{"id":20,"date":"2016-06-07T21:04:13","date_gmt":"2016-06-07T21:04:13","guid":{"rendered":"http:\/\/labs.icahn.mssm.edu\/panlab\/?page_id=20"},"modified":"2016-06-07T21:25:28","modified_gmt":"2016-06-07T21:25:28","slug":"the-early-drug-effort","status":"publish","type":"page","link":"https:\/\/labs.icahn.mssm.edu\/panlab\/the-early-drug-effort\/","title":{"rendered":""},"content":{"rendered":"<p><img loading=\"lazy\" decoding=\"async\" class=\"aligncenter size-full wp-image-21\" src=\"https:\/\/labs.icahn.mssm.edu\/panlab\/wp-content\/uploads\/sites\/90\/2016\/06\/Discovery.png\" alt=\"Discovery\" width=\"900\" height=\"584\" srcset=\"https:\/\/labs.icahn.mssm.edu\/panlab\/wp-content\/uploads\/sites\/90\/2016\/06\/Discovery.png 900w, https:\/\/labs.icahn.mssm.edu\/panlab\/wp-content\/uploads\/sites\/90\/2016\/06\/Discovery-300x195.png 300w\" sizes=\"auto, (max-width: 900px) 100vw, 900px\" \/><\/p>\n<p><strong>Discovery of small molecule modulators of the Cullin-RING E3 ubiquitin ligases<\/strong><\/p>\n<p style=\"text-align: justify\">To date there is no drug-lead like small molecule modulators targeting the catalytic activity of Cullin-RING E3 ubiquitin ligases (CRLs). To meet this challenge we have developed a fluorescence (F\u00f6rster) resonance energy transfer (FRET)-based assay that requires the catalytic activity of a CRL\u2019s core ligase complex. We have then optimized this assay into a robust high throughput-screening (HTS) platform. Preliminary HTS has resulted in identification of a score of compounds that bind to CRL\u2019s core ligase complex and inhibit its activity. The newly identified CRL core ligase inhibitor exhibits a broad cytotoxic activity against a panel of solid and hematopoietic tumor cell lines, suggesting therapeutic potential for this class of inhibitors.<\/p>\n","protected":false},"excerpt":{"rendered":"<p>Discovery of small molecule modulators of the Cullin-RING E3 ubiquitin ligases To date there is no drug-lead like small molecule modulators targeting the catalytic activity of Cullin-RING E3 ubiquitin ligases (CRLs). To meet this challenge we have developed a fluorescence (F\u00f6rster) resonance energy transfer (FRET)-based assay that requires the catalytic activity of a CRL\u2019s core [&hellip;]<\/p>\n","protected":false},"author":146,"featured_media":0,"parent":0,"menu_order":0,"comment_status":"closed","ping_status":"closed","template":"","meta":{"footnotes":""},"class_list":["post-20","page","type-page","status-publish","hentry"],"aioseo_notices":[],"_links":{"self":[{"href":"https:\/\/labs.icahn.mssm.edu\/panlab\/wp-json\/wp\/v2\/pages\/20","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/labs.icahn.mssm.edu\/panlab\/wp-json\/wp\/v2\/pages"}],"about":[{"href":"https:\/\/labs.icahn.mssm.edu\/panlab\/wp-json\/wp\/v2\/types\/page"}],"author":[{"embeddable":true,"href":"https:\/\/labs.icahn.mssm.edu\/panlab\/wp-json\/wp\/v2\/users\/146"}],"replies":[{"embeddable":true,"href":"https:\/\/labs.icahn.mssm.edu\/panlab\/wp-json\/wp\/v2\/comments?post=20"}],"version-history":[{"count":2,"href":"https:\/\/labs.icahn.mssm.edu\/panlab\/wp-json\/wp\/v2\/pages\/20\/revisions"}],"predecessor-version":[{"id":55,"href":"https:\/\/labs.icahn.mssm.edu\/panlab\/wp-json\/wp\/v2\/pages\/20\/revisions\/55"}],"wp:attachment":[{"href":"https:\/\/labs.icahn.mssm.edu\/panlab\/wp-json\/wp\/v2\/media?parent=20"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}