{"id":2454,"date":"2018-12-12T16:18:00","date_gmt":"2018-12-12T16:18:00","guid":{"rendered":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/?p=2454"},"modified":"2026-01-26T16:28:04","modified_gmt":"2026-01-26T16:28:04","slug":"a-roadmap-for-protac-development","status":"publish","type":"post","link":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/2018\/12\/12\/a-roadmap-for-protac-development\/","title":{"rendered":"A Roadmap for PROTAC Development"},"content":{"rendered":"<p>Our SAR story disclosing dual Brd7\/9 PROTAC degrader VZ185 is published in J. Med. Chem.<\/p>\n<p>Congratulations to\u00a0Vittoria,\u00a0Scott,\u00a0Chiara\u00a0and\u00a0Andrea, and all our collaborators for their contributions to this work!<\/p>\n<h2 class=\"wp-block-heading\">Related Links<\/h2>\n<ul>\n<li><a href=\"https:\/\/www.promegaconnections.com\/a-roadmap-for-protac-development\/\" target=\"_blank\" rel=\"noreferrer noopener\">Promega Connections blog: \u201cA Roadmap for PROTAC Development\u201d<\/a><\/li>\n<\/ul>\n<div id='gallery-1' class='gallery galleryid-2454 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\/brd79-protac-1.jpeg'><img loading=\"lazy\" decoding=\"async\" width=\"1024\" height=\"435\" src=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-1-1024x435.jpeg\" class=\"attachment-large size-large\" alt=\"ToC Graphic for SAR story disclosing dual Brd7\/9 PROTAC degrader VZ185 is published in J. Med. Chem\" srcset=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-1-1024x435.jpeg 1024w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-1-300x127.jpeg 300w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-1-768x326.jpeg 768w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-1.jpeg 1319w\" sizes=\"auto, (max-width: 1024px) 100vw, 1024px\" \/><\/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\/brd79-protac-2.jpeg'><img loading=\"lazy\" decoding=\"async\" width=\"986\" height=\"912\" src=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-2.jpeg\" class=\"attachment-large size-large\" alt=\"Figure 1. Chemical structures of parent (1a, 1b, 2\u20134) and modified (1c, 2a\u20134a) BRD7\/9 and E3 ligase ligands. Functional groups selected for conjugation are shown in blue on parent ligands and in red on modified ligands.\" srcset=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-2.jpeg 986w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-2-300x277.jpeg 300w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-2-768x710.jpeg 768w\" sizes=\"auto, (max-width: 986px) 100vw, 986px\" \/><\/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\/brd79-protac-3.jpeg'><img loading=\"lazy\" decoding=\"async\" width=\"1024\" height=\"493\" src=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-3-1024x493.jpeg\" class=\"attachment-large size-large\" alt=\"Scheme 1. Synthesis of the BRD7\/9 Ligand 1c\" srcset=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-3-1024x493.jpeg 1024w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-3-300x144.jpeg 300w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-3-768x370.jpeg 768w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-3-1536x739.jpeg 1536w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-3-2048x986.jpeg 2048w\" sizes=\"auto, (max-width: 1024px) 100vw, 1024px\" \/><\/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\/brd79-protac-4.jpeg'><img loading=\"lazy\" decoding=\"async\" width=\"1024\" height=\"880\" src=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-4-1024x880.jpeg\" class=\"attachment-large size-large\" alt=\"Scheme 2. Synthesis of the First Generation of Degraders\" srcset=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-4-1024x880.jpeg 1024w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-4-300x258.jpeg 300w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-4-768x660.jpeg 768w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-4-1536x1320.jpeg 1536w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-4-2048x1760.jpeg 2048w\" sizes=\"auto, (max-width: 1024px) 100vw, 1024px\" \/><\/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\/brd79-protac-5.jpeg'><img loading=\"lazy\" decoding=\"async\" width=\"1024\" height=\"381\" src=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-5-1024x381.jpeg\" class=\"attachment-large size-large\" alt=\"Figure 2. Screening of first generation of degraders.\" srcset=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-5-1024x381.jpeg 1024w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-5-300x112.jpeg 300w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-5-768x286.jpeg 768w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-5-1536x571.jpeg 1536w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-5-2048x761.jpeg 2048w\" sizes=\"auto, (max-width: 1024px) 100vw, 1024px\" \/><\/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\/brd79-protac-6.jpeg'><img loading=\"lazy\" decoding=\"async\" width=\"1024\" height=\"195\" src=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-6-1024x195.jpeg\" class=\"attachment-large size-large\" alt=\"Figure 3. Structures of compounds 7 and 21.\" srcset=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-6-1024x195.jpeg 1024w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-6-300x57.jpeg 300w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-6-768x147.jpeg 768w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-6-1536x293.jpeg 1536w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-6-2048x391.jpeg 2048w\" sizes=\"auto, (max-width: 1024px) 100vw, 1024px\" \/><\/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\/brd79-protac-7.jpeg'><img loading=\"lazy\" decoding=\"async\" width=\"1024\" height=\"950\" src=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-7-1024x950.jpeg\" class=\"attachment-large size-large\" alt=\"Figure 4. Ternary complex formation and analysis of binding mode for compound 5.\" srcset=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-7-1024x950.jpeg 1024w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-7-300x278.jpeg 300w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-7-768x712.jpeg 768w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-7-1536x1425.jpeg 1536w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-7.jpeg 1684w\" sizes=\"auto, (max-width: 1024px) 100vw, 1024px\" \/><\/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\/brd79-protac-8.jpeg'><img loading=\"lazy\" decoding=\"async\" width=\"1024\" height=\"277\" src=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-8-1024x277.jpeg\" class=\"attachment-large size-large\" alt=\"Scheme 3. Synthesis of Compound 23\" srcset=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-8-1024x277.jpeg 1024w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-8-300x81.jpeg 300w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-8-768x208.jpeg 768w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-8-1536x416.jpeg 1536w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-8-2048x554.jpeg 2048w\" sizes=\"auto, (max-width: 1024px) 100vw, 1024px\" \/><\/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\/brd79-protac-9.jpeg'><img loading=\"lazy\" decoding=\"async\" width=\"1024\" height=\"644\" src=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-9-1024x644.jpeg\" class=\"attachment-large size-large\" alt=\"Scheme 4. Synthesis of Compounds 26\u201331\" srcset=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-9-1024x644.jpeg 1024w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-9-300x189.jpeg 300w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-9-768x483.jpeg 768w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-9-1536x967.jpeg 1536w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-9-2048x1289.jpeg 2048w\" sizes=\"auto, (max-width: 1024px) 100vw, 1024px\" \/><\/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\/brd79-protac-10.jpeg'><img loading=\"lazy\" decoding=\"async\" width=\"1024\" height=\"628\" src=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-10-1024x628.jpeg\" class=\"attachment-large size-large\" alt=\"Figure 5. Compound 26 induces rapid and profound depletion of BRD9 in cells\" srcset=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-10-1024x628.jpeg 1024w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-10-300x184.jpeg 300w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-10-768x471.jpeg 768w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-10-1536x942.jpeg 1536w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-10.jpeg 1754w\" sizes=\"auto, (max-width: 1024px) 100vw, 1024px\" \/><\/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\/brd79-protac-11.jpeg'><img loading=\"lazy\" decoding=\"async\" width=\"1024\" height=\"730\" src=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-11-1024x730.jpeg\" class=\"attachment-large size-large\" alt=\"Figure 6. Improved ternary complex formation by series-2 degraders.\" srcset=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-11-1024x730.jpeg 1024w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-11-300x214.jpeg 300w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-11-768x548.jpeg 768w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-11.jpeg 1275w\" sizes=\"auto, (max-width: 1024px) 100vw, 1024px\" \/><\/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\/brd79-protac-12.jpeg'><img loading=\"lazy\" decoding=\"async\" width=\"864\" height=\"1024\" src=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-12-864x1024.jpeg\" class=\"attachment-large size-large\" alt=\"Scheme 5. General Synthetic Routes for Third-Generation Compounds\" srcset=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-12-864x1024.jpeg 864w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-12-253x300.jpeg 253w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-12-768x911.jpeg 768w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-12-1295x1536.jpeg 1295w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-12-1727x2048.jpeg 1727w\" sizes=\"auto, (max-width: 864px) 100vw, 864px\" \/><\/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\/brd79-protac-13.jpg'><img loading=\"lazy\" decoding=\"async\" width=\"661\" height=\"1024\" src=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-13-661x1024.jpg\" class=\"attachment-large size-large\" alt=\"Figure 7. Screening of third generation of degraders\" srcset=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-13-661x1024.jpg 661w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-13-194x300.jpg 194w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-13-768x1190.jpg 768w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-13-992x1536.jpg 992w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-13-1322x2048.jpg 1322w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-13.jpg 1920w\" sizes=\"auto, (max-width: 661px) 100vw, 661px\" \/><\/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\/brd79-protac-14.jpeg'><img loading=\"lazy\" decoding=\"async\" width=\"1024\" height=\"705\" src=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-14-1024x705.jpeg\" class=\"attachment-large size-large\" alt=\"Figure 8. VZ185 induces strong and rapid degradation in a time- and dose-dependent manner.\" srcset=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-14-1024x705.jpeg 1024w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-14-300x207.jpeg 300w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-14-768x529.jpeg 768w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-14-1536x1058.jpeg 1536w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-14.jpeg 1767w\" sizes=\"auto, (max-width: 1024px) 100vw, 1024px\" \/><\/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\/brd79-protac-15.jpeg'><img loading=\"lazy\" decoding=\"async\" width=\"1024\" height=\"582\" src=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-15-1024x582.jpeg\" class=\"attachment-large size-large\" alt=\"Figure 9. Quantitative live-cell kinetics of VZ185 induced degradation of BRD7 and BRD9\" srcset=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-15-1024x582.jpeg 1024w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-15-300x171.jpeg 300w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-15-768x437.jpeg 768w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-15.jpeg 1360w\" sizes=\"auto, (max-width: 1024px) 100vw, 1024px\" \/><\/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\/brd79-protac-16.jpeg'><img loading=\"lazy\" decoding=\"async\" width=\"1024\" height=\"258\" src=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-16-1024x258.jpeg\" class=\"attachment-large size-large\" alt=\"Figure 9. Quantitative live-cell kinetics of VZ185 induced degradation of BRD7 and BRD9\" srcset=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-16-1024x258.jpeg 1024w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-16-300x75.jpeg 300w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-16-768x193.jpeg 768w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-16.jpeg 1510w\" sizes=\"auto, (max-width: 1024px) 100vw, 1024px\" \/><\/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\/brd79-protac-17.jpeg'><img loading=\"lazy\" decoding=\"async\" width=\"1024\" height=\"456\" src=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-17-1024x456.jpeg\" class=\"attachment-large size-large\" alt=\"Figure 11. Effect of BRD7\/9 degradation on viability of BRD9-sensitive cancer cell lines.\" srcset=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-17-1024x456.jpeg 1024w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-17-300x134.jpeg 300w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-17-768x342.jpeg 768w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-17-1536x685.jpeg 1536w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-17.jpeg 1889w\" sizes=\"auto, (max-width: 1024px) 100vw, 1024px\" \/><\/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\/brd79-protac-18.jpeg'><img loading=\"lazy\" decoding=\"async\" width=\"1000\" height=\"613\" src=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-18.jpeg\" class=\"attachment-large size-large\" alt=\"Figure 12. Impact of VZ185 on the cellular proteome after treatment of RI-1 cells with 100 nM compound for 4 h before harvesting.\" srcset=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-18.jpeg 1000w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-18-300x184.jpeg 300w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/brd79-protac-18-768x471.jpeg 768w\" sizes=\"auto, (max-width: 1000px) 100vw, 1000px\" \/><\/a>\n\t\t\t<\/div><\/figure>\n\t\t<\/div>\n\n","protected":false},"excerpt":{"rendered":"<p>Our SAR story disclosing dual Brd7\/9 PROTAC degrader VZ185 is published in J. Med. Chem. Congratulations to\u00a0Vittoria,\u00a0Scott,\u00a0Chiara\u00a0and\u00a0Andrea, and all our collaborators for their contributions to this work! Related Links Promega Connections blog: \u201cA Roadmap for PROTAC Development\u201d<\/p>\n","protected":false},"author":1,"featured_media":0,"comment_status":"open","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[18,4],"tags":[],"class_list":["post-2454","post","type-post","status-publish","format-standard","hentry","category-18","category-news"],"blocksy_meta":[],"_links":{"self":[{"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/posts\/2454","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=2454"}],"version-history":[{"count":2,"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/posts\/2454\/revisions"}],"predecessor-version":[{"id":4867,"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/posts\/2454\/revisions\/4867"}],"wp:attachment":[{"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/media?parent=2454"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/categories?post=2454"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/tags?post=2454"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}