2-11-2008 lecture part 1 - Nuclear receptor translocation...

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Nuclear receptor translocation is an important drug mechanism these are steroid hormone Nuclear receptor translocation into the nucleus is of impact for the pharmacology of common drugs: Upon ligand binding of i.e. cortisol at the nuclear receptor the protein is translocated from the cytoplasm to the nucleus . Nuclear receptors are transcription factors, which are activated by ligand binding or in other words: ligand binding to the receptor leads to transfer of the activated receptor into to the nucleus through the NPC. 1
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Nuclear receptor translocation is an important activation mechanism for steroid hormones Nuclear receptors are transcription factors, which are activated by ligand binding or in other words: ligand binding to the receptor leads to transfer of the activated receptor into the nucleus. The classical example is the action of steroid hormones (left). 2
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Nuclear receptor translocation is an important hormone/drug mechanism testosterone – estrogen – cortizol – VD – parathyroid – VA - retinoic acid need the NPC to enter the nuc Nuclear receptors are a family of intracellular receptors . Typical ligands working by nuclear receptors are: thyroid hormones , retinoic acid and steroids (cortisone!) and others (compare fig.) . Of note : the speed of drug action is slow compared to other drugs acting on i.e. seven transmembrane helix receptors (i.e. catecholamines), since these nuclear receptors act on the transcriptome level. Nuclear receptor translocation is an important hormone/drug mechanism Nuclear receptors are a family of intracellular receptors . An important drug target are the p eroxisome p roliferation a ctivating r eceptors ( PPARs ). Drugs acting on PPARs are i.e. the thiazolidinediones (TZD) derivatives ( glitazones ), which are important for the treatment of diabetes. 3
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Different lignad are used for different PPARs to influence the FA turn over by influencing transcription of the corresponding gene These are drug which bind to a certain rece ptn which then included in the nuc and then act on the transcription level Peroxisome-proliferator activator receptor ligands are important drugs for the treatment of diabetes 4
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This note was uploaded on 05/30/2010 for the course MEDICEN 2100 taught by Professor Saba during the Spring '10 term at Columbia State Community College.

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2-11-2008 lecture part 1 - Nuclear receptor translocation...

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