{"id":322,"date":"2022-05-31T13:53:24","date_gmt":"2022-05-31T13:53:24","guid":{"rendered":"https:\/\/amm-journal.org\/?p=322"},"modified":"2022-05-31T13:53:24","modified_gmt":"2022-05-31T13:53:24","slug":"protac-degraders-with-ligands-recruiting-mdm2-e3-ubiquitin-ligase-an-updated-perspective","status":"publish","type":"post","link":"https:\/\/amm-journal.org\/index.php\/2022\/05\/31\/protac-degraders-with-ligands-recruiting-mdm2-e3-ubiquitin-ligase-an-updated-perspective\/","title":{"rendered":"PROTAC degraders with ligands recruiting MDM2 E3 ubiquitin ligase: an updated perspective"},"content":{"rendered":"

Announcing a new review article publication for Acta Materia Medica<\/em> journal. \u00a0Mouse double minute 2 (MDM2) is an oncogenic E3 ligase that effectively degrades the tumor suppressor p53. In the past two decades, many MDM2 inhibitors that disrupt MDM2-p53 binding have been discovered and developed. Given that MDM2 and p53 form an auto-regulatory loop, in which p53 undergoes targeted degradation as a substrate of MDM2, and p53 targets MDM2 for transcriptional upregulation, these MDM2 inhibitors have limited efficacy. After rapid\u00a0in vivo<\/em>\u00a0clearance of the MDM2 inhibitors, p53 is degraded by accumulated MDM2. Fortunately, proteolysis targeting chimeras (PROTACs), a novel therapeutic strategy, overcome the limitations of MDM2 inhibitors. Several MDM2 inhibitors developed in the past two decades have been used in PROTAC technology in two applications: 1) binding and targeting endogenous MDM2 for PROTAC-based degradation and 2) binding endogenous MDM2 as a PROTAC E3 ligand for PROTAC-based degradation of other oncogenic proteins.<\/p>\n

In this review, the authors summarize current progress in the discovery and development of MDM2-based PROTAC drugs, and discuss future perspectives and challenges in their application as effective treatments for human cancer.<\/p>\n

Article Reference:<\/strong> Xin Han, Wenyi Wei and Yi Sun. PROTAC degraders with ligands recruiting MDM2 E3 ubiquitin ligase: an updated perspective.\u00a0Acta Materia Medica.\u00a0<\/em>Vol. 1(2):244-259. DOI: 10.15212\/AMM-2022-0010<\/p>\n

https:\/\/www.scienceopen.com\/hosted-document?doi=10.15212\/AMM-2022-0010<\/a><\/p>\n

Keywords:<\/strong> MDM2, E3 ligase ligand, PROTAC, degradation, human cancer, drug discovery<\/p>\n

Acta Materia Medica<\/em> welcomes the submission of research articles, review articles, databases, mini reviews, commentaries, editorials, short communications, case report articles and study protocols.<\/p>\n

Submission Process<\/strong><\/p>\n

Submissions to Acta Materia Medica<\/em> are made using ScholarOne, the online submission and peer review system. Registration and access are available at https:\/\/mc04.manuscriptcentral.com\/ammed<\/a><\/p>\n

Queries about the journal can be sent to editorialoffice@amm-journal.org.<\/p>\n

Please visit https:\/\/amm-journal.org\/<\/a> to learn more about the journal.<\/p>\n

Editorial Board:<\/strong> https:\/\/amm-journal.org\/index.php\/editorial-board\/<\/a><\/p>\n

There are no author submission or article processing fees.<\/p>\n

Follow Acta Materia Medica <\/em><\/strong>on Twitter https:\/\/twitter.com\/AMM_journal<\/a>\u00a0 ; Facebook<\/a> (https:\/\/www.facebook.com\/AMMjournal<\/a>)<\/p>\n

eISSN <\/strong>2737-7946<\/p>\n","protected":false},"excerpt":{"rendered":"

Announcing a new review article publication for Acta Materia Medica journal. \u00a0Mouse double minute 2 (MDM2) is an oncogenic E3 ligase that effectively degrades the tumor suppressor p53. In the past two decades, many MDM2 inhibitors that disrupt MDM2-p53 binding have been discovered and developed. Given that MDM2 and p53 form an auto-regulatory loop, in […]<\/p>\n","protected":false},"author":1,"featured_media":0,"comment_status":"open","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[2],"tags":[63,65,62,64,61,13],"class_list":["post-322","post","type-post","status-publish","format-standard","hentry","category-news-and-events","tag-degradation","tag-drug-discovery","tag-e3-ligase-ligand","tag-human-cancer","tag-mdm2","tag-protac"],"yoast_head":"\nPROTAC degraders with ligands recruiting MDM2 E3 ubiquitin ligase: an updated perspective - AMM Journal<\/title>\n<meta name=\"robots\" content=\"index, follow, max-snippet:-1, max-image-preview:large, max-video-preview:-1\" \/>\n<link rel=\"canonical\" href=\"https:\/\/amm-journal.org\/index.php\/2022\/05\/31\/protac-degraders-with-ligands-recruiting-mdm2-e3-ubiquitin-ligase-an-updated-perspective\/\" \/>\n<meta property=\"og:locale\" content=\"en_GB\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"PROTAC degraders with ligands recruiting MDM2 E3 ubiquitin ligase: an updated perspective - AMM Journal\" \/>\n<meta property=\"og:description\" content=\"Announcing a new review article publication for Acta Materia Medica journal. \u00a0Mouse double minute 2 (MDM2) is an oncogenic E3 ligase that effectively degrades the tumor suppressor p53. In the past two decades, many MDM2 inhibitors that disrupt MDM2-p53 binding have been discovered and developed. Given that MDM2 and p53 form an auto-regulatory loop, in […]\" \/>\n<meta property=\"og:url\" content=\"https:\/\/amm-journal.org\/index.php\/2022\/05\/31\/protac-degraders-with-ligands-recruiting-mdm2-e3-ubiquitin-ligase-an-updated-perspective\/\" \/>\n<meta property=\"og:site_name\" content=\"AMM Journal\" \/>\n<meta property=\"article:published_time\" content=\"2022-05-31T13:53:24+00:00\" \/>\n<meta name=\"author\" content=\"Compuscript\" \/>\n<meta name=\"twitter:card\" content=\"summary_large_image\" \/>\n<meta name=\"twitter:label1\" content=\"Written by\" \/>\n\t<meta name=\"twitter:data1\" content=\"Compuscript\" \/>\n\t<meta name=\"twitter:label2\" content=\"Estimated reading time\" \/>\n\t<meta name=\"twitter:data2\" content=\"2 minutes\" \/>\n<script type=\"application\/ld+json\" class=\"yoast-schema-graph\">{\"@context\":\"https:\\\/\\\/schema.org\",\"@graph\":[{\"@type\":\"Article\",\"@id\":\"https:\\\/\\\/amm-journal.org\\\/index.php\\\/2022\\\/05\\\/31\\\/protac-degraders-with-ligands-recruiting-mdm2-e3-ubiquitin-ligase-an-updated-perspective\\\/#article\",\"isPartOf\":{\"@id\":\"https:\\\/\\\/amm-journal.org\\\/index.php\\\/2022\\\/05\\\/31\\\/protac-degraders-with-ligands-recruiting-mdm2-e3-ubiquitin-ligase-an-updated-perspective\\\/\"},\"author\":{\"name\":\"Compuscript\",\"@id\":\"https:\\\/\\\/amm-journal.org\\\/#\\\/schema\\\/person\\\/0935dba5c919585e39f756ce09930a67\"},\"headline\":\"PROTAC degraders with ligands recruiting MDM2 E3 ubiquitin ligase: an updated perspective\",\"datePublished\":\"2022-05-31T13:53:24+00:00\",\"mainEntityOfPage\":{\"@id\":\"https:\\\/\\\/amm-journal.org\\\/index.php\\\/2022\\\/05\\\/31\\\/protac-degraders-with-ligands-recruiting-mdm2-e3-ubiquitin-ligase-an-updated-perspective\\\/\"},\"wordCount\":354,\"commentCount\":0,\"keywords\":[\"degradation\",\"drug discovery\",\"E3 ligase ligand\",\"human cancer\",\"MDM2\",\"PROTAC\"],\"articleSection\":[\"News and Events\"],\"inLanguage\":\"en-GB\",\"potentialAction\":[{\"@type\":\"CommentAction\",\"name\":\"Comment\",\"target\":[\"https:\\\/\\\/amm-journal.org\\\/index.php\\\/2022\\\/05\\\/31\\\/protac-degraders-with-ligands-recruiting-mdm2-e3-ubiquitin-ligase-an-updated-perspective\\\/#respond\"]}]},{\"@type\":\"WebPage\",\"@id\":\"https:\\\/\\\/amm-journal.org\\\/index.php\\\/2022\\\/05\\\/31\\\/protac-degraders-with-ligands-recruiting-mdm2-e3-ubiquitin-ligase-an-updated-perspective\\\/\",\"url\":\"https:\\\/\\\/amm-journal.org\\\/index.php\\\/2022\\\/05\\\/31\\\/protac-degraders-with-ligands-recruiting-mdm2-e3-ubiquitin-ligase-an-updated-perspective\\\/\",\"name\":\"PROTAC degraders with ligands recruiting MDM2 E3 ubiquitin ligase: an updated perspective - AMM Journal\",\"isPartOf\":{\"@id\":\"https:\\\/\\\/amm-journal.org\\\/#website\"},\"datePublished\":\"2022-05-31T13:53:24+00:00\",\"author\":{\"@id\":\"https:\\\/\\\/amm-journal.org\\\/#\\\/schema\\\/person\\\/0935dba5c919585e39f756ce09930a67\"},\"breadcrumb\":{\"@id\":\"https:\\\/\\\/amm-journal.org\\\/index.php\\\/2022\\\/05\\\/31\\\/protac-degraders-with-ligands-recruiting-mdm2-e3-ubiquitin-ligase-an-updated-perspective\\\/#breadcrumb\"},\"inLanguage\":\"en-GB\",\"potentialAction\":[{\"@type\":\"ReadAction\",\"target\":[\"https:\\\/\\\/amm-journal.org\\\/index.php\\\/2022\\\/05\\\/31\\\/protac-degraders-with-ligands-recruiting-mdm2-e3-ubiquitin-ligase-an-updated-perspective\\\/\"]}]},{\"@type\":\"BreadcrumbList\",\"@id\":\"https:\\\/\\\/amm-journal.org\\\/index.php\\\/2022\\\/05\\\/31\\\/protac-degraders-with-ligands-recruiting-mdm2-e3-ubiquitin-ligase-an-updated-perspective\\\/#breadcrumb\",\"itemListElement\":[{\"@type\":\"ListItem\",\"position\":1,\"name\":\"Home\",\"item\":\"https:\\\/\\\/amm-journal.org\\\/\"},{\"@type\":\"ListItem\",\"position\":2,\"name\":\"PROTAC degraders with ligands recruiting MDM2 E3 ubiquitin ligase: an updated perspective\"}]},{\"@type\":\"WebSite\",\"@id\":\"https:\\\/\\\/amm-journal.org\\\/#website\",\"url\":\"https:\\\/\\\/amm-journal.org\\\/\",\"name\":\"AMM Journal\",\"description\":\"\",\"potentialAction\":[{\"@type\":\"SearchAction\",\"target\":{\"@type\":\"EntryPoint\",\"urlTemplate\":\"https:\\\/\\\/amm-journal.org\\\/?s={search_term_string}\"},\"query-input\":{\"@type\":\"PropertyValueSpecification\",\"valueRequired\":true,\"valueName\":\"search_term_string\"}}],\"inLanguage\":\"en-GB\"},{\"@type\":\"Person\",\"@id\":\"https:\\\/\\\/amm-journal.org\\\/#\\\/schema\\\/person\\\/0935dba5c919585e39f756ce09930a67\",\"name\":\"Compuscript\",\"image\":{\"@type\":\"ImageObject\",\"inLanguage\":\"en-GB\",\"@id\":\"https:\\\/\\\/secure.gravatar.com\\\/avatar\\\/fb3d42af3c1b48f4d76adf5524c6c3447a369d2a7bcb666ef995240441912a6b?s=96&d=mm&r=g\",\"url\":\"https:\\\/\\\/secure.gravatar.com\\\/avatar\\\/fb3d42af3c1b48f4d76adf5524c6c3447a369d2a7bcb666ef995240441912a6b?s=96&d=mm&r=g\",\"contentUrl\":\"https:\\\/\\\/secure.gravatar.com\\\/avatar\\\/fb3d42af3c1b48f4d76adf5524c6c3447a369d2a7bcb666ef995240441912a6b?s=96&d=mm&r=g\",\"caption\":\"Compuscript\"},\"sameAs\":[\"https:\\\/\\\/amm-journal.org\"],\"url\":\"https:\\\/\\\/amm-journal.org\\\/index.php\\\/author\\\/ammjadmin\\\/\"}]}<\/script>\n<!-- \/ Yoast SEO plugin. -->","yoast_head_json":{"title":"PROTAC degraders with ligands recruiting MDM2 E3 ubiquitin ligase: an updated perspective - AMM Journal","robots":{"index":"index","follow":"follow","max-snippet":"max-snippet:-1","max-image-preview":"max-image-preview:large","max-video-preview":"max-video-preview:-1"},"canonical":"https:\/\/amm-journal.org\/index.php\/2022\/05\/31\/protac-degraders-with-ligands-recruiting-mdm2-e3-ubiquitin-ligase-an-updated-perspective\/","og_locale":"en_GB","og_type":"article","og_title":"PROTAC degraders with ligands recruiting MDM2 E3 ubiquitin ligase: an updated perspective - AMM Journal","og_description":"Announcing a new review article publication for Acta Materia Medica journal. \u00a0Mouse double minute 2 (MDM2) is an oncogenic E3 ligase that effectively degrades the tumor suppressor p53. In the past two decades, many MDM2 inhibitors that disrupt MDM2-p53 binding have been discovered and developed. Given that MDM2 and p53 form an auto-regulatory loop, in […]","og_url":"https:\/\/amm-journal.org\/index.php\/2022\/05\/31\/protac-degraders-with-ligands-recruiting-mdm2-e3-ubiquitin-ligase-an-updated-perspective\/","og_site_name":"AMM Journal","article_published_time":"2022-05-31T13:53:24+00:00","author":"Compuscript","twitter_card":"summary_large_image","twitter_misc":{"Written by":"Compuscript","Estimated reading time":"2 minutes"},"schema":{"@context":"https:\/\/schema.org","@graph":[{"@type":"Article","@id":"https:\/\/amm-journal.org\/index.php\/2022\/05\/31\/protac-degraders-with-ligands-recruiting-mdm2-e3-ubiquitin-ligase-an-updated-perspective\/#article","isPartOf":{"@id":"https:\/\/amm-journal.org\/index.php\/2022\/05\/31\/protac-degraders-with-ligands-recruiting-mdm2-e3-ubiquitin-ligase-an-updated-perspective\/"},"author":{"name":"Compuscript","@id":"https:\/\/amm-journal.org\/#\/schema\/person\/0935dba5c919585e39f756ce09930a67"},"headline":"PROTAC degraders with ligands recruiting MDM2 E3 ubiquitin ligase: an updated perspective","datePublished":"2022-05-31T13:53:24+00:00","mainEntityOfPage":{"@id":"https:\/\/amm-journal.org\/index.php\/2022\/05\/31\/protac-degraders-with-ligands-recruiting-mdm2-e3-ubiquitin-ligase-an-updated-perspective\/"},"wordCount":354,"commentCount":0,"keywords":["degradation","drug discovery","E3 ligase ligand","human cancer","MDM2","PROTAC"],"articleSection":["News and Events"],"inLanguage":"en-GB","potentialAction":[{"@type":"CommentAction","name":"Comment","target":["https:\/\/amm-journal.org\/index.php\/2022\/05\/31\/protac-degraders-with-ligands-recruiting-mdm2-e3-ubiquitin-ligase-an-updated-perspective\/#respond"]}]},{"@type":"WebPage","@id":"https:\/\/amm-journal.org\/index.php\/2022\/05\/31\/protac-degraders-with-ligands-recruiting-mdm2-e3-ubiquitin-ligase-an-updated-perspective\/","url":"https:\/\/amm-journal.org\/index.php\/2022\/05\/31\/protac-degraders-with-ligands-recruiting-mdm2-e3-ubiquitin-ligase-an-updated-perspective\/","name":"PROTAC degraders with ligands recruiting MDM2 E3 ubiquitin ligase: an updated perspective - AMM Journal","isPartOf":{"@id":"https:\/\/amm-journal.org\/#website"},"datePublished":"2022-05-31T13:53:24+00:00","author":{"@id":"https:\/\/amm-journal.org\/#\/schema\/person\/0935dba5c919585e39f756ce09930a67"},"breadcrumb":{"@id":"https:\/\/amm-journal.org\/index.php\/2022\/05\/31\/protac-degraders-with-ligands-recruiting-mdm2-e3-ubiquitin-ligase-an-updated-perspective\/#breadcrumb"},"inLanguage":"en-GB","potentialAction":[{"@type":"ReadAction","target":["https:\/\/amm-journal.org\/index.php\/2022\/05\/31\/protac-degraders-with-ligands-recruiting-mdm2-e3-ubiquitin-ligase-an-updated-perspective\/"]}]},{"@type":"BreadcrumbList","@id":"https:\/\/amm-journal.org\/index.php\/2022\/05\/31\/protac-degraders-with-ligands-recruiting-mdm2-e3-ubiquitin-ligase-an-updated-perspective\/#breadcrumb","itemListElement":[{"@type":"ListItem","position":1,"name":"Home","item":"https:\/\/amm-journal.org\/"},{"@type":"ListItem","position":2,"name":"PROTAC degraders with ligands recruiting MDM2 E3 ubiquitin ligase: an updated perspective"}]},{"@type":"WebSite","@id":"https:\/\/amm-journal.org\/#website","url":"https:\/\/amm-journal.org\/","name":"AMM Journal","description":"","potentialAction":[{"@type":"SearchAction","target":{"@type":"EntryPoint","urlTemplate":"https:\/\/amm-journal.org\/?s={search_term_string}"},"query-input":{"@type":"PropertyValueSpecification","valueRequired":true,"valueName":"search_term_string"}}],"inLanguage":"en-GB"},{"@type":"Person","@id":"https:\/\/amm-journal.org\/#\/schema\/person\/0935dba5c919585e39f756ce09930a67","name":"Compuscript","image":{"@type":"ImageObject","inLanguage":"en-GB","@id":"https:\/\/secure.gravatar.com\/avatar\/fb3d42af3c1b48f4d76adf5524c6c3447a369d2a7bcb666ef995240441912a6b?s=96&d=mm&r=g","url":"https:\/\/secure.gravatar.com\/avatar\/fb3d42af3c1b48f4d76adf5524c6c3447a369d2a7bcb666ef995240441912a6b?s=96&d=mm&r=g","contentUrl":"https:\/\/secure.gravatar.com\/avatar\/fb3d42af3c1b48f4d76adf5524c6c3447a369d2a7bcb666ef995240441912a6b?s=96&d=mm&r=g","caption":"Compuscript"},"sameAs":["https:\/\/amm-journal.org"],"url":"https:\/\/amm-journal.org\/index.php\/author\/ammjadmin\/"}]}},"_links":{"self":[{"href":"https:\/\/amm-journal.org\/index.php\/wp-json\/wp\/v2\/posts\/322","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/amm-journal.org\/index.php\/wp-json\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/amm-journal.org\/index.php\/wp-json\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/amm-journal.org\/index.php\/wp-json\/wp\/v2\/users\/1"}],"replies":[{"embeddable":true,"href":"https:\/\/amm-journal.org\/index.php\/wp-json\/wp\/v2\/comments?post=322"}],"version-history":[{"count":1,"href":"https:\/\/amm-journal.org\/index.php\/wp-json\/wp\/v2\/posts\/322\/revisions"}],"predecessor-version":[{"id":323,"href":"https:\/\/amm-journal.org\/index.php\/wp-json\/wp\/v2\/posts\/322\/revisions\/323"}],"wp:attachment":[{"href":"https:\/\/amm-journal.org\/index.php\/wp-json\/wp\/v2\/media?parent=322"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/amm-journal.org\/index.php\/wp-json\/wp\/v2\/categories?post=322"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/amm-journal.org\/index.php\/wp-json\/wp\/v2\/tags?post=322"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}