{"id":2416,"date":"2019-02-22T15:07:00","date_gmt":"2019-02-22T15:07:00","guid":{"rendered":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/?p=2416"},"modified":"2026-01-26T16:28:04","modified_gmt":"2026-01-26T16:28:04","slug":"crbn-versus-vhl","status":"publish","type":"post","link":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/2019\/02\/22\/crbn-versus-vhl\/","title":{"rendered":"CRBN versus VHL"},"content":{"rendered":"<p>Our new PROTAC paper on hijacking E3 ligases against each others is now published in Bioorg. Med. Chem.<\/p>\n<p><a href=\"https:\/\/doi.org\/10.1016\/j.bmc.2019.02.048\">Read the full paper Open Access<\/a>.<\/p>\n<p>Well done Miriam, Chiara, Scott and Andrea on this work!<\/p>\n<div id='gallery-1' class='gallery galleryid-2416 gallery-columns-3 gallery-size-large'><figure class='gallery-item'>\n\t\t\t<div class='gallery-icon landscape'>\n\t\t\t\t<a href='https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/ToC-CRBN-VHL-revised-01-2-scaled.jpg'><img loading=\"lazy\" decoding=\"async\" width=\"1024\" height=\"730\" src=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/ToC-CRBN-VHL-revised-01-2-scaled.jpg\" class=\"attachment-large size-large\" alt=\"ToC Graphic for CRBN VHL\" \/><\/a>\n\t\t\t<\/div><\/figure><figure class='gallery-item'>\n\t\t\t<div class='gallery-icon landscape'>\n\t\t\t\t<a href='https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/CRBN-VHL-2-scaled.jpg'><img loading=\"lazy\" decoding=\"async\" width=\"1024\" height=\"895\" src=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/CRBN-VHL-2-scaled.jpg\" class=\"attachment-large size-large\" alt=\"Figure 1. Previously published homo-PROTACs CM11 and CC15a, which induce self-degradation of the E3 ligases VHL and CRBN, respectively\" \/><\/a>\n\t\t\t<\/div><\/figure><figure class='gallery-item'>\n\t\t\t<div class='gallery-icon portrait'>\n\t\t\t\t<a href='https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/CRBN-VHL-fig02-scaled.jpg'><img loading=\"lazy\" decoding=\"async\" width=\"664\" height=\"1024\" src=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/CRBN-VHL-fig02-scaled.jpg\" class=\"attachment-large size-large\" alt=\"Figure 2. Design of VHL-CRBN conjugates explored in this work\" \/><\/a>\n\t\t\t<\/div><\/figure><figure class='gallery-item'>\n\t\t\t<div class='gallery-icon landscape'>\n\t\t\t\t<a href='https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/CRBN-VHL-fig03-scaled.jpg'><img loading=\"lazy\" decoding=\"async\" width=\"1024\" height=\"563\" src=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/CRBN-VHL-fig03-scaled.jpg\" class=\"attachment-large size-large\" alt=\"Figure 3. Chemical structure of VHL ligands 1 and 2, and CRBN ligand 3\" \/><\/a>\n\t\t\t<\/div><\/figure><figure class='gallery-item'>\n\t\t\t<div class='gallery-icon landscape'>\n\t\t\t\t<a href='https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/CRBN-VHL-scheme01-scaled.jpg'><img loading=\"lazy\" decoding=\"async\" width=\"1024\" height=\"216\" src=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/CRBN-VHL-scheme01-scaled.jpg\" class=\"attachment-large size-large\" alt=\"Scheme 1. Synthesis of PROTACs 7a-b\" \/><\/a>\n\t\t\t<\/div><\/figure><figure class='gallery-item'>\n\t\t\t<div class='gallery-icon landscape'>\n\t\t\t\t<a href='https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/CRBN-VHL-scheme02-scaled.jpg'><img loading=\"lazy\" decoding=\"async\" width=\"1024\" height=\"770\" src=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/CRBN-VHL-scheme02-scaled.jpg\" class=\"attachment-large size-large\" alt=\"Scheme 2. Synthesis of PROTACs 14a-e\" \/><\/a>\n\t\t\t<\/div><\/figure><figure class='gallery-item'>\n\t\t\t<div class='gallery-icon landscape'>\n\t\t\t\t<a href='https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/CRBN-VHL-scheme03-scaled.jpg'><img loading=\"lazy\" decoding=\"async\" width=\"1024\" height=\"490\" src=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/CRBN-VHL-scheme03-scaled.jpg\" class=\"attachment-large size-large\" alt=\"Scheme 3. Synthesis of PROTACs 18a-c\" \/><\/a>\n\t\t\t<\/div><\/figure><figure class='gallery-item'>\n\t\t\t<div class='gallery-icon landscape'>\n\t\t\t\t<a href='https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/CRBN-VHL-scheme04-scaled.jpg'><img loading=\"lazy\" decoding=\"async\" width=\"1024\" height=\"601\" src=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/CRBN-VHL-scheme04-scaled.jpg\" class=\"attachment-large size-large\" alt=\"Scheme 4. Synthesis of PROTACs 22a-c\" \/><\/a>\n\t\t\t<\/div><\/figure><figure class='gallery-item'>\n\t\t\t<div class='gallery-icon landscape'>\n\t\t\t\t<a href='https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/CRBN-VHL-fig04.jpg'><img loading=\"lazy\" decoding=\"async\" width=\"1024\" height=\"552\" src=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/CRBN-VHL-fig04.jpg\" class=\"attachment-large size-large\" alt=\"Figure 4. Screening of VHL-CRBN hetero-PROTACs\" \/><\/a>\n\t\t\t<\/div><\/figure><figure class='gallery-item'>\n\t\t\t<div class='gallery-icon landscape'>\n\t\t\t\t<a href='https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/CRBN-VHL-fig05-scaled.jpg'><img loading=\"lazy\" decoding=\"async\" width=\"1024\" height=\"859\" src=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/CRBN-VHL-fig05-scaled.jpg\" class=\"attachment-large size-large\" alt=\"Figure 5. Compound 14a induces rapid depletion of CRBN, but not of VHL\" \/><\/a>\n\t\t\t<\/div><\/figure>\n\t\t<\/div>\n\n","protected":false},"excerpt":{"rendered":"<p>Our new PROTAC paper on hijacking E3 ligases against each others is now published in Bioorg. Med. Chem. Read the full paper Open Access. Well done Miriam, Chiara, Scott and Andrea on this work!<\/p>\n","protected":false},"author":1,"featured_media":0,"comment_status":"open","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[17,4],"tags":[],"class_list":["post-2416","post","type-post","status-publish","format-standard","hentry","category-17","category-news"],"blocksy_meta":{"styles_descriptor":{"styles":{"desktop":"","tablet":"","mobile":""},"google_fonts":[],"version":7}},"_links":{"self":[{"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/posts\/2416","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=2416"}],"version-history":[{"count":2,"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/posts\/2416\/revisions"}],"predecessor-version":[{"id":4865,"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/posts\/2416\/revisions\/4865"}],"wp:attachment":[{"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/media?parent=2416"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/categories?post=2416"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/tags?post=2416"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}