{"id":2318,"date":"2020-07-30T11:01:00","date_gmt":"2020-07-30T10:01:00","guid":{"rendered":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/?p=2318"},"modified":"2026-01-26T16:28:03","modified_gmt":"2026-01-26T16:28:03","slug":"our-review-on-probing-epigenetic-reader-domains-with-chemical-biology","status":"publish","type":"post","link":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/2020\/07\/30\/our-review-on-probing-epigenetic-reader-domains-with-chemical-biology\/","title":{"rendered":"Our review on probing epigenetic reader domains with chemical biology"},"content":{"rendered":"<p>Our review on probing epigenetic reader domains with chemical biology is now published in Current Opinion in Chemical Biology<br \/>for website.<\/p>\n<p>Congratulations to Alessandra Cipriano, well done!\u00a0Alessandra\u00a0was a visiting PhD student with us, from Gianluca Sbardella\u2019s group at the University of Salerno<\/p>\n<p><a href=\"https:\/\/doi.org\/10.1016\/j.cbpa.2020.05.006\">Read the article<\/a>.<\/p>\n<p><strong>Authors<\/strong>: Alessandra Cipriano, Gianluca Sbardella* and Alessio Ciulli*<\/p>\n<p><strong>Title<\/strong>: Targeting epigenetic reader domains by chemical biology<\/p>\n<h2 class=\"wp-block-heading\"><strong>Abstract<\/strong><\/h2>\n<p>Over the past years, growing interest toward post-translational modifications (PTMs) of histones and nonhistone proteins has prompted academia and industrial research groups to develop different approaches to better understand the link between PTMs and pathological states. Selective recognition of PTMs is carried out by reader modules, which mediate the biological readout of epigenetic mechanisms. Progress in medicinal chemistry and chemical biology has contributed to corroborate the role of reader domains in chromatin-binding proteins as potential therapeutic targets. Here, we review the state-of-the-art of the most important small molecules developed to date, with a particular attention on contemporary chemical biology approaches, including photoaffinity probes, cyclic peptides, bifunctional inhibitors, and PROTAC degraders.<\/p>\n<div id='gallery-1' class='gallery galleryid-2318 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\/current-opinion-chemical-biology-for-website.png'><img loading=\"lazy\" decoding=\"async\" width=\"1024\" height=\"707\" src=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/current-opinion-chemical-biology-for-website-1024x707.png\" class=\"attachment-large size-large\" alt=\"Copy of article for Current opinion in Chemical biology\" srcset=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/current-opinion-chemical-biology-for-website-1024x707.png 1024w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/current-opinion-chemical-biology-for-website-300x207.png 300w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/current-opinion-chemical-biology-for-website-768x531.png 768w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/current-opinion-chemical-biology-for-website.png 1213w\" 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\/current-opinion-chemical-biology-Fig1_0.jpg'><img loading=\"lazy\" decoding=\"async\" width=\"1024\" height=\"847\" src=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/current-opinion-chemical-biology-Fig1_0-1024x847.jpg\" class=\"attachment-large size-large\" alt=\"Figure 1. Structural architecture of reader domains\" srcset=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/current-opinion-chemical-biology-Fig1_0-1024x847.jpg 1024w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/current-opinion-chemical-biology-Fig1_0-300x248.jpg 300w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/current-opinion-chemical-biology-Fig1_0-768x636.jpg 768w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/current-opinion-chemical-biology-Fig1_0-1536x1271.jpg 1536w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/current-opinion-chemical-biology-Fig1_0-2048x1695.jpg 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 portrait'>\n\t\t\t\t<a href='https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/current-opinion-chemical-biology-Fig2_0.jpg'><img loading=\"lazy\" decoding=\"async\" width=\"807\" height=\"1024\" src=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/current-opinion-chemical-biology-Fig2_0-807x1024.jpg\" class=\"attachment-large size-large\" alt=\"Figure 2. Photoaffinity probes and click chemistry approaches\" srcset=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/current-opinion-chemical-biology-Fig2_0-807x1024.jpg 807w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/current-opinion-chemical-biology-Fig2_0-236x300.jpg 236w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/current-opinion-chemical-biology-Fig2_0-768x975.jpg 768w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/current-opinion-chemical-biology-Fig2_0-1210x1536.jpg 1210w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/current-opinion-chemical-biology-Fig2_0-1613x2048.jpg 1613w\" sizes=\"auto, (max-width: 807px) 100vw, 807px\" \/><\/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\/current-opinion-chemical-biology-Fig3_0.jpg'><img loading=\"lazy\" decoding=\"async\" width=\"757\" height=\"1024\" src=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/current-opinion-chemical-biology-Fig3_0-757x1024.jpg\" class=\"attachment-large size-large\" alt=\"Figure 3. Fragment-based and peptide-based approaches\" srcset=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/current-opinion-chemical-biology-Fig3_0-757x1024.jpg 757w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/current-opinion-chemical-biology-Fig3_0-222x300.jpg 222w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/current-opinion-chemical-biology-Fig3_0-768x1038.jpg 768w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/current-opinion-chemical-biology-Fig3_0-1136x1536.jpg 1136w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/current-opinion-chemical-biology-Fig3_0-1515x2048.jpg 1515w\" sizes=\"auto, (max-width: 757px) 100vw, 757px\" \/><\/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\/current-opinion-chemical-biology-Fig4_0.jpg'><img loading=\"lazy\" decoding=\"async\" width=\"1024\" height=\"918\" src=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/current-opinion-chemical-biology-Fig4_0-1024x918.jpg\" class=\"attachment-large size-large\" alt=\"Figure 4. Bivalent ligands of epigenetic readers\" srcset=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/current-opinion-chemical-biology-Fig4_0-1024x918.jpg 1024w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/current-opinion-chemical-biology-Fig4_0-300x269.jpg 300w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/current-opinion-chemical-biology-Fig4_0-768x688.jpg 768w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/current-opinion-chemical-biology-Fig4_0-1536x1377.jpg 1536w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/current-opinion-chemical-biology-Fig4_0-2048x1836.jpg 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 portrait'>\n\t\t\t\t<a href='https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/current-opinion-chemical-biology-Fig5_0.jpg'><img loading=\"lazy\" decoding=\"async\" width=\"719\" height=\"1024\" src=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/current-opinion-chemical-biology-Fig5_0-719x1024.jpg\" class=\"attachment-large size-large\" alt=\"Figure 5. PROTAC degraders of epigenetic readers\" srcset=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/current-opinion-chemical-biology-Fig5_0-719x1024.jpg 719w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/current-opinion-chemical-biology-Fig5_0-211x300.jpg 211w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/current-opinion-chemical-biology-Fig5_0-768x1094.jpg 768w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/current-opinion-chemical-biology-Fig5_0-1078x1536.jpg 1078w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/current-opinion-chemical-biology-Fig5_0-1437x2048.jpg 1437w\" sizes=\"auto, (max-width: 719px) 100vw, 719px\" \/><\/a>\n\t\t\t<\/div><\/figure>\n\t\t<\/div>\n\n","protected":false},"excerpt":{"rendered":"<p>Our review on probing epigenetic reader domains with chemical biology is now published in Current Opinion in Chemical Biologyfor website. Congratulations to Alessandra Cipriano, well done!\u00a0Alessandra\u00a0was a visiting PhD student with us, from Gianluca Sbardella\u2019s group at the University of Salerno Read the article. Authors: Alessandra Cipriano, Gianluca Sbardella* and Alessio Ciulli* Title: Targeting epigenetic [&hellip;]<\/p>\n","protected":false},"author":1,"featured_media":0,"comment_status":"open","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[15,4],"tags":[],"class_list":["post-2318","post","type-post","status-publish","format-standard","hentry","category-15","category-news"],"blocksy_meta":[],"_links":{"self":[{"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/posts\/2318","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=2318"}],"version-history":[{"count":2,"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/posts\/2318\/revisions"}],"predecessor-version":[{"id":4854,"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/posts\/2318\/revisions\/4854"}],"wp:attachment":[{"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/media?parent=2318"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/categories?post=2318"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/tags?post=2318"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}