{"id":4682,"date":"2019-04-01T11:25:46","date_gmt":"2019-04-01T09:25:46","guid":{"rendered":"https:\/\/www.tarosdiscovery.com\/unkategorisiert\/clinical-candidates-modulating-protein-protein-interactions-the-fragment-based-experience\/"},"modified":"2024-01-26T10:52:27","modified_gmt":"2024-01-26T09:52:27","slug":"clinical-candidates-modulating-protein-protein-interactions-the-fragment-based-experience","status":"publish","type":"post","link":"https:\/\/www.tarosdiscovery.com\/de\/news\/clinical-candidates-modulating-protein-protein-interactions-the-fragment-based-experience-2\/","title":{"rendered":"Clinical candidates modulating protein-protein interactions: The fragment-based experience"},"content":{"rendered":"\t\t
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Clinical candidates modulating protein-protein interactions: The fragment-based experience<\/h1>\t\t\t\t<\/div>\n\t\t\t\t<\/div>\n\t\t\t\t\t<\/div>\n\t\t<\/div>\n\t\t\t\t\t<\/div>\n\t\t<\/section>\n\t\t\t\t
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Dario Valenti, Stanimira Hristeva, Dimitrios Tzalis, and Christian Ottmann<\/h3>\n

Eur. J. Med. Chem., Apr. 2019, 167, pp 76-95,\u00a0\u00a0DOI: 10.1016\/j.ejmech.2019.01.084;<\/strong><\/p>\n\t\t\t\t\t\t\t\t<\/div>\n\t\t\t\t<\/div>\n\t\t\t\t

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Abstract:<\/strong><\/p>\n

Protein-protein interactions\u00a0(PPIs) cover a very wide range of\u00a0biological\u00a0functions and consequently have become one of the favourite targets for new therapeutic strategies. PPIs are strongly characterised by an intricate and\u00a0dynamic\u00a0network of\u00a0surface\u00a0interactions occurring between two or more\u00a0proteins. Because of the complexity of these interactions, many strategies have been applied with the aim to find selective\u00a0modulators\u00a0for a specific protein-protein complex. During the last decade, fragment-based approaches have served many\u00a0drug\u00a0discovery programs with an impressive increment of contributions, gaining a remarkable\u00a0role\u00a0in PPIs modulators\u2019\u00a0development. In this review, we detail the successful fragment-to-clinical candidate\u00a0evolutions\u00a0related to PPI\u00a0modulation. An overview on the\u00a0physico-chemical properties\u00a0of both fragment hits and\u00a0lead compounds\u00a0will be presented together with a statistical analysis of their distribution.<\/p>\n\t\t\t\t\t\t\t\t<\/div>\n\t\t\t\t<\/div>\n\t\t\t\t\t<\/div>\n\t\t<\/div>\n\t\t\t\t

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Interessiert Sie diese Publikation? Kontaktieren Sie unsere Wissenschaftler<\/h2>\t\t\t\t<\/div>\n\t\t\t\t<\/div>\n\t\t\t\t
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Medizinalchemie<\/p>\n\t\t\t\t\t\t\t\t<\/div>\n\t\t\t\t<\/div>\n\t\t\t\t

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Wirkstoffforschung<\/h3>\t\t\t\t<\/div>\n\t\t\t\t<\/div>\n\t\t\t\t
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Das internationale Team von Taros verf\u00fcgt kombiniert \u00fcber mehr als 180 Jahre Erfahrung in der pharmazeutischen F&E. Als Team haben wir an mehr als 120 biomolekularen\u2026<\/p>\n\t\t\t\t\t\t\t\t<\/div>\n\t\t\t\t<\/div>\n\t\t\t\t

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Performance Chemicals<\/p>\n\t\t\t\t\t\t\t\t<\/div>\n\t\t\t\t<\/div>\n\t\t\t\t

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Materialwissenschaft<\/h3>\t\t\t\t<\/div>\n\t\t\t\t<\/div>\n\t\t\t\t
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Wir entwickeln mit Ihnen Performance Chemicals zur Verbesserung Ihrer Materialien, Kunststoffe, Beschichtungen, Farbstoffe und Druckfarben\u2026<\/p>\n\t\t\t\t\t\t\t\t<\/div>\n\t\t\t\t<\/div>\n\t\t\t\t

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Interessiert?<\/h3>\t\t\t\t<\/div>\n\t\t\t\t<\/div>\n\t\t\t\t
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Als ein europaweit f\u00fchrendes und unabh\u00e4ngiges Auftragsforschungsunternehmen (CRO) bieten wir Ihnen das gesamte Spektrum der (metall)organischen Synthesechemie.<\/h3>\t\t\t\t<\/div>\n\t\t\t\t<\/div>\n\t\t\t\t
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Wir praktizieren einen pragmatischen sowie kundenorientierten Ansatz, um die Erwartungen an uns trotz h\u00f6chster Herausforderungen zu \u00fcbertreffen. Unsere erfahrenen Chemiker sind geschult, wirtschaftliche, \u00f6kologische sowie sicherheitstechnische Bedingungen f\u00fcr alle Phasen des Projekts zu evaluieren.<\/p>\n\t\t\t\t\t\t\t\t<\/div>\n\t\t\t\t<\/div>\n\t\t\t\t

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Dario Valenti, Stanimira Hristeva, Dimitrios Tzalis, and Christian Ottmann
\nEur. J. Med. Chem., Apr. 2019, 167, pp 76-95, DOI: 10.1016\/j.ejmech.2019.01.084;<\/p>\n","protected":false},"author":6,"featured_media":0,"comment_status":"closed","ping_status":"closed","sticky":false,"template":"","format":"standard","meta":{"site-sidebar-layout":"default","site-content-layout":"","ast-site-content-layout":"default","site-content-style":"default","site-sidebar-style":"default","ast-global-header-display":"","ast-banner-title-visibility":"","ast-main-header-display":"","ast-hfb-above-header-display":"","ast-hfb-below-header-display":"","ast-hfb-mobile-header-display":"","site-post-title":"","ast-breadcrumbs-content":"","ast-featured-img":"","footer-sml-layout":"","theme-transparent-header-meta":"default","adv-header-id-meta":"","stick-header-meta":"","header-above-stick-meta":"","header-main-stick-meta":"","header-below-stick-meta":"","astra-migrate-meta-layouts":"default","ast-page-background-enabled":"default","ast-page-background-meta":{"desktop":{"background-color":"var(--ast-global-color-4)","background-image":"","background-repeat":"repeat","background-position":"center center","background-size":"auto","background-attachment":"scroll","background-type":"","background-media":"","overlay-type":"","overlay-color":"","overlay-opacity":"","overlay-gradient":""},"tablet":{"background-color":"","background-image":"","background-repeat":"repeat","background-position":"center center","background-size":"auto","background-attachment":"scroll","background-type":"","background-media":"","overlay-type":"","overlay-color":"","overlay-opacity":"","overlay-gradient":""},"mobile":{"background-color":"","background-image":"","background-repeat":"repeat","background-position":"center center","background-size":"auto","background-attachment":"scroll","background-type":"","background-media":"","overlay-type":"","overlay-color":"","overlay-opacity":"","overlay-gradient":""}},"ast-content-background-meta":{"desktop":{"background-color":"var(--ast-global-color-5)","background-image":"","background-repeat":"repeat","background-position":"center center","background-size":"auto","background-attachment":"scroll","background-type":"","background-media":"","overlay-type":"","overlay-color":"","overlay-opacity":"","overlay-gradient":""},"tablet":{"background-color":"var(--ast-global-color-5)","background-image":"","background-repeat":"repeat","background-position":"center center","background-size":"auto","background-attachment":"scroll","background-type":"","background-media":"","overlay-type":"","overlay-color":"","overlay-opacity":"","overlay-gradient":""},"mobile":{"background-color":"var(--ast-global-color-5)","background-image":"","background-repeat":"repeat","background-position":"center center","background-size":"auto","background-attachment":"scroll","background-type":"","background-media":"","overlay-type":"","overlay-color":"","overlay-opacity":"","overlay-gradient":""}},"footnotes":""},"categories":[23],"tags":[],"class_list":["post-4682","post","type-post","status-publish","format-standard","hentry","category-publikationen"],"_links":{"self":[{"href":"https:\/\/www.tarosdiscovery.com\/de\/wp-json\/wp\/v2\/posts\/4682","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/www.tarosdiscovery.com\/de\/wp-json\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/www.tarosdiscovery.com\/de\/wp-json\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/www.tarosdiscovery.com\/de\/wp-json\/wp\/v2\/users\/6"}],"replies":[{"embeddable":true,"href":"https:\/\/www.tarosdiscovery.com\/de\/wp-json\/wp\/v2\/comments?post=4682"}],"version-history":[{"count":0,"href":"https:\/\/www.tarosdiscovery.com\/de\/wp-json\/wp\/v2\/posts\/4682\/revisions"}],"wp:attachment":[{"href":"https:\/\/www.tarosdiscovery.com\/de\/wp-json\/wp\/v2\/media?parent=4682"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/www.tarosdiscovery.com\/de\/wp-json\/wp\/v2\/categories?post=4682"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/www.tarosdiscovery.com\/de\/wp-json\/wp\/v2\/tags?post=4682"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}