{"id":61929,"date":"2018-03-09T22:49:48","date_gmt":"2018-03-09T22:49:48","guid":{"rendered":"https:\/\/www.deberes.net\/tesis\/sin-categoria\/diseno-sa%c2%adntesis-y-actividad-biologica-de-un-nuevo-ligando-superagonista-amcr277a-del-receptor-nuclear-de-la-vitamina-d\/"},"modified":"2018-03-09T22:49:48","modified_gmt":"2018-03-09T22:49:48","slug":"diseno-sa%c2%adntesis-y-actividad-biologica-de-un-nuevo-ligando-superagonista-amcr277a-del-receptor-nuclear-de-la-vitamina-d","status":"publish","type":"post","link":"https:\/\/www.deberes.net\/tesis\/santiago-de-compostela\/diseno-sa%c2%adntesis-y-actividad-biologica-de-un-nuevo-ligando-superagonista-amcr277a-del-receptor-nuclear-de-la-vitamina-d\/","title":{"rendered":"Dise\u00f1o, s\u00edntesis y actividad biol\u00f3gica de un nuevo ligando superagonista (amcr277a) del receptor nuclear de la vitamina d"},"content":{"rendered":"<h2>Tesis doctoral de <strong> Cezar Rodrigues Luis <\/strong><\/h2>\n<p>Omando como base la superposici\u00f3n de las estructuras cristalinas de los complejos formados por el receptor mutado de moras (moras-vdr) con los superagonistas (mc1288 y kh1060) y la hormona natural calcitriol, se ha dise\u00f1ado el nuevo an\u00e1logo de la vitamina d \u00abamcr277a\u00bb. Los c\u00e1lculos de docking indican que este nuevo an\u00e1logo se enlaza mejor al vdr mutado de moras que la propia hormona natural. Con el objeto de conocer su actividad biol\u00f3gica, se realiz\u00f3 su s\u00edntesis v\u00eda ruta wittig-horner. Los ensayos biol\u00f3gicos demuestran que el nuevo compuesto se comporta como un nuevo superagonista del calcitriol (elevada acci\u00f3n en la transactivaci\u00f3n y en la inhibici\u00f3n de la proliferaci\u00f3n de c\u00e9lulas tumorales) de potencial inter\u00e9s cl\u00ednico. La estructura cristalina del complejo formada por amcr277a y el receptor vdr-moras explica bien la elevada afinidad del nuevo ligando por el receptor. El trabajo ha sido objeto de una patente internacional (authors: moras d, mouri\u00f1o a, rodrigues lc, rochel n, wurtz jl. Title: preparation of vitamin d derivatives as vitamin d receptor agonists. Register: pct int. Appl. (2007<\/p>\n<p>&nbsp;<\/p>\n<h3>Datos acad\u00e9micos de la tesis doctoral \u00ab<strong>Dise\u00f1o, s\u00edntesis y actividad biol\u00f3gica de un nuevo ligando superagonista (amcr277a) del receptor nuclear de la vitamina d<\/strong>\u00ab<\/h3>\n<ul>\n<li><strong>T\u00edtulo de la tesis:<\/strong>\u00a0 Dise\u00f1o, s\u00edntesis y actividad biol\u00f3gica de un nuevo ligando superagonista (amcr277a) del receptor nuclear de la vitamina d <\/li>\n<li><strong>Autor:<\/strong>\u00a0 Cezar Rodrigues Luis <\/li>\n<li><strong>Universidad:<\/strong>\u00a0 Santiago de compostela<\/li>\n<li><strong>Fecha de lectura de la tesis:<\/strong>\u00a0 14\/12\/2007<\/li>\n<\/ul>\n<p>&nbsp;<\/p>\n<h3>Direcci\u00f3n y tribunal<\/h3>\n<ul>\n<li><strong>Director de la tesis<\/strong>\n<ul>\n<li>Antonio Mouri\u00f1o Mosquera<\/li>\n<\/ul>\n<\/li>\n<li><strong>Tribunal<\/strong>\n<ul>\n<li>Presidente del tribunal: Guillermo Mart\u00ednez Massanet <\/li>\n<li>Francisco Foubelo (vocal)<\/li>\n<li>Miguel Card\u00e1 Us\u00f3 (vocal)<\/li>\n<li>Marisa Artmann (vocal)<\/li>\n<\/ul>\n<\/li>\n<\/ul>\n<p>&nbsp;<\/p>\n","protected":false},"excerpt":{"rendered":"<p>Tesis doctoral de Cezar Rodrigues Luis Omando como base la superposici\u00f3n de las estructuras cristalinas de los complejos formados por [&hellip;]<\/p>\n","protected":false},"author":1,"featured_media":0,"comment_status":"open","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"site-sidebar-layout":"default","site-content-layout":"","ast-site-content-layout":"","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":"","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 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