{"id":417,"date":"2021-12-29T11:11:41","date_gmt":"2021-12-29T11:11:41","guid":{"rendered":"http:\/\/tbioinfo.icgeb.res.in\/bioinfo\/?p=417"},"modified":"2022-02-08T11:17:42","modified_gmt":"2022-02-08T11:17:42","slug":"a-plasmodium-falciparum-protein-tyrosine-phosphatase-inhibitor-identified-from-the-chembl-ntd-database-blocks-parasite-growth","status":"publish","type":"post","link":"https:\/\/bioinfo.icgeb.res.in\/bioinfo\/index.php\/2021\/12\/29\/a-plasmodium-falciparum-protein-tyrosine-phosphatase-inhibitor-identified-from-the-chembl-ntd-database-blocks-parasite-growth\/","title":{"rendered":"A Plasmodium falciparum protein tyrosine phosphatase inhibitor identified from the ChEMBL-NTD database blocks parasite growth"},"content":{"rendered":"<h2>Abstract<\/h2>\n<p style=\"text-align: justify;\">Post-translational modifications, especially reversible phosphorylation, are among the most common mechanisms that regulate protein function and biological processes in\u00a0<i>Plasmodium<\/i>\u00a0species. Of the\u00a0<i>Plasmodium<\/i>\u00a0phosphatases, phosphatase of regenerating liver (<i>Pf<\/i>PRL) is secreted and is an essential phosphatase. Here, we expressed\u00a0<i>Pf<\/i>PRL in a heterologous expression system, and then purified and characterized its phosphatase activity. We found that Novartis_003209, a previously identified inhibitor, inhibited the\u00a0<i>Pf<\/i>PRL phosphatase activity of recombinant\u00a0<i>Pf<\/i>PRL and blocked\u00a0<i>in\u00a0vitro<\/i>\u00a0parasite growth in a dose-dependent manner. Further,\u00a0<i>in\u00a0silico<\/i>\u00a0docking analysis of Novartis_003209 with all four\u00a0<i>P.\u00a0falciparum<\/i>\u00a0tyrosine phosphatases (PTP) demonstrated that Novartis_003209 is a\u00a0<i>Plasmodium<\/i>\u00a0PTP inhibitor. Overall, our results identify a scaffold as a potential starting point to design a PTP-specific inhibitor.<\/p>\n<p>Click here to know more:-\u00a0\u00a0<a href=\"https:\/\/febs.onlinelibrary.wiley.com\/doi\/full\/10.1002\/2211-5463.13171\">https:\/\/febs.onlinelibrary.wiley.com\/doi\/full\/10.1002\/2211-5463.13171<\/a><\/p>\n","protected":false},"excerpt":{"rendered":"<p>Abstract Post-translational modifications, especially reversible phosphorylation, are among the most common mechanisms that regulate protein function and biological processes in\u00a0Plasmodium\u00a0species. Of the\u00a0Plasmodium\u00a0phosphatases, phosphatase of regenerating liver (PfPRL) is secreted and is an essential phosphatase. Here, we expressed\u00a0PfPRL in a heterologous expression system, and then purified and characterized its phosphatase activity. We found that Novartis_003209, a [&hellip;]<\/p>\n","protected":false},"author":1,"featured_media":418,"comment_status":"closed","ping_status":"closed","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[5],"tags":[],"_links":{"self":[{"href":"https:\/\/bioinfo.icgeb.res.in\/bioinfo\/index.php\/wp-json\/wp\/v2\/posts\/417"}],"collection":[{"href":"https:\/\/bioinfo.icgeb.res.in\/bioinfo\/index.php\/wp-json\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/bioinfo.icgeb.res.in\/bioinfo\/index.php\/wp-json\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/bioinfo.icgeb.res.in\/bioinfo\/index.php\/wp-json\/wp\/v2\/users\/1"}],"replies":[{"embeddable":true,"href":"https:\/\/bioinfo.icgeb.res.in\/bioinfo\/index.php\/wp-json\/wp\/v2\/comments?post=417"}],"version-history":[{"count":2,"href":"https:\/\/bioinfo.icgeb.res.in\/bioinfo\/index.php\/wp-json\/wp\/v2\/posts\/417\/revisions"}],"predecessor-version":[{"id":754,"href":"https:\/\/bioinfo.icgeb.res.in\/bioinfo\/index.php\/wp-json\/wp\/v2\/posts\/417\/revisions\/754"}],"wp:featuredmedia":[{"embeddable":true,"href":"https:\/\/bioinfo.icgeb.res.in\/bioinfo\/index.php\/wp-json\/wp\/v2\/media\/418"}],"wp:attachment":[{"href":"https:\/\/bioinfo.icgeb.res.in\/bioinfo\/index.php\/wp-json\/wp\/v2\/media?parent=417"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/bioinfo.icgeb.res.in\/bioinfo\/index.php\/wp-json\/wp\/v2\/categories?post=417"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/bioinfo.icgeb.res.in\/bioinfo\/index.php\/wp-json\/wp\/v2\/tags?post=417"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}