{"id":22509,"date":"2026-09-14T11:02:40","date_gmt":"2026-09-14T11:02:40","guid":{"rendered":"https:\/\/www.sygnaturediscovery.com\/poster\/criblage-de-fragments-pour-les-liants-vhl-et-developpement-de-protac\/"},"modified":"2026-11-12T13:54:57","modified_gmt":"2026-11-12T13:54:57","slug":"criblage-de-fragments-pour-les-liants-vhl-et-developpement-de-protac","status":"publish","type":"poster","link":"https:\/\/www.sygnaturediscovery.com\/fr\/poster\/criblage-de-fragments-pour-les-liants-vhl-et-developpement-de-protac\/","title":{"rendered":"Criblage de fragments pour les liants VHL et d\u00e9veloppement de PROTAC"},"content":{"rendered":"\n<p class=\"wp-block-paragraph\">La ligase E3 de Von Hippel-Lindau (VHL) est l&rsquo;une des cibles de d\u00e9gradation prot\u00e9ique les plus utilis\u00e9es dans la d\u00e9couverte de PROTAC. Cependant, le nombre limit\u00e9 de ligands VHL disponibles et leurs propri\u00e9t\u00e9s physico-chimiques complexes continuent de freiner le d\u00e9veloppement de d\u00e9gradeurs de VHL biodisponibles par voie orale.<\/p>\n\n<p class=\"wp-block-paragraph\">Cet article explore comment le criblage par fragments peut r\u00e9v\u00e9ler de nouveaux points de d\u00e9part efficaces pour la d\u00e9couverte de ligands de VHL. Gr\u00e2ce \u00e0 la technologie Spectral Shift (SpS) et \u00e0 la biblioth\u00e8que de fragments Sygnature, les chercheurs ont identifi\u00e9 des ligands jusqu&rsquo;alors inconnus du complexe VHL-ElonginC-ElonginB (VCB) et caract\u00e9ris\u00e9 leurs sites de liaison par cristallographie aux rayons X. <\/p>\n\n<h2 class=\"wp-block-heading has-text-2-xl-font-size\" style=\"padding-top:var(--wp--preset--spacing--30)\">Identification de nouvelles opportunit\u00e9s pour la d\u00e9gradation cibl\u00e9e des prot\u00e9ines <\/h2>\n\n<p class=\"wp-block-paragraph\">Les approches bas\u00e9es sur la fragmentation sont particuli\u00e8rement adapt\u00e9es \u00e0 la d\u00e9couverte de nouveaux sites de liaison et \u00e0 la g\u00e9n\u00e9ration de ligands \u00e0 haute efficacit\u00e9 pour l&rsquo;optimisation en chimie m\u00e9dicinale. Dans cette \u00e9tude, environ 1\u00a0600 fragments ont \u00e9t\u00e9 cribl\u00e9s contre le complexe VCB, ce qui a permis d&rsquo;identifier 12 ligands confirm\u00e9s pr\u00e9sentant des affinit\u00e9s reproductibles. Des tests de comp\u00e9tition et des \u00e9tudes structurales ult\u00e9rieurs ont r\u00e9v\u00e9l\u00e9 des sites de liaison distincts de la poche HIF bien caract\u00e9ris\u00e9e.<\/p>\n\n<p class=\"wp-block-paragraph\">T\u00e9l\u00e9chargez l&rsquo;affiche pour en savoir plus\u00a0:<\/p>\n\n<ul class=\"wp-block-list\">\n<li>Criblage par d\u00e9calage spectral d&rsquo;environ 1\u00a0600 fragments contre le complexe VCB.<\/li>\n\n\n\n<li>Identification de 12 fragments confirm\u00e9s avec des valeurs de KD reproductibles.<\/li>\n\n\n\n<li>Tests de comp\u00e9tition d\u00e9montrant une liaison en dehors du site d&rsquo;interaction HIF.<\/li>\n\n\n\n<li>Caract\u00e9risation par cristallographie aux rayons X de quatre ligands de fragments\u00a0;<\/li>\n\n\n\n<li>d\u00e9couverte d\u2019une nouvelle poche de liaison \u00e0 l\u2019\u00e9longine B\u00a0;<\/li>\n\n\n\n<li>opportunit\u00e9s de d\u00e9velopper de nouveaux amorces PROTAC efficaces pour le recrutement de VHL par ligand.<\/li>\n<\/ul>\n\n<h2 class=\"wp-block-heading has-text-2-xl-font-size\" style=\"padding-top:var(--wp--preset--spacing--30)\">Des fragments d&rsquo;impact aux nouveaux gestionnaires PROTAC <\/h2>\n\n<p class=\"wp-block-paragraph\">L&rsquo;analyse structurale a permis d&rsquo;identifier un fragment particuli\u00e8rement prometteur, F4, se liant \u00e0 une poche jusqu&rsquo;alors inexploit\u00e9e de l&rsquo;\u00e9longine B. Contrairement aux sites de liaison connus qui chevauchent des interfaces d&rsquo;interaction prot\u00e9ine-prot\u00e9ine critiques, ce nouveau site semble accessible au sein du complexe actif de la ligase E3 et offre une voie potentielle pour le d\u00e9veloppement de ligands alternatifs recrutant VHL. <\/p>\n\n<p class=\"wp-block-paragraph\">Ces r\u00e9sultats d\u00e9montrent comment la combinaison du criblage de fragments, de la caract\u00e9risation biophysique et de la biologie structurale peut r\u00e9v\u00e9ler de nouvelles opportunit\u00e9s dans la d\u00e9gradation cibl\u00e9e des prot\u00e9ines et soutenir le d\u00e9veloppement de th\u00e9rapies d\u00e9gradantes de nouvelle g\u00e9n\u00e9ration. <\/p>\n","protected":false},"excerpt":{"rendered":"","protected":false},"featured_media":22511,"template":"","category":[790,1410,1416,1471,1429,1262,820,815],"class_list":["post-22509","poster","type-poster","status-publish","has-post-thumbnail","hentry","category-bioscience","category-caracterisation-des-proteines","category-cristallographie-aux-rayons-x","category-degradation-ciblee-des-proteines","category-developpement-des-essais","category-essais-biophysiques","category-modalites","category-proteines-et-structure"],"acf":[],"yoast_head":"<!-- This site is optimized with the Yoast SEO Premium plugin v28.8 (Yoast SEO v28.8) - https:\/\/yoast.com\/product\/yoast-seo-premium-wordpress\/ -->\n<title>Criblage de fragments pour les liants VHL et le d\u00e9veloppement de PROTAC -<\/title>\n<meta name=\"description\" content=\"Le criblage par d\u00e9calage spectral a permis d&#039;identifier 12 fragments VHL-EloC-EloB se liant \u00e0 l&#039;enzyme. Des \u00e9tudes structurales ont r\u00e9v\u00e9l\u00e9 un nouveau site de liaison \u00e0 l&#039;\u00e9longine B pour l&#039;optimisation de l&#039;amorce PROTAC.\" \/>\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\/poster\/criblage-de-fragments-pour-les-liants-vhl-et-developpement-de-protac\/\" \/>\n<meta property=\"og:locale\" content=\"fr_CA\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Criblage de fragments pour les liants VHL et d\u00e9veloppement de PROTAC\" \/>\n<meta property=\"og:description\" content=\"Le criblage par d\u00e9calage spectral a permis d&#039;identifier 12 fragments VHL-EloC-EloB se liant \u00e0 l&#039;enzyme. Des \u00e9tudes structurales ont r\u00e9v\u00e9l\u00e9 un nouveau site de liaison \u00e0 l&#039;\u00e9longine B pour l&#039;optimisation de l&#039;amorce PROTAC.\" \/>\n<meta property=\"og:url\" content=\"https:\/\/www.sygnaturediscovery.com\/fr\/poster\/criblage-de-fragments-pour-les-liants-vhl-et-developpement-de-protac\/\" \/>\n<meta property=\"og:site_name\" content=\"Sygnature\" \/>\n<meta property=\"article:modified_time\" content=\"2026-11-12T13:54:57+00:00\" \/>\n<meta property=\"og:image\" content=\"https:\/\/www.sygnaturediscovery.com\/wp-content\/uploads\/2026\/08\/fragment-screening-vhl-binders-protac-development.webp\" \/>\n\t<meta property=\"og:image:width\" content=\"500\" \/>\n\t<meta property=\"og:image:height\" content=\"360\" \/>\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=\"2 minutes\" \/>\n<script type=\"application\/ld+json\" class=\"yoast-schema-graph\">{\"@context\":\"https:\\\/\\\/schema.org\",\"@graph\":[{\"@type\":\"WebPage\",\"@id\":\"https:\\\/\\\/www.sygnaturediscovery.com\\\/fr\\\/poster\\\/criblage-de-fragments-pour-les-liants-vhl-et-developpement-de-protac\\\/\",\"url\":\"https:\\\/\\\/www.sygnaturediscovery.com\\\/fr\\\/poster\\\/criblage-de-fragments-pour-les-liants-vhl-et-developpement-de-protac\\\/\",\"name\":\"Criblage de fragments pour les liants VHL et le d\u00e9veloppement de PROTAC -\",\"isPartOf\":{\"@id\":\"https:\\\/\\\/www.sygnaturediscovery.com\\\/fr\\\/#website\"},\"primaryImageOfPage\":{\"@id\":\"https:\\\/\\\/www.sygnaturediscovery.com\\\/fr\\\/poster\\\/criblage-de-fragments-pour-les-liants-vhl-et-developpement-de-protac\\\/#primaryimage\"},\"image\":{\"@id\":\"https:\\\/\\\/www.sygnaturediscovery.com\\\/fr\\\/poster\\\/criblage-de-fragments-pour-les-liants-vhl-et-developpement-de-protac\\\/#primaryimage\"},\"thumbnailUrl\":\"https:\\\/\\\/www.sygnaturediscovery.com\\\/wp-content\\\/uploads\\\/2026\\\/08\\\/fragment-screening-vhl-binders-protac-development.webp\",\"datePublished\":\"2026-09-14T11:02:40+00:00\",\"dateModified\":\"2026-11-12T13:54:57+00:00\",\"description\":\"Le criblage par d\u00e9calage spectral a permis d'identifier 12 fragments VHL-EloC-EloB se liant \u00e0 l'enzyme. 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