{"id":13703,"date":"2023-03-07T10:02:22","date_gmt":"2023-03-07T10:02:22","guid":{"rendered":"https:\/\/www.sygnaturediscovery.com\/une-nouvelle-plateforme-devrait-accelerer-la-degradation-ciblee-des-proteines-a-un-stade-precoce\/"},"modified":"2026-02-11T09:51:12","modified_gmt":"2026-02-11T09:51:12","slug":"une-nouvelle-plateforme-devrait-accelerer-la-degradation-ciblee-des-proteines-a-un-stade-precoce","status":"publish","type":"post","link":"https:\/\/www.sygnaturediscovery.com\/fr\/une-nouvelle-plateforme-devrait-accelerer-la-degradation-ciblee-des-proteines-a-un-stade-precoce\/","title":{"rendered":"Une nouvelle plateforme devrait acc\u00e9l\u00e9rer la d\u00e9gradation cibl\u00e9e des prot\u00e9ines \u00e0 un stade pr\u00e9coce."},"content":{"rendered":"

Sygnature Discovery, soci\u00e9t\u00e9 mondiale int\u00e9gr\u00e9e de d\u00e9couverte de m\u00e9dicaments, a d\u00e9voil\u00e9 une nouvelle plateforme facilitant l’assemblage et l’examen combinatoires \u00e0 haut d\u00e9bit de d\u00e9gradeurs mol\u00e9culaires ( CHARMED<\/a> ), en r\u00e9ponse \u00e0 une augmentation soutenue de la demande pour son expertise multidisciplinaire.<\/p>\n

Qu’est-ce que la plateforme CHARMED ?<\/h2>\n

D\u00e9velopp\u00e9e en interne chez Sygnature Discovery, CHARMED est une plateforme technologique con\u00e7ue pour acc\u00e9l\u00e9rer et soutenir les programmes de d\u00e9gradation cibl\u00e9e des prot\u00e9ines<\/a> (TPD) en phase pr\u00e9coce.<\/p>\n

Elle offre une combinaison de chimie \u00e0 haut d\u00e9bit, de biologie in vitro<\/em> et d’essais DMPK, ainsi qu’un acc\u00e8s \u00e0 des plaques 96 puits \u00ab pr\u00eates \u00e0 \u00eatre coupl\u00e9es \u00bb qui tirent parti de divers connecteurs et de t\u00eates de r\u00e9action de ligases populaires, permettant une synth\u00e8se, un criblage et une caract\u00e9risation rapides de d\u00e9gradeurs bifonctionnels afin d’acc\u00e9l\u00e9rer l’identification de compos\u00e9s candidats pour de nouvelles cibles.<\/p>\n

Le Dr Simon Hirst, fondateur et PDG de Sygnature Discovery, d\u00e9clare : \u00ab La plateforme CHARMED combine notre expertise interne de classe mondiale en chimie, en biologie in vitro<\/em> et en DMPK avec une bo\u00eete \u00e0 outils pratique qui aide les clients \u00e0 acc\u00e9l\u00e9rer leur d\u00e9couverte de m\u00e9dicaments.<\/p>\n

Avantages de CHARMED<\/h2>\n

\u00ab Dans l\u2019ensemble du secteur, nous constatons un int\u00e9r\u00eat consid\u00e9rable pour la d\u00e9gradation cibl\u00e9e des prot\u00e9ines, mais de nombreuses organisations peinent \u00e0 trouver des points de d\u00e9part pour leurs programmes ou des mol\u00e9cules poss\u00e9dant les propri\u00e9t\u00e9s ad\u00e9quates pour r\u00e9ussir en clinique. \u00bb<\/p>\n

<\/em>\u00ab L\u2019un des principaux d\u00e9fis pos\u00e9s par la d\u00e9gradation cibl\u00e9e des prot\u00e9ines et les mol\u00e9cules bifonctionnelles r\u00e9side dans le fait que leurs propri\u00e9t\u00e9s physiques sont inhabituelles et ne respectent pas la \u00ab r\u00e8gle des cinq \u00bb. De ce fait, nous devons d\u00e9velopper des technologies permettant d\u2019\u00e9valuer ces propri\u00e9t\u00e9s et de les filtrer afin de s\u00e9lectionner les mol\u00e9cules offrant les meilleurs r\u00e9sultats. \u00bb<\/p>\n

\u00ab Avec la plateforme CHARMED, nous r\u00e9unissons plusieurs technologies de Sygnature, en combinant nos capacit\u00e9s de chimie \u00e0 haut d\u00e9bit avec la biologie \u00e0 haut d\u00e9bit \u00bb, explique Simon. \u00ab Nous soutenons la synth\u00e8se rapide de mol\u00e9cules bifonctionnelles gr\u00e2ce \u00e0 une s\u00e9rie de tests et de plateformes qui permettront d\u2019\u00e9valuer leur potentiel pour la suite du d\u00e9veloppement. \u00bb<\/p>\n

Le Dr Roland Hjerpe est chercheur principal en biosciences chez Sygnature Discovery et dirige les travaux sur la d\u00e9gradation cibl\u00e9e des prot\u00e9ines. Il explique : \u00ab Dans la plupart des cas, la d\u00e9gradation cibl\u00e9e des prot\u00e9ines repose sur le rapprochement d\u2019une ligase d\u2019ubiquitine avec une prot\u00e9ine cible. De ce fait, cette m\u00e9thode ne n\u00e9cessite pas que la prot\u00e9ine cible poss\u00e8de un site actif ou une poche de liaison fonctionnelle bien d\u00e9finie et accessible. Cela signifie que des m\u00e9thodes de criblage par affinit\u00e9, bas\u00e9es sur la spectrom\u00e9trie de masse \u00e0 s\u00e9lection d\u2019affinit\u00e9 (ASMS) ou sur des banques cod\u00e9es par ADN (DEL), peuvent \u00eatre utilis\u00e9es pour identifier des ligands susceptibles de se lier \u00e0 n\u2019importe quelle poche disponible sur la prot\u00e9ine cible. Cependant, toutes les prot\u00e9ines ne sont pas identiques et toutes les prot\u00e9ines cibles ne sont pas facilement d\u00e9gradables. \u00bb <\/p>\n

C\u2019est l\u00e0 qu\u2019intervient CHARMED : cette plateforme permet aux organisations d\u2019\u00e9valuer rapidement la faisabilit\u00e9 d\u2019un projet de d\u00e9gradation de leur prot\u00e9ine d\u2019int\u00e9r\u00eat \u00e0 l\u2019aide de deux des ligases les plus courantes, acc\u00e9l\u00e9rant ainsi leur projet, r\u00e9duisant les risques et les d\u00e9lais. Elle offre un moyen rapide de collecter des donn\u00e9es et de s\u00e9lectionner un grand nombre de mol\u00e9cules parmi un ensemble plus restreint. De plus, Sygnature Discovery propose l\u2019interpr\u00e9tation des donn\u00e9es et l\u2019expertise int\u00e9gr\u00e9e n\u00e9cessaire pour acc\u00e9l\u00e9rer les projets.<\/p>\n

Ce que Sygnature Discovery peut vous offrir<\/h2>\n

Le Dr Simon Hirst ajoute : \u00ab Alors que certaines organisations continuent de d\u00e9l\u00e9guer les diff\u00e9rentes \u00e9tapes du processus de d\u00e9couverte de m\u00e9dicaments \u00e0 des CRO du monde entier, nous sommes convaincus qu’une approche plus int\u00e9gr\u00e9e est nettement plus efficace. Nos scientifiques exp\u00e9riment\u00e9s int\u00e8grent l’\u00e9quipe de recherche du projet, contribuent \u00e0 la r\u00e9solution des probl\u00e8mes et font progresser les projets. Forts d’une exp\u00e9rience r\u00e9ussie avec plus de 21 candidats cliniques \u00e0 notre actif, nous poss\u00e9dons l’expertise n\u00e9cessaire pour faire une r\u00e9elle diff\u00e9rence et maximiser les chances de succ\u00e8s des projets. En effet, nos \u00e9quipes de chercheurs en d\u00e9couverte de m\u00e9dicaments, regroup\u00e9es au sein de Sygnature Discovery, proposent une offre int\u00e9gr\u00e9e capable de mener un projet de l’identification de la cible jusqu’\u00e0 l’obtention d’un candidat m\u00e9dicament exp\u00e9rimental (IND). \u00bb<\/p>\n

CHARMED propose la synth\u00e8se parall\u00e8le de compos\u00e9s d\u00e9gradeurs PROTAC bifonctionnels ; une collection en stock de nouveaux linkers et ligands de ligase pour l’optimisation des compos\u00e9s candidats, des tests de d\u00e9gradation HTRF\u00ae<\/sup> , AlphaLISA\u00ae<\/sup> ou syst\u00e8me Jess pour les cibles endog\u00e8nes ; des tests de d\u00e9gradation cin\u00e9tique sur cellules vivantes modifi\u00e9es et une \u00e9valuation ADME in vitro<\/em> \u00e0 haut d\u00e9bit.<\/p>\n

 <\/p>\n","protected":false},"excerpt":{"rendered":"","protected":false},"author":1,"featured_media":13705,"comment_status":"closed","ping_status":"closed","sticky":false,"template":"","format":"standard","meta":{"_acf_changed":false,"footnotes":""},"category":[820,822],"tags":[885,881,883,887,860,880,891,866,824,825,856,829,898,897,874,872,889,862,868,864,895,893,870,858,878,828,876],"class_list":["post-13703","post","type-post","status-publish","format-standard","has-post-thumbnail","hentry","category-modalites","category-tpd","tag-approche-integree","tag-assemblage-a-haut-debit","tag-biologie-in-vitro","tag-candidat-a-un-nouveau-medicament-experimental-ind","tag-chasseurs-de-drogue","tag-cibles-endogenes","tag-composes-de-plomb","tag-composes-protac-bifonctionnels","tag-decouverte-de-la-signature","tag-decouverte-de-medicaments","tag-decouverte-integree-de-medicaments","tag-degradation-ciblee-des-proteines","tag-degradation-des-proteines","tag-degradeurs-moleculaires","tag-developpement-de-medicaments","tag-dosages-dmpk","tag-essais-de-degradation-cinetique","tag-evaluation-adme","tag-industrie-biopharmaceutique","tag-molecules-bifonctionnelles","tag-ogives-de-ligase","tag-optimisation-des-leads","tag-plateforme-charmed","tag-recherche-et-developpement","tag-stade-precoce","tag-synthese-rapide","tag-technologie-de-decouverte-de-medicaments"],"acf":[],"yoast_head":"\nUne 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