{"id":4688,"date":"2019-02-01T11:40:40","date_gmt":"2019-02-01T10:40:40","guid":{"rendered":"https:\/\/www.tarosdiscovery.com\/unkategorisiert\/dpd-inspired-discovery-of-novel-lsrk-kinase-inhibitors-an-opportunity-to-fight-antimicrobial-resistance\/"},"modified":"2024-01-26T10:58:59","modified_gmt":"2024-01-26T09:58:59","slug":"dpd-inspired-discovery-of-novel-lsrk-kinase-inhibitors-an-opportunity-to-fight-antimicrobial-resistance","status":"publish","type":"post","link":"https:\/\/www.tarosdiscovery.com\/de\/news\/dpd-inspired-discovery-of-novel-lsrk-kinase-inhibitors-an-opportunity-to-fight-antimicrobial-resistance-2\/","title":{"rendered":"DPD-Inspired Discovery of Novel LsrK Kinase Inhibitors: An Opportunity To Fight Antimicrobial Resistance"},"content":{"rendered":"\t\t
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DPD-Inspired Discovery of Novel LsrK Kinase Inhibitors: An Opportunity To Fight Antimicrobial Resistance<\/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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Silvia Stotani, Viviana Gatta, Prasanthi Medarametla, Mohan Padmanaban, Anna Karawajczyk, Fabrizio Giordanetto, P\u00e4ivi Tammela, Tuomo Laitinen, Antti Poso, Dimitros Tzalis, and Simona Collina<\/p>\n

J. Med. Chem., Feb. 2019,\u00a0\u00a0DOI: 10.1021\/acs.jmedchem.9b00025;<\/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

Antibiotic resistance is posing a continuous threat to global public health and represents a huge burden for society as a whole. In the past decade, the interference with bacterial quorum sensing (QS) (i.e., cell\u2013cell communication) mechanisms has extensively been investigated as a valid therapeutic approach in the pursuit of a next generation of antimicrobials. (S)-4,5-Dihydroxy-2,3-pentanedione, commonly known as (S)-DPD, a small signaling molecule that modulates QS in both Gram-negative and Gram-positive bacteria, is phosphorylated by LsrK, and the resulting phospho-DPD activates QS. We designed and prepared a small library of DPD derivatives, characterized by five different scaffolds, and evaluated their LsrK inhibition in the context of QS interference. SAR studies highlighted the pyrazole moiety as an essential structural element for LsrK inhibition. Particularly, four compounds were found to be micromolar LsrK inhibitors (IC50ranging between 100 \u03bcM and 500 \u03bcM) encouraging further exploration of novel analogues as potential new antimicrobials.<\/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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Silvia Stotani, Viviana Gatta, Prasanthi Medarametla, Mohan Padmanaban, Anna Karawajczyk, Fabrizio Giordanetto, P\u00e4ivi Tammela,…
\nJ. Med. Chem., Feb. 2019, DOI: 10.1021\/acs.jmedchem.9b00025;<\/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-4688","post","type-post","status-publish","format-standard","hentry","category-publikationen"],"_links":{"self":[{"href":"https:\/\/www.tarosdiscovery.com\/de\/wp-json\/wp\/v2\/posts\/4688","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=4688"}],"version-history":[{"count":0,"href":"https:\/\/www.tarosdiscovery.com\/de\/wp-json\/wp\/v2\/posts\/4688\/revisions"}],"wp:attachment":[{"href":"https:\/\/www.tarosdiscovery.com\/de\/wp-json\/wp\/v2\/media?parent=4688"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/www.tarosdiscovery.com\/de\/wp-json\/wp\/v2\/categories?post=4688"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/www.tarosdiscovery.com\/de\/wp-json\/wp\/v2\/tags?post=4688"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}