{"id":4668,"date":"2019-09-18T12:25:53","date_gmt":"2019-09-18T10:25:53","guid":{"rendered":"https:\/\/www.tarosdiscovery.com\/unkategorisiert\/set-up-and-screening-of-a-fragment-library-targeting-the-14-3-3-protein-interface\/"},"modified":"2024-01-26T10:34:51","modified_gmt":"2024-01-26T09:34:51","slug":"set-up-and-screening-of-a-fragment-library-targeting-the-14-3-3-protein-interface","status":"publish","type":"post","link":"https:\/\/www.tarosdiscovery.com\/de\/set-up-and-screening-of-a-fragment-library-targeting-the-14-3-3-protein-interface\/","title":{"rendered":"Set-up and screening of a fragment library targeting the 14-3-3 protein interface"},"content":{"rendered":"\t\t
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Set-up and screening of a fragment library targeting the 14-3-3 protein interface<\/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, Jo\u00e3o Filipe Neves, Fran\u00e7ois-Xavier Cantrelle, Stanimira Hristeva, Domenico Lentini Santo, Tom\u00e1\u0161 Ob\u0161il, Xavier Hanoulle, Laura M. Levy, Dimitrios Tzalis, Isabelle Landrieu, Christian Ottmann<\/h3>\n

Med. Chem. Commun., Jul 2019, DOI:10.1039\/C9MD00215D<\/h3>\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\u2013protein interactions (PPIs) are at the core of regulation mechanisms in biological systems and consequently became an attractive target for therapeutic intervention. PPIs involving the adapter protein 14-3-3 are representative examples given the broad range of partner proteins forming a complex with one of its seven human isoforms. Given the challenges represented by the nature of these interactions, fragment-based approaches offer a valid alternative for the development of PPI modulators. After having assembled a fragment set tailored on PPIs\u2019 modulation, we started a screening campaign on the sigma isoform of 14-3-3 adapter proteins. Through the use of both mono- and bi-dimensional nuclear magnetic resonance spectroscopy measurements, coupled with differential scanning fluorimetry, three fragment hits were identified. These molecules bind the protein at two different regions distant from the usual binding groove highlighting new possibilities for selective modulation of 14-3-3 complexes.<\/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, Jo\u00e3o Filipe Neves, Fran\u00e7ois-Xavier Cantrelle, Stanimira Hristeva, Domenico Lentini Santo, Tom\u00e1\u0161 Ob\u0161il, Xavier Hanoulle, Laura M. Levy, Dimitrios Tzalis, Isabelle Landrieu, Christian Ottmann
\nMed. Chem. Commun., Jul 2019, DOI:10.1039\/C9MD00215D<\/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-4668","post","type-post","status-publish","format-standard","hentry","category-publikationen"],"_links":{"self":[{"href":"https:\/\/www.tarosdiscovery.com\/de\/wp-json\/wp\/v2\/posts\/4668","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=4668"}],"version-history":[{"count":0,"href":"https:\/\/www.tarosdiscovery.com\/de\/wp-json\/wp\/v2\/posts\/4668\/revisions"}],"wp:attachment":[{"href":"https:\/\/www.tarosdiscovery.com\/de\/wp-json\/wp\/v2\/media?parent=4668"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/www.tarosdiscovery.com\/de\/wp-json\/wp\/v2\/categories?post=4668"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/www.tarosdiscovery.com\/de\/wp-json\/wp\/v2\/tags?post=4668"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}