{"id":13431,"date":"2024-03-26T09:10:00","date_gmt":"2024-03-26T09:10:00","guid":{"rendered":"https:\/\/www.sygnaturediscovery.com\/?post_type=journal-paper&#038;p=13431"},"modified":"2026-01-30T09:16:28","modified_gmt":"2026-01-30T09:16:28","slug":"breaking-bad-proteins-discovery-approaches-and-the-road-to-clinic-for-degraders","status":"publish","type":"journal-paper","link":"https:\/\/www.sygnaturediscovery.com\/fr\/journal-paper\/breaking-bad-proteins-discovery-approaches-and-the-road-to-clinic-for-degraders\/","title":{"rendered":"Breaking Bad Proteins\u2014Discovery Approaches and the Road to Clinic for Degraders"},"content":{"rendered":"\n<p class=\"wp-block-paragraph\">Corentin Bouvier, <strong>Rachel Lawrence<\/strong>, <strong>Francesca Cavallo<\/strong>, Wendy Xolalpa, <strong>Allan Jordan<\/strong>,<strong> Roland Hjerpe<\/strong>, Manuel S. Rodriguez<a href=\"mailto:corentin.bouvier@lcc-toulouse.fr\"><\/a><\/p>\n\n\n\n<p class=\"wp-block-paragraph\"><strong>Abstract<\/strong><\/p>\n\n\n\n<p class=\"wp-block-paragraph\">Proteolysis-targeting chimeras (PROTACs) describe compounds that bind to and induce degradation of a target by simultaneously binding to a ubiquitin ligase. More generally referred to as bifunctional degraders, PROTACs have led the way in the field of targeted protein degradation (TPD), with several compounds currently undergoing clinical testing. Alongside bifunctional degraders, single-moiety compounds, or molecular glue degraders (MGDs), are increasingly being considered as a viable approach for development of therapeutics, driven by advances in rational discovery approaches. This review focuses on drug discovery with respect to bifunctional and molecular glue degraders within the ubiquitin proteasome system, including analysis of mechanistic concepts and discovery approaches, with an overview of current clinical and pre-clinical degrader status in oncology, neurodegenerative and inflammatory disease.<\/p>\n\n\n\n<p class=\"wp-block-paragraph\">Ref: <a href=\"https:\/\/www.mdpi.com\/2073-4409\/13\/7\/578\">Cells 2024<\/a><\/p>\n\n\n\n<p class=\"wp-block-paragraph\"><\/p>\n","protected":false},"excerpt":{"rendered":"","protected":false},"featured_media":0,"template":"","category":[686,743],"resource_tag":[],"class_list":["post-13431","journal-paper","type-journal-paper","status-publish","hentry","category-modalities","category-tpd"],"acf":[],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v28.6 - https:\/\/yoast.com\/product\/yoast-seo-wordpress\/ -->\n<title>Breaking Bad Proteins: Degrader Discovery to the Clinic<\/title>\n<meta name=\"description\" content=\"Review of bifunctional PROTAC and molecular glue degraders, their mechanisms and status in oncology, neurodegenerative and inflammatory disease. 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