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The inducible enzyme microsomal prostaglandin E synthase\u20101 (mPGES\u20101), catalyzing the terminal step of PGE\n                    <jats:sub>2<\/jats:sub>\n                    biosynthesis, is an attractive target for selective PGE\n                    <jats:sub>2<\/jats:sub>\n                    inhibition. To identify mPGES\u20101 inhibitors, we investigated the effect of aminothiazoles on inflammation\u2010induced PGE\n                    <jats:sub>2<\/jats:sub>\n                    synthesis\n                    <jats:italic>in vitro<\/jats:italic>\n                    , using human gingival fibroblasts stimulated with the cytokine IL\u20101\u03b2 and a cell\u2010free mPGES\u20101 activity assay, as well as on inflammation\u2010induced bone resorption\n                    <jats:italic>in vivo<\/jats:italic>\n                    , using ligature\u2010induced experimental periodontitis in Sprague\u2010Dawley rats. Aminothiazoles 4\u2010([4\u2010(2\u2010naphthyl)\u20101,3\u2010thiazol\u20102\u2010yl]amino)phenol (TH\u2010848) and 4\u2010(3\u2010fluoro\u20104\u2010methoxyphenyl)\u2010\n                    <jats:italic>N<\/jats:italic>\n                    \u2010(4\u2010phenoxyphenyl)\u20101,3\u2010thiazol\u20102\u2010amine (TH\u2010644) reduced IL\u20101\u03b2\u2010induced PGE\n                    <jats:sub>2<\/jats:sub>\n                    production in fibroblasts (IC\n                    <jats:sub>50<\/jats:sub>\n                    1.1 and 1.5 \u03bcM, respectively) as well as recombinant mPGES\u20101 activity, without affecting activity or expression of the upstream enzyme cyclooxygenase\u20102. In ligature\u2010induced experimental periodontitis, alveolar bone loss, assessed by X\u2010ray imaging, was reduced by 46% by local treatment with TH\u2010848, compared to vehicle, without any systemic effects on PGE\n                    <jats:sub>2<\/jats:sub>\n                    , 6\u2010keto PGF\n                    <jats:sub>1\u03b1<\/jats:sub>\n                    , LTB\n                    <jats:sub>4<\/jats:sub>\n                    or cytokine levels. In summary, these results demonstrate that the aminothiazoles represent novel mPGES\u20101 inhibitors for inhibition of PGE\n                    <jats:sub>2<\/jats:sub>\n                    production and reduction of bone resorption in experimental periodontitis, and may be used as potential anti\u2010inflammatory drugs for treatment of chronic inflammatory diseases, including periodontitis.\u2014Kats, A., B\u00e5ge, T., Georgsson, P., J\u00f6nsson, J., Quezada, H. C., Gustafsson, A., Jansson, L., Lindberg, C., N\u00e4sstr\u00f6m, K., Yucel\u2010Lindberg, T. Inhibition of microsomal prostaglandin E synthase\u20101 by aminothiazoles decreases prostaglandin E\n                    <jats:sub>2<\/jats:sub>\n                    synthesis\n                    <jats:italic>in vitro<\/jats:italic>\n                    and ameliorates experimental periodontitis\n                    <jats:italic>in vivo<\/jats:italic>\n                    .\n                    <jats:italic>FASEB J.<\/jats:italic>\n                    27, 2328\u20132341 (2013).\n                    <jats:ext-link xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" xlink:href=\"http:\/\/www.fasebj.org\">www.fasebj.org<\/jats:ext-link>\n                  <\/jats:p>","DOI":"10.1096\/fj.12-214445","type":"journal-article","created":{"date-parts":[[2013,2,28]],"date-time":"2013-02-28T13:34:59Z","timestamp":1362058499000},"page":"2328-2341","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":24,"title":["Inhibition of microsomal prostaglandin E synthase\u20101 by aminothiazoles decreases prostaglandin E\n                    <sub>2<\/sub>\n                    synthesis\n                    <i>in vitro<\/i>\n                    and ameliorates experimental periodontitis\n                    <i>in vivo<\/i>"],"prefix":"10.1096","volume":"27","author":[{"given":"Anna","family":"Kats","sequence":"first","affiliation":[{"name":"Division of Periodontology Department of Dental Medicine Karolinska Institutet Huddinge Sweden"},{"name":"Division of Pediatric Dentistry Karolinska Institutet Huddinge Sweden"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Tove","family":"B\u00e5ge","sequence":"additional","affiliation":[{"name":"Division of Periodontology Department of Dental Medicine Karolinska Institutet Huddinge Sweden"},{"name":"Division of Pediatric Dentistry Karolinska Institutet Huddinge 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