{"id":3110,"date":"2015-03-06T12:31:54","date_gmt":"2015-03-06T12:31:54","guid":{"rendered":"http:\/\/revoscience.com\/en\/?p=3110"},"modified":"2015-03-06T12:31:54","modified_gmt":"2015-03-06T12:31:54","slug":"genetic-modification-aids-cancer-drug-discovery","status":"publish","type":"post","link":"https:\/\/www.revoscience.com\/en\/genetic-modification-aids-cancer-drug-discovery\/","title":{"rendered":"Genetic modification aids cancer drug discovery"},"content":{"rendered":"

Genetically modifying cancer cells can aid in clarifying new cancer drugs\u2019 mechanism of action, according to a new study by researchers at KU Leuven\u2019s Laboratory of Virology and Chemotherapy (Rega Institute).<\/em><\/strong><\/span><\/p>\n

\"download<\/a>In the human cell, the nucleus contains our DNA and acts as a \u2018control centre\u2019 while the cytoplasm \u2013 the compartment around the nucleus \u2013 acts as the cell\u2019s \u2018body\u2019. It is here that proteins are produced and recycled.<\/span><\/p>\n

But whether a protein is active or not depends on its location in the cell \u2013 either in the nucleus or in the cytoplasm. The cell uses a transport system to ensure that a protein gets where it needs to be. In healthy cells, proteins are constantly being transported between the nucleus and the cytoplasm.\u00a0<\/span><\/p>\n

Transport in and out of the nucleus occurs with the help of various transport proteins. The most well-known among them, Exportin-1, transports more than 200 different proteins. Among Exportin-1\u2019s passengers are tumour-suppressing proteins. When in the nucleus, these proteins are able to detect damaged DNA and trigger cell death.<\/span><\/p>\n

But some cancers disrupt Exportin-1\u2019s normal functioning by transporting anti-cancer proteins out of the nucleus and into the cytoplasm \u2013 where they are prevented from carrying out their cancer-suppressing work.<\/span><\/p>\n

KPT-330<\/span><\/p>\n

Researchers at the Rega Institute and the Department of Chemistry previously reported an inhibitor of the Exportin-1 taxi. Karyopharm Therapeutics Inc., a clinical-stage pharmaceutical company focused on discovery and development of novel drugs directed against nuclear transport targets, has identified and developed the advanced Exportin-1 inhibitor KPT-330 for the treatment of cancer.<\/span><\/p>\n

In this new study, published online in\u00a0Chemistry & Biology<\/span><\/a><\/em>, the researchers confirm that KPT-330 is able to target and block the Exportin-1 taxi with extraordinary precision.<\/span><\/p>\n

The researchers\u2019 verification technique is borrowed from virology, explains senior author Dirk Daelemans: \u201cTo develop a novel molecule into a drug, we need to first be able to verify that it targets exactly what we want it to target and nothing else. This is called drug-target validation. For antiviral drugs, drug-target validation is achieved through gene modification. But while it is relatively easy to genetically modify a virus, applying the same technique to potential anti-cancer drugs was nearly impossible \u2013 until now.\u201d<\/span><\/p>\n

\u201cWe know that the molecule KPT-330 attaches to a particular amino acid, a building block of the Exportin-1 protein,\u201d continues Professor Daelemans. \u201cThanks to the latest developments in gene technology, we were able to modify that particular Exportin-1 amino acid in cancer cells.\u201d<\/span><\/p>\n

\u201cThe result? The key no longer fit in the lock and KPT-330\u2019s anti-cancer effect disappeared. This was the proof we needed to show that this molecule acts exclusively on the Exportin-1 taxi and no other targets. This technique can be used to develop other anti-cancer drugs as well, which bodes very well for the discovery and development of future cancer drugs,\u201d says Professor Daelemans.<\/span><\/p>\n","protected":false},"excerpt":{"rendered":"

Genetically modifying cancer cells can aid in clarifying new cancer drugs\u2019 mechanism of action, according to a new study by researchers at KU Leuven\u2019s Laboratory of Virology and Chemotherapy (Rega Institute). In the human cell, the nucleus contains our DNA and acts as a \u2018control centre\u2019 while the cytoplasm \u2013 the compartment around the nucleus […]<\/p>\n","protected":false},"author":6,"featured_media":3111,"comment_status":"open","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[17],"tags":[],"class_list":["post-3110","post","type-post","status-publish","format-standard","has-post-thumbnail","hentry","category-research"],"featured_image_urls":{"full":["https:\/\/www.revoscience.com\/en\/wp-content\/uploads\/2015\/03\/download-1.jpg",278,181,false],"thumbnail":["https:\/\/www.revoscience.com\/en\/wp-content\/uploads\/2015\/03\/download-1-150x150.jpg",150,150,true],"medium":["https:\/\/www.revoscience.com\/en\/wp-content\/uploads\/2015\/03\/download-1.jpg",278,181,false],"medium_large":["https:\/\/www.revoscience.com\/en\/wp-content\/uploads\/2015\/03\/download-1.jpg",278,181,false],"large":["https:\/\/www.revoscience.com\/en\/wp-content\/uploads\/2015\/03\/download-1.jpg",278,181,false],"1536x1536":["https:\/\/www.revoscience.com\/en\/wp-content\/uploads\/2015\/03\/download-1.jpg",278,181,false],"2048x2048":["https:\/\/www.revoscience.com\/en\/wp-content\/uploads\/2015\/03\/download-1.jpg",278,181,false],"ultp_layout_landscape_large":["https:\/\/www.revoscience.com\/en\/wp-content\/uploads\/2015\/03\/download-1.jpg",278,181,false],"ultp_layout_landscape":["https:\/\/www.revoscience.com\/en\/wp-content\/uploads\/2015\/03\/download-1.jpg",278,181,false],"ultp_layout_portrait":["https:\/\/www.revoscience.com\/en\/wp-content\/uploads\/2015\/03\/download-1.jpg",278,181,false],"ultp_layout_square":["https:\/\/www.revoscience.com\/en\/wp-content\/uploads\/2015\/03\/download-1.jpg",278,181,false],"newspaper-x-single-post":["https:\/\/www.revoscience.com\/en\/wp-content\/uploads\/2015\/03\/download-1.jpg",278,181,false],"newspaper-x-recent-post-big":["https:\/\/www.revoscience.com\/en\/wp-content\/uploads\/2015\/03\/download-1.jpg",278,181,false],"newspaper-x-recent-post-list-image":["https:\/\/www.revoscience.com\/en\/wp-content\/uploads\/2015\/03\/download-1.jpg",95,62,false],"web-stories-poster-portrait":["https:\/\/www.revoscience.com\/en\/wp-content\/uploads\/2015\/03\/download-1.jpg",278,181,false],"web-stories-publisher-logo":["https:\/\/www.revoscience.com\/en\/wp-content\/uploads\/2015\/03\/download-1.jpg",96,63,false],"web-stories-thumbnail":["https:\/\/www.revoscience.com\/en\/wp-content\/uploads\/2015\/03\/download-1.jpg",150,98,false]},"author_info":{"info":["Amrita Tuladhar"]},"category_info":"Research<\/a>","tag_info":"Research","comment_count":"0","_links":{"self":[{"href":"https:\/\/www.revoscience.com\/en\/wp-json\/wp\/v2\/posts\/3110","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/www.revoscience.com\/en\/wp-json\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/www.revoscience.com\/en\/wp-json\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/www.revoscience.com\/en\/wp-json\/wp\/v2\/users\/6"}],"replies":[{"embeddable":true,"href":"https:\/\/www.revoscience.com\/en\/wp-json\/wp\/v2\/comments?post=3110"}],"version-history":[{"count":0,"href":"https:\/\/www.revoscience.com\/en\/wp-json\/wp\/v2\/posts\/3110\/revisions"}],"wp:featuredmedia":[{"embeddable":true,"href":"https:\/\/www.revoscience.com\/en\/wp-json\/wp\/v2\/media\/3111"}],"wp:attachment":[{"href":"https:\/\/www.revoscience.com\/en\/wp-json\/wp\/v2\/media?parent=3110"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/www.revoscience.com\/en\/wp-json\/wp\/v2\/categories?post=3110"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/www.revoscience.com\/en\/wp-json\/wp\/v2\/tags?post=3110"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}