{"id":2872,"date":"2013-12-04T16:51:00","date_gmt":"2013-12-04T16:51:00","guid":{"rendered":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/?p=2872"},"modified":"2026-01-26T17:02:07","modified_gmt":"2026-01-26T17:02:07","slug":"targeting-the-low-druggability-baz2b-bromodomain-using-fragment-based-drug-design","status":"publish","type":"post","link":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/2013\/12\/04\/targeting-the-low-druggability-baz2b-bromodomain-using-fragment-based-drug-design\/","title":{"rendered":"Targeting the low-druggability BAZ2B bromodomain using fragment-based drug design"},"content":{"rendered":"\n<p>Our paper targeting the low-druggability BAZ2B bromodomain using fragment-based drug design is now published in J. Med. Chem.<\/p>\n\n\n\n<p><a href=\"http:\/\/dx.doi.org\/10.1021\/jm401582c\">You can read our paper open-access<\/a>.<\/p>\n\n\n\n<figure class=\"wp-block-gallery has-nested-images columns-4 is-cropped brgr gallery wp-block-gallery-1 is-layout-flex wp-block-gallery-is-layout-flex\">\n<figure class=\"wp-block-image size-full\"><img loading=\"lazy\" decoding=\"async\" width=\"467\" height=\"500\" data-id=\"2873\" src=\"https:\/\/sites.dundee.ac.uk\/wp-content\/uploads\/sites\/233\/2024\/01\/targeting-low-druggability-baz2b-jm-2013-01582c_0003.jpg\" alt=\"Table 1. Structures, IC50 Values Determined by AlphaScreen, and Ligand Efficiencies of Validated Fragment Hits\" class=\"wp-image-2873\" srcset=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/targeting-low-druggability-baz2b-jm-2013-01582c_0003.jpg 467w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/targeting-low-druggability-baz2b-jm-2013-01582c_0003-280x300.jpg 280w\" sizes=\"auto, (max-width: 467px) 100vw, 467px\" \/><figcaption class=\"wp-element-caption\">Table 1. Structures, IC50 Values Determined by AlphaScreen, and Ligand Efficiencies of Validated Fragment Hits<\/figcaption><\/figure>\n\n\n\n<figure class=\"wp-block-image size-full\"><img loading=\"lazy\" decoding=\"async\" width=\"455\" height=\"458\" data-id=\"2874\" src=\"https:\/\/sites.dundee.ac.uk\/wp-content\/uploads\/sites\/233\/2024\/01\/targeting-low-druggability-baz2b-4-jm-2013-01582c_0002.jpeg\" alt=\"Figure 2. Overlay of the crystal structures of fragments 3 (shown pink) and 6 (shown cyan) illustrates the rationale for fragment merging\" class=\"wp-image-2874\" srcset=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/targeting-low-druggability-baz2b-4-jm-2013-01582c_0002.jpeg 455w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/targeting-low-druggability-baz2b-4-jm-2013-01582c_0002-298x300.jpeg 298w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/targeting-low-druggability-baz2b-4-jm-2013-01582c_0002-150x150.jpeg 150w\" sizes=\"auto, (max-width: 455px) 100vw, 455px\" \/><figcaption class=\"wp-element-caption\">Figure 2. Overlay of the crystal structures of fragments 3 (shown pink) and 6 (shown cyan) illustrates the rationale for fragment merging<\/figcaption><\/figure>\n\n\n\n<figure class=\"wp-block-image size-full\"><img loading=\"lazy\" decoding=\"async\" width=\"2050\" height=\"618\" data-id=\"2875\" src=\"https:\/\/sites.dundee.ac.uk\/wp-content\/uploads\/sites\/233\/2024\/01\/targeting-low-druggability-baz2b-jm-2013-01582c_0001_fig2.jpeg\" alt=\"Figure 1. Crystal Structures of the BAZ2B bromodomain in complex with (a) acetyllysine PDB 4NR9, (b) 1 PDB 4NRB, (c) 3 PDB 4NRC, and (d) 6 PDB 4NRA\" class=\"wp-image-2875\" srcset=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/targeting-low-druggability-baz2b-jm-2013-01582c_0001_fig2.jpeg 2050w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/targeting-low-druggability-baz2b-jm-2013-01582c_0001_fig2-300x90.jpeg 300w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/targeting-low-druggability-baz2b-jm-2013-01582c_0001_fig2-1024x309.jpeg 1024w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/targeting-low-druggability-baz2b-jm-2013-01582c_0001_fig2-768x232.jpeg 768w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/targeting-low-druggability-baz2b-jm-2013-01582c_0001_fig2-1536x463.jpeg 1536w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/targeting-low-druggability-baz2b-jm-2013-01582c_0001_fig2-2048x617.jpeg 2048w\" sizes=\"auto, (max-width: 2050px) 100vw, 2050px\" \/><figcaption class=\"wp-element-caption\">Figure 1. Crystal Structures of the BAZ2B bromodomain in complex with (a) acetyllysine PDB 4NR9, (b) 1 PDB 4NRB, (c) 3 PDB 4NRC, and (d) 6 PDB 4NRA<\/figcaption><\/figure>\n\n\n\n<figure class=\"wp-block-image size-full\"><img loading=\"lazy\" decoding=\"async\" width=\"1280\" height=\"1180\" data-id=\"2876\" src=\"https:\/\/sites.dundee.ac.uk\/wp-content\/uploads\/sites\/233\/2024\/01\/targeting-low-druggability-baz2b-toc_0.png\" alt=\"Table of content graphic for targeting low drugability\" class=\"wp-image-2876\" srcset=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/targeting-low-druggability-baz2b-toc_0.png 1280w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/targeting-low-druggability-baz2b-toc_0-300x277.png 300w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/targeting-low-druggability-baz2b-toc_0-1024x944.png 1024w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/targeting-low-druggability-baz2b-toc_0-768x708.png 768w\" sizes=\"auto, (max-width: 1280px) 100vw, 1280px\" \/><figcaption class=\"wp-element-caption\">Table of content graphic for targeting low drugability<\/figcaption><\/figure>\n<\/figure>\n","protected":false},"excerpt":{"rendered":"<p>Our paper targeting the low-druggability BAZ2B bromodomain using fragment-based drug design is now published in J. Med. Chem. You can read our paper open-access.<\/p>\n","protected":false},"author":1,"featured_media":0,"comment_status":"open","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[16,4],"tags":[],"class_list":["post-2872","post","type-post","status-publish","format-standard","hentry","category-16","category-news"],"blocksy_meta":[],"_links":{"self":[{"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/posts\/2872","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=2872"}],"version-history":[{"count":3,"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/posts\/2872\/revisions"}],"predecessor-version":[{"id":4903,"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/posts\/2872\/revisions\/4903"}],"wp:attachment":[{"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/media?parent=2872"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/categories?post=2872"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/tags?post=2872"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}