{"id":49639,"date":"2018-05-23T00:00:00","date_gmt":"2018-05-22T23:00:00","guid":{"rendered":"http:\/\/www.pcb.ub.edu\/researchers-develop-a-new-class-of-covalent-inhibitor-for-a-protein-involved-in-brain-diseases\/"},"modified":"2020-11-18T14:56:07","modified_gmt":"2020-11-18T13:56:07","slug":"researchers-develop-a-new-class-of-covalent-inhibitor-for-a-protein-involved-in-brain-diseases","status":"publish","type":"post","link":"https:\/\/www.pcb.ub.edu\/en\/researchers-develop-a-new-class-of-covalent-inhibitor-for-a-protein-involved-in-brain-diseases\/","title":{"rendered":"Researchers develop a new class of covalent inhibitor for a protein involved in brain diseases"},"content":{"rendered":"<p>Most POP inhibitors developed to date have a short half-life in blood, do not show sufficient selectivity for the protein, and do not cross the blood-brain barrier (which protects the brain), thus limiting their potential as drugs.<\/p>\n<p>Work done by IRB Barcelona postdoctoral fellow\u00a0Salvador Guardiola\u00a0describes the first class of POP inhibitor characterised by long half-life, selectivity and capacity to enter the brain. The\u00a0<a href=\"https:\/\/www.irbbarcelona.org\/en\/research\/design-synthesis-and-structure-of-peptides-and-proteins\" target=\"_blank\" rel=\"noopener noreferrer\">Design, Synthesis and Structure of Peptides and Proteins<\/a>\u00a0lab, headed by\u00a0Ernest Giralt, has generated and characterised a family of 15 modified peptides (small proteins), called peptidomimetics, which have shown promising results.<\/p>\n<p>&#8220;Natural peptides are not stable in tissues and have relatively weak activity. In contrast, if we modify them with synthetic amino acids and introduce functional groups designed to react with the therapeutic target, we can achieve peptides that are much more active and efficient,&#8221; explains Guardiola.<\/p>\n<p>At low concentrations, these new peptides inhibit POP in a rapid, specific and sustained manner, both in the isolated enzyme and in human intact cells. In addition, they are highly selective for two proteases that are similar to POP (DPPIV and FAP) and show a high capacity to cross the blood-brain barrier, say the researchers.<\/p>\n<p>&#8220;These inhibitors pave the way for the development of new treatments for diseases of the central nervous system and will also contribute to studies on the role of POP in these disorders and to the \u00a0development of inhibitors of other proteases,&#8221; explains \u00a0Giralt, who is also a senior professor at the University of Barcelona (UB).<\/p>\n<p>This study has been funded by the Ministry of Economy and Competitiveness, ERDFs, and the Catalan government.<\/p>\n<p>\n\u25ba\u00a0<strong>Reference article<\/strong>: Salvador Guardiola, Roger Prades, Laura Mendieta, Arwin J. Brouwer, Jelle Streefkerk, Laura Nevola, Teresa Tarrag\u00f3, Rob M. J. Liskamp, Ernest Giralt. &#8220;<a href=\"https:\/\/www.cell.com\/cell-chemical-biology\/fulltext\/S2451-9456(18)30143-0\" target=\"_blank\" rel=\"noopener noreferrer\">Targeted covalent inhibition of prolyl oligopeptidase (POP): discovery of sulfonylfluoride peptidomimetics<\/a>&#8220;. Cell Chemical Biology\u00a0(2018) DOI:\u00a010.1016\/j.chembiol.2018.04.013<\/p>\n","protected":false},"excerpt":{"rendered":"<p>An article published in\u00a0Cell Chemical Biology\u00a0by scientists at the Institute for Research in Biomedicine (<a href=\"http:\/\/www.pcb.ub.edu\/portal\/en\/cerca?p_p_id=cercador_WAR_empleatsempresesportlet&amp;p_p_lifecycle=0&amp;p_p_state=maximized&amp;p_p_mode=view&amp;p_p_col_id=column-1&amp;p_p_col_count=1&amp;_cercador_WAR_empleatsempresesportlet_jspPage=%2Fhtml%2Fcommon%2Fdetall-empresa.jsp&amp;_cercador_WAR_empleatsempresesportlet_empresaId=ENT_000001&amp;_cercador_WAR_empleatsempresesportlet_redirect=%2Fportal%2Fca%2Fcerca%3Fp_p_id%3Dcercador_WAR_empleatsempresesportlet%26p_p_lifecycle%3D0%26p_p_mode%3Dview%26_cercador_WAR_empleatsempresesportlet_keywords%3Dirb%26_cercador_WAR_empleatsempresesportlet_tab%3D1\" target=\"_blank\" rel=\"noopener noreferrer\">IRB Barcelona<\/a>) in Barcelona Science Park (PCB) describes a new class of prolyl oligopeptidase (POP) inhibitors. Found mostly in the brain, POP protein\u00a0has emerged as an \u201cattractive\u00b7\u201d therapeutic target for the treatment of several cognitive and neurodegenerative disorders, such as Parkinson\u2019s disease and schizophrenia.The work was done in collaboration with the biotech <a href=\"http:\/\/www.pcb.ub.edu\/portal\/en\/cerca?p_p_id=cercador_WAR_empleatsempresesportlet&amp;p_p_lifecycle=0&amp;p_p_state=maximized&amp;p_p_mode=view&amp;p_p_col_id=column-1&amp;p_p_col_count=1&amp;_cercador_WAR_empleatsempresesportlet_jspPage=%2Fhtml%2Fcommon%2Fdetall-empresa.jsp&amp;_cercador_WAR_empleatsempresesportlet_empresaId=ENT_005306&amp;_cercador_WAR_empleatsempresesportlet_redirect=%2Fportal%2Fes%2Fcerca%3Fp_p_id%3Dcercador_WAR_empleatsempresesportlet%26p_p_lifecycle%3D0%26p_p_mode%3Dview%26_cercador_WAR_empleatsempresesportlet_keywords%3Diproteos%26_cercador_WAR_empleatsempresesportlet_tab%3D1\" target=\"_blank\" rel=\"noopener noreferrer\">Iproteos<\/a>, based in PCB and scientists at the University of Glasgow (Scotland, UK) and the Utrecht Institute for Pharmaceutical Sciences (the Netherlands).\u00a0The study has also involved the\u00a0<a href=\"http:\/\/www.rmn.ub.es\/lrb\/index.php\" target=\"_blank\" rel=\"noopener noreferrer\">Nuclear Magnetic Resonance Laboratory (LRB)<\/a>\u00a0\u2013wich is part of\u00a0<a href=\"http:\/\/www.ccit.ub.edu\/CA\/home.html\" target=\"_blank\" rel=\"noopener noreferrer\">CCiTUB<\/a>\u00a0and\u00a0it&#8217;s located\u00a0in the Cluster building of the Park\u2013 and the Barcelona Supercomputing Center (BSC).<\/p>\n<p>\u00a0<\/p>\n","protected":false},"author":1,"featured_media":53675,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"_acf_changed":false,"inline_featured_image":false,"footnotes":""},"categories":[8],"tags":[],"class_list":["post-49639","post","type-post","status-publish","format-standard","has-post-thumbnail","category-uncategorized"],"acf":[],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v27.7 - https:\/\/yoast.com\/product\/yoast-seo-wordpress\/ -->\n<title>Researchers develop a new class of covalent inhibitor for a protein involved in brain diseases - Parc Cient\u00edfic de Barcelona<\/title>\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.pcb.ub.edu\/en\/researchers-develop-a-new-class-of-covalent-inhibitor-for-a-protein-involved-in-brain-diseases\/\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Researchers develop a new class of covalent inhibitor for a protein involved in brain diseases - Parc Cient\u00edfic de Barcelona\" \/>\n<meta property=\"og:description\" content=\"An article published in\u00a0Cell Chemical Biology\u00a0by scientists at the Institute for Research in Biomedicine (IRB Barcelona) in Barcelona Science Park (PCB) describes a new class of prolyl oligopeptidase (POP) inhibitors. Found mostly in the brain, POP protein\u00a0has emerged as an \u201cattractive\u00b7\u201d therapeutic target for the treatment of several cognitive and neurodegenerative disorders, such as Parkinson\u2019s disease and schizophrenia.The work was done in collaboration with the biotech Iproteos, based in PCB and scientists at the University of Glasgow (Scotland, UK) and the Utrecht Institute for Pharmaceutical Sciences (the Netherlands).\u00a0The study has also involved the\u00a0Nuclear Magnetic Resonance Laboratory (LRB)\u00a0\u2013wich is part of\u00a0CCiTUB\u00a0and\u00a0it&#039;s located\u00a0in the Cluster building of the Park\u2013 and the Barcelona Supercomputing Center (BSC). \u00a0\" \/>\n<meta property=\"og:url\" content=\"https:\/\/www.pcb.ub.edu\/en\/researchers-develop-a-new-class-of-covalent-inhibitor-for-a-protein-involved-in-brain-diseases\/\" \/>\n<meta property=\"og:site_name\" content=\"Parc Cient\u00edfic de Barcelona\" \/>\n<meta property=\"article:published_time\" content=\"2018-05-22T23:00:00+00:00\" \/>\n<meta property=\"article:modified_time\" content=\"2020-11-18T13:56:07+00:00\" \/>\n<meta property=\"og:image\" content=\"https:\/\/www.pcb.ub.edu\/wp-content\/uploads\/2018\/05\/16057070365fb5251c5f758.jpeg\" \/>\n\t<meta property=\"og:image:width\" content=\"600\" \/>\n\t<meta property=\"og:image:height\" content=\"670\" \/>\n\t<meta property=\"og:image:type\" content=\"image\/jpeg\" \/>\n<meta name=\"author\" content=\"adminpcb\" \/>\n<meta name=\"twitter:card\" content=\"summary_large_image\" \/>\n<meta name=\"twitter:label1\" content=\"Written by\" \/>\n\t<meta name=\"twitter:data1\" content=\"adminpcb\" \/>\n\t<meta name=\"twitter:label2\" content=\"Est. reading time\" \/>\n\t<meta name=\"twitter:data2\" content=\"2 minutes\" \/>\n<script type=\"application\/ld+json\" class=\"yoast-schema-graph\">{\"@context\":\"https:\\\/\\\/schema.org\",\"@graph\":[{\"@type\":\"Article\",\"@id\":\"https:\\\/\\\/www.pcb.ub.edu\\\/en\\\/researchers-develop-a-new-class-of-covalent-inhibitor-for-a-protein-involved-in-brain-diseases\\\/#article\",\"isPartOf\":{\"@id\":\"https:\\\/\\\/www.pcb.ub.edu\\\/en\\\/researchers-develop-a-new-class-of-covalent-inhibitor-for-a-protein-involved-in-brain-diseases\\\/\"},\"author\":{\"name\":\"adminpcb\",\"@id\":\"https:\\\/\\\/www.pcb.ub.edu\\\/es\\\/#\\\/schema\\\/person\\\/d13cab05cd0a75b17fddca8496481021\"},\"headline\":\"Researchers develop a new class of covalent inhibitor for a protein involved in brain diseases\",\"datePublished\":\"2018-05-22T23:00:00+00:00\",\"dateModified\":\"2020-11-18T13:56:07+00:00\",\"mainEntityOfPage\":{\"@id\":\"https:\\\/\\\/www.pcb.ub.edu\\\/en\\\/researchers-develop-a-new-class-of-covalent-inhibitor-for-a-protein-involved-in-brain-diseases\\\/\"},\"wordCount\":324,\"image\":{\"@id\":\"https:\\\/\\\/www.pcb.ub.edu\\\/en\\\/researchers-develop-a-new-class-of-covalent-inhibitor-for-a-protein-involved-in-brain-diseases\\\/#primaryimage\"},\"thumbnailUrl\":\"https:\\\/\\\/www.pcb.ub.edu\\\/wp-content\\\/uploads\\\/2018\\\/05\\\/16057070365fb5251c5f758.jpeg\",\"inLanguage\":\"en-US\"},{\"@type\":\"WebPage\",\"@id\":\"https:\\\/\\\/www.pcb.ub.edu\\\/en\\\/researchers-develop-a-new-class-of-covalent-inhibitor-for-a-protein-involved-in-brain-diseases\\\/\",\"url\":\"https:\\\/\\\/www.pcb.ub.edu\\\/en\\\/researchers-develop-a-new-class-of-covalent-inhibitor-for-a-protein-involved-in-brain-diseases\\\/\",\"name\":\"Researchers develop a new class of covalent inhibitor for a protein involved in brain diseases - 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