph.14752"},{"key":"e_1_2_12_4_1","doi-asserted-by":"publisher","DOI":"10.1111\/bph.14112"},{"key":"e_1_2_12_5_1","doi-asserted-by":"publisher","DOI":"10.1177\/1753425911435265"},{"key":"e_1_2_12_6_1","doi-asserted-by":"publisher","DOI":"10.1093\/infdis\/113.1.22"},{"key":"e_1_2_12_7_1","doi-asserted-by":"publisher","DOI":"10.1007\/s00280-015-2766-z"},{"key":"e_1_2_12_8_1","doi-asserted-by":"publisher","DOI":"10.1007\/978-1-4939-7896-0_8"},{"key":"e_1_2_12_9_1","doi-asserted-by":"publisher","DOI":"10.1111\/all.12650"},{"key":"e_1_2_12_10_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.canlet.2006.12.004"},{"key":"e_1_2_12_11_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ceca.2017.08.002"},{"key":"e_1_2_12_12_1","doi-asserted-by":"publisher","DOI":"10.1007\/978-1-4939-7896-0_7"},{"key":"e_1_2_12_13_1","doi-asserted-by":"publisher","DOI":"10.1111\/bph.14153"},{"key":"e_1_2_12_14_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bpj.2008.11.015"},{"key":"e_1_2_12_15_1","doi-asserted-by":"publisher","DOI":"10.1007\/s10753-014-9990-2"},{"key":"e_1_2_12_16_1","doi-asserted-by":"publisher","DOI":"10.3389\/fimmu.2012.00130"},{"key":"e_1_2_12_17_1","doi-asserted-by":"publisher","DOI":"10.1053\/j.seminoncol.2015.09.022"},{"issue":"4","key":"e_1_2_12_18_1","doi-asserted-by":"crossref","first-page":"2243","DOI":"10.4049\/jimmunol.162.4.2243","article-title":"The role of actin microfilaments in the down\u2010regulation of the degranulation response in RBL\u20102H3 mast cells","volume":"162","author":"Frigeri L.","year":"1999","journal-title":"Journal of Immunology"},{"key":"e_1_2_12_19_1","doi-asserted-by":"publisher","DOI":"10.3390\/molecules23113039"},{"key":"e_1_2_12_20_1","doi-asserted-by":"publisher","DOI":"10.1021\/acs.jafc.7b04314"},{"issue":"3","key":"e_1_2_12_21_1","first-page":"218","article-title":"Integrated signalling pathways for mast\u2010cell activation. 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