ADMS 3502 Study Guide - Final Guide: Rosiglitazone, Peroxisome Proliferator-Activated Receptor Gamma, Endocrinology

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Causes cushing"s syndrome which is characterized by obesity, buffalo hump and osteoporosis: liver x receptor, 24, 25-epoxycholesterol & 17-hydroxycholesterol. Require only the non-rxr ligand to be present . Zinc fingers are the most characteristic motifs in the steroid receptor superfamily and are regulated for dna binding. Agonist exposes the nr box on the af2 helix in the lbd. This promotes interactions w coactivator & disrupts interactions w corepressor. Some coactivators possess hat activity and can recruit other hat proteins. Hat (histone acetyltransferase) causes histone acetylation and methylation. This opens up the condensed chromatin and allows access to transcription factors. 2. a) group 1 nr1 -heterodimers w rxr (adopted orphans) tr, ppar, lxr, fxr, vdr, 2. b) group 2 nr2 -heterodimer partner to group 1 nrs rxr / / . Group 1 & 2 bind low affinity ligands like fatty acids, cholesterol metabolites, vitamins etc. Group 3 nr3 -homodimers (classic receptor) er, mr, pr, ar, binds high affinity ligands like steroids.

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