{"id":2620,"date":"2016-07-13T10:05:00","date_gmt":"2016-07-13T09:05:00","guid":{"rendered":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/?p=2620"},"modified":"2026-01-26T16:28:05","modified_gmt":"2026-01-26T16:28:05","slug":"advanced-chemical-genetics-for-epigenetics","status":"publish","type":"post","link":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/2016\/07\/13\/advanced-chemical-genetics-for-epigenetics\/","title":{"rendered":"Advanced chemical genetics for epigenetics"},"content":{"rendered":"<p>Our review on advanced chemical genetics for epigenetics is now published in Current Opinion in Chemical Biology!<\/p>\n<p>Well done Andrew, Kwok-Ho and Michael!<\/p>\n<p><a href=\"http:\/\/dx.doi.org\/10.1016\/j.cbpa.2016.06.031\">Read our review open access<\/a>.<\/p>\n<h2 class=\"wp-block-heading\"><strong>Review synopsis<\/strong><\/h2>\n<p>\u00a0In conventional chemical genetics, cell-active small-molecules directly block protein activity, altering phenotype. However these molecules may not be sufficiently selective or effective at modulating complex epigenetic pathways. By mutating the target protein, and creating a mutant-selective inhibitor, the bump-and-hole approach can provide single-target selectivity. PROTAC molecules direct their target to proteosomal degradation by recruiting an E3 ubiquitin ligase, resulting in more efficacious target downregulation.<\/p>\n<div id='gallery-1' class='gallery galleryid-2620 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\/advanced-chemical-genetics-epigenetics-Abstract-V3.png'><img loading=\"lazy\" decoding=\"async\" width=\"1024\" height=\"391\" src=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/advanced-chemical-genetics-epigenetics-Abstract-V3-1024x391.png\" class=\"attachment-large size-large\" alt=\"Graphical abstract for\" srcset=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/advanced-chemical-genetics-epigenetics-Abstract-V3-1024x391.png 1024w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/advanced-chemical-genetics-epigenetics-Abstract-V3-300x115.png 300w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/advanced-chemical-genetics-epigenetics-Abstract-V3-768x293.png 768w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/advanced-chemical-genetics-epigenetics-Abstract-V3.png 1527w\" 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\/advanced-chemical-genetics-epigenetics-fig1.png'><img loading=\"lazy\" decoding=\"async\" width=\"701\" height=\"1024\" src=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/advanced-chemical-genetics-epigenetics-fig1-701x1024.png\" class=\"attachment-large size-large\" alt=\"Figure 1. Chemical genetics, and its use in epigenetics\" srcset=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/advanced-chemical-genetics-epigenetics-fig1-701x1024.png 701w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/advanced-chemical-genetics-epigenetics-fig1-205x300.png 205w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/advanced-chemical-genetics-epigenetics-fig1-768x1122.png 768w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/advanced-chemical-genetics-epigenetics-fig1-1051x1536.png 1051w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/advanced-chemical-genetics-epigenetics-fig1-1402x2048.png 1402w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/advanced-chemical-genetics-epigenetics-fig1.png 1607w\" sizes=\"auto, (max-width: 701px) 100vw, 701px\" \/><\/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\/advanced-chemical-genetics-epigenetics-chemical-tools.png'><img loading=\"lazy\" decoding=\"async\" width=\"601\" height=\"1024\" src=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/advanced-chemical-genetics-epigenetics-chemical-tools-601x1024.png\" class=\"attachment-large size-large\" alt=\"Figure 2. Chemical probes as chemical tools.\" srcset=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/advanced-chemical-genetics-epigenetics-chemical-tools-601x1024.png 601w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/advanced-chemical-genetics-epigenetics-chemical-tools-176x300.png 176w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/advanced-chemical-genetics-epigenetics-chemical-tools-768x1309.png 768w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/advanced-chemical-genetics-epigenetics-chemical-tools-902x1536.png 902w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/advanced-chemical-genetics-epigenetics-chemical-tools.png 1050w\" sizes=\"auto, (max-width: 601px) 100vw, 601px\" \/><\/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\/advanced-chemical-genetics-epigenetics-BaH-V2.png'><img loading=\"lazy\" decoding=\"async\" width=\"718\" height=\"1024\" src=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/advanced-chemical-genetics-epigenetics-BaH-V2-718x1024.png\" class=\"attachment-large size-large\" alt=\"Figure 3. Selective target inhibition via bump-and-hole\" srcset=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/advanced-chemical-genetics-epigenetics-BaH-V2-718x1024.png 718w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/advanced-chemical-genetics-epigenetics-BaH-V2-210x300.png 210w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/advanced-chemical-genetics-epigenetics-BaH-V2-768x1096.png 768w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/advanced-chemical-genetics-epigenetics-BaH-V2-1076x1536.png 1076w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/advanced-chemical-genetics-epigenetics-BaH-V2-1435x2048.png 1435w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/advanced-chemical-genetics-epigenetics-BaH-V2.png 1621w\" sizes=\"auto, (max-width: 718px) 100vw, 718px\" \/><\/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\/advanced-chemical-genetics-epigenetics-PROTAC-V2-CS5-copy_ac_kc.png'><img loading=\"lazy\" decoding=\"async\" width=\"679\" height=\"1024\" src=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/advanced-chemical-genetics-epigenetics-PROTAC-V2-CS5-copy_ac_kc-679x1024.png\" class=\"attachment-large size-large\" alt=\"Figure 4. Chemically induced protein degradation via PROTAC\" srcset=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/advanced-chemical-genetics-epigenetics-PROTAC-V2-CS5-copy_ac_kc-679x1024.png 679w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/advanced-chemical-genetics-epigenetics-PROTAC-V2-CS5-copy_ac_kc-199x300.png 199w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/advanced-chemical-genetics-epigenetics-PROTAC-V2-CS5-copy_ac_kc-768x1159.png 768w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/advanced-chemical-genetics-epigenetics-PROTAC-V2-CS5-copy_ac_kc-1018x1536.png 1018w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/advanced-chemical-genetics-epigenetics-PROTAC-V2-CS5-copy_ac_kc-1358x2048.png 1358w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/advanced-chemical-genetics-epigenetics-PROTAC-V2-CS5-copy_ac_kc.png 1630w\" sizes=\"auto, (max-width: 679px) 100vw, 679px\" \/><\/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\/advanced-chemical-genetics-epigenetics-Publication_recognition.jpg'><img loading=\"lazy\" decoding=\"async\" width=\"1024\" height=\"724\" src=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/advanced-chemical-genetics-epigenetics-Publication_recognition-1024x724.jpg\" class=\"attachment-large size-large\" alt=\"Publication certificate for advanced chemical genetics for epigenetics\" srcset=\"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/advanced-chemical-genetics-epigenetics-Publication_recognition-1024x724.jpg 1024w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/advanced-chemical-genetics-epigenetics-Publication_recognition-300x212.jpg 300w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/advanced-chemical-genetics-epigenetics-Publication_recognition-768x543.jpg 768w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/advanced-chemical-genetics-epigenetics-Publication_recognition-1536x1085.jpg 1536w, https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-content\/uploads\/sites\/233\/2024\/01\/advanced-chemical-genetics-epigenetics-Publication_recognition-2048x1447.jpg 2048w\" sizes=\"auto, (max-width: 1024px) 100vw, 1024px\" \/><\/a>\n\t\t\t<\/div><\/figure>\n\t\t<\/div>\n\n","protected":false},"excerpt":{"rendered":"<p>Our review on advanced chemical genetics for epigenetics is now published in Current Opinion in Chemical Biology! Well done Andrew, Kwok-Ho and Michael! Read our review open access. Review synopsis \u00a0In conventional chemical genetics, cell-active small-molecules directly block protein activity, altering phenotype. However these molecules may not be sufficiently selective or effective at modulating complex [&hellip;]<\/p>\n","protected":false},"author":1,"featured_media":0,"comment_status":"open","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[20,4],"tags":[],"class_list":["post-2620","post","type-post","status-publish","format-standard","hentry","category-20","category-news"],"blocksy_meta":[],"_links":{"self":[{"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/posts\/2620","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=2620"}],"version-history":[{"count":2,"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/posts\/2620\/revisions"}],"predecessor-version":[{"id":4872,"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/posts\/2620\/revisions\/4872"}],"wp:attachment":[{"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/media?parent=2620"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/categories?post=2620"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/sites.dundee.ac.uk\/alessio-ciulli\/wp-json\/wp\/v2\/tags?post=2620"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}