{"id":13435,"date":"2024-09-19T09:22:00","date_gmt":"2024-09-19T09:22:00","guid":{"rendered":"https:\/\/www.sygnaturediscovery.com\/?post_type=journal-paper&p=13435"},"modified":"2026-01-30T09:27:09","modified_gmt":"2026-01-30T09:27:09","slug":"to-homeostasis-and-beyond-recent-advances-in-the-medicinal-chemistry-of-heterobifunctional-derivatives","status":"publish","type":"journal-paper","link":"https:\/\/www.sygnaturediscovery.com\/fr\/journal-paper\/to-homeostasis-and-beyond-recent-advances-in-the-medicinal-chemistry-of-heterobifunctional-derivatives\/","title":{"rendered":"To homeostasis and beyond! Recent advances in the medicinal chemistry of heterobifunctional derivatives"},"content":{"rendered":"\n

Diana Castagna,\u00a0Benoit Gourdet,\u00a0Roland Hjerpe,\u00a0Philip MacFaul,\u00a0Andrew Novak,\u00a0Guillaume Revol,\u00a0Etienne Rochette,\u00a0Allan Jordan<\/strong><\/p>\n\n\n\n

Abstract<\/strong><\/p>\n\n\n\n

The field of induced proximity therapeutics has expanded dramatically over the past 3 years, and heterobifunctional derivatives continue to form a significant component of the activities in this field. Here, we review recent advances in the field from the perspective of the medicinal chemist, with a particular focus upon informative case studies, alongside a review of emerging topics such as Direct-To-Biology (D2B) methodology and utilities for heterobifunctional compounds beyond E3 ligase mediated degradation. We also include a critical evaluation of the latest thinking around the optimisation of physicochemical and pharmacokinetic attributes of these beyond Role of Five molecules, to deliver appropriate therapeutic exposure in vivo.<\/p>\n\n\n\n

Ref: Prog Med Chem 2024<\/a><\/p>\n\n\n\n

<\/p>\n","protected":false},"excerpt":{"rendered":"","protected":false},"featured_media":0,"template":"","category":[681,682,686,743],"resource_tag":[],"class_list":["post-13435","journal-paper","type-journal-paper","status-publish","hentry","category-bioscience","category-chemistry","category-modalities","category-tpd"],"acf":[],"yoast_head":"\nTo homeostasis and beyond! Recent advances in the medicinal chemistry of heterobifunctional derivatives - Sygnature<\/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:\/\/www.sygnaturediscovery.com\/fr\/journal-paper\/to-homeostasis-and-beyond-recent-advances-in-the-medicinal-chemistry-of-heterobifunctional-derivatives\/\" \/>\n<meta property=\"og:locale\" content=\"fr_CA\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"To homeostasis and beyond! Recent advances in the medicinal chemistry of heterobifunctional derivatives - Sygnature\" \/>\n<meta property=\"og:url\" content=\"https:\/\/www.sygnaturediscovery.com\/fr\/journal-paper\/to-homeostasis-and-beyond-recent-advances-in-the-medicinal-chemistry-of-heterobifunctional-derivatives\/\" \/>\n<meta property=\"og:site_name\" content=\"Sygnature\" \/>\n<meta property=\"article:modified_time\" content=\"2026-01-30T09:27:09+00:00\" \/>\n<meta property=\"og:image\" content=\"https:\/\/www.sygnaturediscovery.com\/wp-content\/uploads\/2026\/02\/sygnature-hit-to-lead-team-collaboration-scaled.webp\" \/>\n\t<meta property=\"og:image:width\" content=\"2560\" \/>\n\t<meta property=\"og:image:height\" content=\"1707\" \/>\n\t<meta property=\"og:image:type\" content=\"image\/webp\" \/>\n<meta name=\"twitter:card\" content=\"summary_large_image\" \/>\n<meta name=\"twitter:label1\" content=\"Estimation du temps de lecture\" \/>\n\t<meta name=\"twitter:data1\" content=\"1 minute\" \/>\n<script type=\"application\/ld+json\" class=\"yoast-schema-graph\">{\"@context\":\"https:\/\/schema.org\",\"@graph\":[{\"@type\":\"WebPage\",\"@id\":\"https:\/\/www.sygnaturediscovery.com\/fr\/journal-paper\/to-homeostasis-and-beyond-recent-advances-in-the-medicinal-chemistry-of-heterobifunctional-derivatives\/\",\"url\":\"https:\/\/www.sygnaturediscovery.com\/fr\/journal-paper\/to-homeostasis-and-beyond-recent-advances-in-the-medicinal-chemistry-of-heterobifunctional-derivatives\/\",\"name\":\"To homeostasis and beyond! Recent advances in the medicinal chemistry of heterobifunctional derivatives - Sygnature\",\"isPartOf\":{\"@id\":\"https:\/\/www.sygnaturediscovery.com\/fr\/#website\"},\"datePublished\":\"2024-09-19T09:22:00+00:00\",\"dateModified\":\"2026-01-30T09:27:09+00:00\",\"breadcrumb\":{\"@id\":\"https:\/\/www.sygnaturediscovery.com\/fr\/journal-paper\/to-homeostasis-and-beyond-recent-advances-in-the-medicinal-chemistry-of-heterobifunctional-derivatives\/#breadcrumb\"},\"inLanguage\":\"fr-CA\",\"potentialAction\":[{\"@type\":\"ReadAction\",\"target\":[\"https:\/\/www.sygnaturediscovery.com\/fr\/journal-paper\/to-homeostasis-and-beyond-recent-advances-in-the-medicinal-chemistry-of-heterobifunctional-derivatives\/\"]}]},{\"@type\":\"BreadcrumbList\",\"@id\":\"https:\/\/www.sygnaturediscovery.com\/fr\/journal-paper\/to-homeostasis-and-beyond-recent-advances-in-the-medicinal-chemistry-of-heterobifunctional-derivatives\/#breadcrumb\",\"itemListElement\":[{\"@type\":\"ListItem\",\"position\":1,\"name\":\"Home\",\"item\":\"https:\/\/www.sygnaturediscovery.com\/fr\/page-daccueil\/\"},{\"@type\":\"ListItem\",\"position\":2,\"name\":\"To homeostasis and beyond! Recent advances in the medicinal chemistry of heterobifunctional derivatives\"}]},{\"@type\":\"WebSite\",\"@id\":\"https:\/\/www.sygnaturediscovery.com\/fr\/#website\",\"url\":\"https:\/\/www.sygnaturediscovery.com\/fr\/\",\"name\":\"Sygnature Discovery\",\"description\":\"\",\"publisher\":{\"@id\":\"https:\/\/www.sygnaturediscovery.com\/fr\/#organization\"},\"alternateName\":\"Sygnature\",\"potentialAction\":[{\"@type\":\"SearchAction\",\"target\":{\"@type\":\"EntryPoint\",\"urlTemplate\":\"https:\/\/www.sygnaturediscovery.com\/fr\/?s={search_term_string}\"},\"query-input\":{\"@type\":\"PropertyValueSpecification\",\"valueRequired\":true,\"valueName\":\"search_term_string\"}}],\"inLanguage\":\"fr-CA\"},{\"@type\":\"Organization\",\"@id\":\"https:\/\/www.sygnaturediscovery.com\/fr\/#organization\",\"name\":\"Sygnature Discovery\",\"url\":\"https:\/\/www.sygnaturediscovery.com\/fr\/\",\"logo\":{\"@type\":\"ImageObject\",\"inLanguage\":\"fr-CA\",\"@id\":\"https:\/\/www.sygnaturediscovery.com\/fr\/#\/schema\/logo\/image\/\",\"url\":\"https:\/\/www.sygnaturediscovery.com\/wp-content\/uploads\/2025\/11\/Logo.svg\",\"contentUrl\":\"https:\/\/www.sygnaturediscovery.com\/wp-content\/uploads\/2025\/11\/Logo.svg\",\"width\":1,\"height\":1,\"caption\":\"Sygnature Discovery\"},\"image\":{\"@id\":\"https:\/\/www.sygnaturediscovery.com\/fr\/#\/schema\/logo\/image\/\"}}]}<\/script>\n<!-- \/ Yoast SEO plugin. -->","yoast_head_json":{"title":"To homeostasis and beyond! Recent advances in the medicinal chemistry of heterobifunctional derivatives - Sygnature","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:\/\/www.sygnaturediscovery.com\/fr\/journal-paper\/to-homeostasis-and-beyond-recent-advances-in-the-medicinal-chemistry-of-heterobifunctional-derivatives\/","og_locale":"fr_CA","og_type":"article","og_title":"To homeostasis and beyond! Recent advances in the medicinal chemistry of heterobifunctional derivatives - Sygnature","og_url":"https:\/\/www.sygnaturediscovery.com\/fr\/journal-paper\/to-homeostasis-and-beyond-recent-advances-in-the-medicinal-chemistry-of-heterobifunctional-derivatives\/","og_site_name":"Sygnature","article_modified_time":"2026-01-30T09:27:09+00:00","og_image":[{"width":2560,"height":1707,"url":"https:\/\/www.sygnaturediscovery.com\/wp-content\/uploads\/2026\/02\/sygnature-hit-to-lead-team-collaboration-scaled.webp","type":"image\/webp"}],"twitter_card":"summary_large_image","twitter_misc":{"Estimation du temps de lecture":"1 minute"},"schema":{"@context":"https:\/\/schema.org","@graph":[{"@type":"WebPage","@id":"https:\/\/www.sygnaturediscovery.com\/fr\/journal-paper\/to-homeostasis-and-beyond-recent-advances-in-the-medicinal-chemistry-of-heterobifunctional-derivatives\/","url":"https:\/\/www.sygnaturediscovery.com\/fr\/journal-paper\/to-homeostasis-and-beyond-recent-advances-in-the-medicinal-chemistry-of-heterobifunctional-derivatives\/","name":"To homeostasis and beyond! Recent advances in the medicinal chemistry of heterobifunctional derivatives - Sygnature","isPartOf":{"@id":"https:\/\/www.sygnaturediscovery.com\/fr\/#website"},"datePublished":"2024-09-19T09:22:00+00:00","dateModified":"2026-01-30T09:27:09+00:00","breadcrumb":{"@id":"https:\/\/www.sygnaturediscovery.com\/fr\/journal-paper\/to-homeostasis-and-beyond-recent-advances-in-the-medicinal-chemistry-of-heterobifunctional-derivatives\/#breadcrumb"},"inLanguage":"fr-CA","potentialAction":[{"@type":"ReadAction","target":["https:\/\/www.sygnaturediscovery.com\/fr\/journal-paper\/to-homeostasis-and-beyond-recent-advances-in-the-medicinal-chemistry-of-heterobifunctional-derivatives\/"]}]},{"@type":"BreadcrumbList","@id":"https:\/\/www.sygnaturediscovery.com\/fr\/journal-paper\/to-homeostasis-and-beyond-recent-advances-in-the-medicinal-chemistry-of-heterobifunctional-derivatives\/#breadcrumb","itemListElement":[{"@type":"ListItem","position":1,"name":"Home","item":"https:\/\/www.sygnaturediscovery.com\/fr\/page-daccueil\/"},{"@type":"ListItem","position":2,"name":"To homeostasis and beyond! Recent advances in the medicinal chemistry of heterobifunctional derivatives"}]},{"@type":"WebSite","@id":"https:\/\/www.sygnaturediscovery.com\/fr\/#website","url":"https:\/\/www.sygnaturediscovery.com\/fr\/","name":"Sygnature Discovery","description":"","publisher":{"@id":"https:\/\/www.sygnaturediscovery.com\/fr\/#organization"},"alternateName":"Sygnature","potentialAction":[{"@type":"SearchAction","target":{"@type":"EntryPoint","urlTemplate":"https:\/\/www.sygnaturediscovery.com\/fr\/?s={search_term_string}"},"query-input":{"@type":"PropertyValueSpecification","valueRequired":true,"valueName":"search_term_string"}}],"inLanguage":"fr-CA"},{"@type":"Organization","@id":"https:\/\/www.sygnaturediscovery.com\/fr\/#organization","name":"Sygnature Discovery","url":"https:\/\/www.sygnaturediscovery.com\/fr\/","logo":{"@type":"ImageObject","inLanguage":"fr-CA","@id":"https:\/\/www.sygnaturediscovery.com\/fr\/#\/schema\/logo\/image\/","url":"https:\/\/www.sygnaturediscovery.com\/wp-content\/uploads\/2025\/11\/Logo.svg","contentUrl":"https:\/\/www.sygnaturediscovery.com\/wp-content\/uploads\/2025\/11\/Logo.svg","width":1,"height":1,"caption":"Sygnature Discovery"},"image":{"@id":"https:\/\/www.sygnaturediscovery.com\/fr\/#\/schema\/logo\/image\/"}}]}},"_links":{"self":[{"href":"https:\/\/www.sygnaturediscovery.com\/fr\/wp-json\/wp\/v2\/journal-paper\/13435","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/www.sygnaturediscovery.com\/fr\/wp-json\/wp\/v2\/journal-paper"}],"about":[{"href":"https:\/\/www.sygnaturediscovery.com\/fr\/wp-json\/wp\/v2\/types\/journal-paper"}],"version-history":[{"count":0,"href":"https:\/\/www.sygnaturediscovery.com\/fr\/wp-json\/wp\/v2\/journal-paper\/13435\/revisions"}],"wp:attachment":[{"href":"https:\/\/www.sygnaturediscovery.com\/fr\/wp-json\/wp\/v2\/media?parent=13435"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/www.sygnaturediscovery.com\/fr\/wp-json\/wp\/v2\/category?post=13435"},{"taxonomy":"resource_tag","embeddable":true,"href":"https:\/\/www.sygnaturediscovery.com\/fr\/wp-json\/wp\/v2\/resource_tag?post=13435"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}