{"id":7162,"date":"2025-11-17T14:50:19","date_gmt":"2025-11-17T19:50:19","guid":{"rendered":"https:\/\/cqdm.org\/?post_type=project&#038;p=7162"},"modified":"2025-11-17T14:55:41","modified_gmt":"2025-11-17T19:55:41","slug":"identification-and-optimization-of-mammalian-fut8-inhibitors","status":"publish","type":"project","link":"https:\/\/cqdm.org\/en\/achievement\/funded-projects\/identification-and-optimization-of-mammalian-fut8-inhibitors\/","title":{"rendered":"Identification and optimization of mammalian FUT8 inhibitors"},"content":{"rendered":"\n<div class=\"wp-block-columns is-layout-flex wp-container-core-columns-is-layout-28f84493 wp-block-columns-is-layout-flex\">\n<div class=\"wp-block-column is-layout-flow wp-block-column-is-layout-flow\">\n<p class=\"is-style-suptitle\"><strong>Principal Investigator<\/strong><\/p>\n\n\n\n<p><strong>David Kwan<\/strong><br>Concordia University<\/p>\n\n\n\n<p><\/p>\n<\/div>\n<\/div>\n\n\n\n<hr class=\"wp-block-separator has-alpha-channel-opacity\"\/>\n\n\n\n<h2 class=\"wp-block-heading\"><span style=\"\">Project of <\/span><strong><strong>$<strong>934,399<\/strong><\/strong><\/strong> <strong><strong><strong><strong><strong><strong><strong><strong><strong><strong><strong><strong><strong><strong><strong><strong><strong><strong><strong><strong><strong><strong><strong><strong><strong><strong><strong><strong><strong><strong><strong><strong><strong><strong><strong><strong><strong><strong><strong><strong><strong><strong><strong><strong><strong><strong><strong><strong><strong><strong>over 3 years<\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/strong><\/h2>\n\n\n\n<ul class=\"wp-block-list is-style-checkmark\">\n<li><strong><strong>Supported by CQDM through:<\/strong><\/strong><br>Minist\u00e8re de l\u2019\u00c9conomie, de l\u2019Innovation et de l\u2019\u00c9nergie du Qu\u00e9bec (MEIE)<\/li>\n\n\n\n<li><strong><strong><strong>And by co-funding partners:<\/strong><\/strong><\/strong><br>&#8211; Paraza Pharma inc.<br>&#8211; GlycoSyn<br>&#8211; Mitacs<br>&#8211; Universit\u00e9 Concordia<\/li>\n<\/ul>\n\n\n\n<hr class=\"wp-block-separator has-alpha-channel-opacity\"\/>\n\n\n\n<h3 class=\"wp-block-heading\">Challenge<\/h3>\n\n\n\n<p>Glycosylation is a post-translational modification on most eukaryotic proteins that influences diverse functions such as protein folding, stability, and receptor activation. FUT8-mediated core-fucosylation of N-glycans is essential for mammalian development and this core fucose moiety is critical for the activation of cell-surface receptors like TGF\u03b2R, EGFR, and VEGFR. Dysregulation of FUT8 is also a marker and driver of many cancers. Identifying inhibitors of FUT8 would provide new and efficient means of producing therapeutic biologics, namely afucosylated monoclonal antibodies (mAbs), which are more effective at targeting cancer cells in vivo than their fucosylated counterparts.<\/p>\n\n\n\n<h3 class=\"wp-block-heading\">Solution<\/h3>\n\n\n\n<p>Together with Paraza Pharma, the team will implement an automated screening strategy and screen a 50,000-compound library using the fluorescence-based FUT8 activity assay developed by the Kwan lab. While this will be a key step in developing small molecule therapeutics targeting FUT8 in cancer patients, a more immediate application will be as process ingredients for controlling core-fucosylation as a post-translational modification of therapeutic antibodies produced in mammalian cell culture.<\/p>\n\n\n\n<h3 class=\"wp-block-heading\">Expected Achievements\/Impact<\/h3>\n\n\n\n<p>Commercialization of FUT8 inhibitors as tools to control glycosylation of biologics production (e.g., cancer targeting therapeutic antibodies) with the field-specific licensing to GlycoSyn will also position us to attract further investment towards development of small molecule therapeutics targeting FUT8 directly in patients.<\/p>\n","protected":false},"featured_media":3830,"template":"","project-category":[96],"class_list":["post-7162","project","type-project","status-publish","has-post-thumbnail","hentry","project-category-small-molecules"],"acf":[],"_links":{"self":[{"href":"https:\/\/cqdm.org\/en\/wp-json\/wp\/v2\/project\/7162","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/cqdm.org\/en\/wp-json\/wp\/v2\/project"}],"about":[{"href":"https:\/\/cqdm.org\/en\/wp-json\/wp\/v2\/types\/project"}],"wp:featuredmedia":[{"embeddable":true,"href":"https:\/\/cqdm.org\/en\/wp-json\/wp\/v2\/media\/3830"}],"wp:attachment":[{"href":"https:\/\/cqdm.org\/en\/wp-json\/wp\/v2\/media?parent=7162"}],"wp:term":[{"taxonomy":"project-category","embeddable":true,"href":"https:\/\/cqdm.org\/en\/wp-json\/wp\/v2\/project-category?post=7162"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}