{"id":3854,"date":"2016-11-18T10:21:51","date_gmt":"2016-11-18T10:21:51","guid":{"rendered":"https:\/\/www.sygnaturediscovery.com\/poster\/fragment-based-hit-identification-epigenetic-target-brd3\/"},"modified":"2025-12-12T11:34:42","modified_gmt":"2025-12-12T11:34:42","slug":"fragment-based-hit-identification-epigenetic-target-brd3","status":"publish","type":"poster","link":"https:\/\/www.sygnaturediscovery.com\/fr\/poster\/fragment-based-hit-identification-epigenetic-target-brd3\/","title":{"rendered":"Fragment-based Hit Identification for the Epigenetic Target BRD3"},"content":{"rendered":"<p><strong>Abstract<\/strong><\/p>\n<p>Sygnature Discovery has designed and synthesised a proprietary fragment library with a high degree of novelty that covers a wide range of chemical space. Comprised of over 900 compounds, most of which are not commercially available (&gt;60%), the library was designed using the \u2018rule of 3\u2019 as a guideline and with a strong emphasis on diversity.<\/p>\n<p>To demonstrate its effectiveness in fragment-based drug discovery, the library was screened against an\u00a0epigenetic target with little previous literature on drug discovery, Bromodomain-containing protein 3 (<a href=\"https:\/\/www.sygnaturediscovery.com\/publications\/case-studies\/fragment-based-hit-discovery-for-the-epigenetic-target-brd3\/\">BRD3<\/a>,\u00a0also known as RING3L). Like other members of the Bromodomain and Extra-Terminalmotif (BET) family,\u00a0BRD3 contains two tandem homologous bromodomains and an extra terminal motif. It functions by binding\u00a0acetylated lysine residues on chromatin and transcriptional regulators, exemplified by the role it plays in the\u00a0regulation of transcription by promoting the binding of GATA1 (Figure 1). Due to this involvement in\u00a0regulation, BET members often play a role in several types of cancer. BRD3, in particular, is associated with a\u00a0number of disease phenotypes. For example, depletion of BRD3 slows growth in cancer models including prostate cancer and medulloblastoma and <a href=\"https:\/\/www.sygnaturediscovery.com\/publications\/case-studies\/fragment-based-hit-discovery-for-the-epigenetic-target-brd3\/\">BRD3<\/a> has been implicated in NUT midline carcinoma (NMT).<\/p>\n<p>While there are a number of available pan-BET inhibitors, the design of specific BRD3 inhibitors may lead to a beneficial clinical outcome with reduced off-target effects. However, bromodomains of the BET family have a high degree of structural similarity, especially in the acetylated lysine binding pocket, making the design of selective inhibitors problematic. BRD3, therefore, represents an intriguing and challenging drug discovery target. While there are a number of available pan-BET inhibitors, the design of specific BRD3 inhibitors may lead to a beneficial clinical outcome with reduced off-target effects. However, bromodomains of the BET family have a high degree of structural similarity, especially in the acetylated lysine binding pocket, making the design of selective inhibitors problematic. BRD3, therefore, represents an intriguing and challenging drug discovery target.<\/p>\n","protected":false},"excerpt":{"rendered":"","protected":false},"featured_media":2476,"template":"","category":[1],"class_list":["post-3854","poster","type-poster","status-publish","has-post-thumbnail","hentry","category-uncategorized"],"acf":[],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v27.9 - https:\/\/yoast.com\/product\/yoast-seo-wordpress\/ -->\n<title>Fragment-based Hit Identification for the Epigenetic Target BRD3 -<\/title>\n<meta name=\"description\" content=\"Sygnature&#039;s unique fragment library demonstrates effective drug discovery through BRD3 screening, targeting an intriguing epigenetic goal.\" \/>\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\/fragment-based-hit-identification-epigenetic-target-brd3\/\" 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