{"id":4044,"date":"2024-06-18T14:09:26","date_gmt":"2024-06-18T14:09:26","guid":{"rendered":"https:\/\/www.sygnaturediscovery.com\/poster\/synthesis-of-leucine-rich-repeat-kinase-2-degraders-for-parkinsons-disease\/"},"modified":"2026-01-22T15:37:45","modified_gmt":"2026-01-22T15:37:45","slug":"synthesis-of-leucine-rich-repeat-kinase-2-degraders-for-parkinsons-disease","status":"publish","type":"poster","link":"https:\/\/www.sygnaturediscovery.com\/fr\/poster\/synthesis-of-leucine-rich-repeat-kinase-2-degraders-for-parkinsons-disease\/","title":{"rendered":"Synthesis of Leucine-rich repeat kinase 2 Degraders for Parkinson&rsquo;s Disease"},"content":{"rendered":"<p>Leucine-rich repeat kinase 2 (LRRK2) is a gene associated with familial Parkinson\u2019s disease (PD) and the G2019S mutation causes an increase in kinase activity. Type I ATP-competitive LRRK2 small-molecule inhibitors (SMIs) are the most predominant strategy developed to treat PD. Despite the preclinical success of several LRRK2 SMIs, dephosphorylation of biomarker sites and LRRK2 aggregation have been reported. The limitations of LRRK2 SMIs provided an opportunity to utilise known SMIs to make novel LRRK2 proteolysis-targeting chimeras (PROTACs). The synthesis of pyrrolopyrimidine-based and aminopyrimidine-based, LRRK2 SMIs and PROTACs, is described herein. The use of common chemical reactions such as nucleophilic aromatic substitutions and reductive aminations gave access to E3 ligase ligand\/ linker scaffolds, for final coupling reactions to the LRRK2 SMI. The synthesised ligands and PROTACs were submitted as candidates for biological assays to examine degrader efficiency.<\/p>\n<p>&nbsp;<\/p>\n<p><em>The poster was presented at the SCI YCP Undergraduate IP and apprenticeship symposium in Manchester on 27<sup>th<\/sup> June 2024.<\/em><\/p>\n","protected":false},"excerpt":{"rendered":"","protected":false},"featured_media":2734,"template":"","category":[682,686,753,714,688,743],"class_list":["post-4044","poster","type-poster","status-publish","has-post-thumbnail","hentry","category-chemistry","category-modalities","category-neuroscience","category-synthetic-chemistry","category-therapeutic-areas","category-tpd"],"acf":[],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v27.3 - https:\/\/yoast.com\/product\/yoast-seo-wordpress\/ -->\n<title>Leucine-rich repeat kinase 2 Degraders Parkinson\u2019s Disease<\/title>\n<meta name=\"description\" content=\"The rise in Parkinson\u2019s disease (PD) cases in recent years has emphasised the need for novel ways to treat this neurodegenerative disorder.\" \/>\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\/synthesis-of-leucine-rich-repeat-kinase-2-degraders-for-parkinsons-disease\/\" \/>\n<meta property=\"og:locale\" content=\"fr_CA\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Leucine-rich repeat kinase 2 Degraders Parkinson\u2019s Disease\" \/>\n<meta property=\"og:description\" content=\"The rise in Parkinson\u2019s disease (PD) cases in recent years has emphasised the need for novel ways to treat this neurodegenerative disorder.\" \/>\n<meta property=\"og:url\" content=\"https:\/\/www.sygnaturediscovery.com\/fr\/poster\/synthesis-of-leucine-rich-repeat-kinase-2-degraders-for-parkinsons-disease\/\" \/>\n<meta property=\"og:site_name\" content=\"Sygnature\" 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