{"id":3890,"date":"2017-01-20T14:39:00","date_gmt":"2017-01-20T14:39:00","guid":{"rendered":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/?p=3890"},"modified":"2026-01-28T09:48:05","modified_gmt":"2026-01-28T09:48:05","slug":"our-paper-studying-the-effect-of-linking-on-the-mechanism-of-action-of-bet-degraders","status":"publish","type":"post","link":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/2017\/01\/20\/our-paper-studying-the-effect-of-linking-on-the-mechanism-of-action-of-bet-degraders\/","title":{"rendered":"Our paper studying the effect of linking on the mechanism of action of BET degraders"},"content":{"rendered":"\n

Read our paper open access<\/a> here. The article will be published as part of the a Special Issue on \u201cInducing Protein Degradation as a Therapeutic Strategy<\/a>\u201c.<\/p>\n\n\n\n

\n
\"ToC
ToC Graphics<\/figcaption><\/figure>\n\n\n\n
\"Chart
Chart 1. Chemical Structures of Ligands for VHL (1) and CRBN (2) and BET Inhibitors 3 (JQ1) and 4 (I- BET726)<\/figcaption><\/figure>\n\n\n\n
\"Chart
Chart 2. Chemical Structures of VHL-Targeting PROTACs Based on 4 and 3 Used in This Study and Chemical Structure of CRBN-Targeting PROTAC 11 (ARV-825)<\/figcaption><\/figure>\n\n\n\n
\"Figure
Figure 1. Co-crystal structures to guide PROTAC linking design<\/figcaption><\/figure>\n\n\n\n
\"Figure
Figure 2. Protein degradation profile of VHL-based BET degraders<\/figcaption><\/figure>\n\n\n\n
\"Figure
Figure 3. Measuring cooperativities of ternary complex formation by ITC<\/figcaption><\/figure>\n\n\n\n
\"Figure
Figure 4. Antiproliferative and Myc-suppression activity of BET degraders and inhibitors<\/figcaption><\/figure>\n\n\n\n
\"Figure
Figure 5. PROTACs\u2019 SAR correlation plots.”<\/figcaption><\/figure>\n\n\n\n
\"J.
J. Med. Chem. Special Issue on “Inducing Protein Degradation as a Therapeutic Strategy<\/figcaption><\/figure>\n<\/figure>\n\n\n\n

<\/p>\n","protected":false},"excerpt":{"rendered":"

Read our paper open access here. The article will be published as part of the a Special Issue on \u201cInducing Protein Degradation as a Therapeutic Strategy\u201c.<\/p>\n","protected":false},"author":1,"featured_media":0,"comment_status":"open","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[19],"tags":[],"class_list":["post-3890","post","type-post","status-publish","format-standard","hentry","category-19"],"blocksy_meta":[],"_links":{"self":[{"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/posts\/3890","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/users\/1"}],"replies":[{"embeddable":true,"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/comments?post=3890"}],"version-history":[{"count":3,"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/posts\/3890\/revisions"}],"predecessor-version":[{"id":4951,"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/posts\/3890\/revisions\/4951"}],"wp:attachment":[{"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/media?parent=3890"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/categories?post=3890"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/tags?post=3890"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}