Glucocorticoid receptor: Difference between revisions

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Michal Harel, Alexander Berchansky

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-{{STRUCTURE_3g6r|  PDB=3g6r  | SIZE=400| SCENE= |right|   CAPTION= Rat glucocorticoid receptor DNA-binding domain complex with DNA and Zn+2 ions, [[3g6r]] }}
+<StructureSection load='3g6r' size='350' side='right' caption='Rat glucocorticoid receptor DNA-binding domain dimer complex with DNA and Zn+2 ions (grey) (PDB entry [[3g6r]])' scene=''>
-<!--
+== Function ==
-Please use the "3D" button above this box to insert a Jmol applet (molecule) on this page.
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-'''Glucocorticoid receptor''' (GCR) is the nuclear receptor binding cortisol and glucocorticoids.  GCR regulates genes involved in development, metabolism and immune response.  The glucocorticoid-bound GCR can either up-regulate the expression of anti-inflammatory proteins (transactivation) or repress the expression of pro-inflammatory proteins (transrepression).  GCR contains 5 domains: N terminal regulatory domain; DNA-binding domain (DBD); hinge region; ligand-binding domain (LBD) and C terminal domain.  GCR interacts with nuclear receptor coactivator 2 (NCOA2) which promotes DNA transcription by acylating histones.
-==3D structures of glucocorticoid receptor==
+'''Glucocorticoid receptor''' (GCR) is the [[Nuclear receptors|nuclear receptor]] binding cortisol and [[glucocorticoids]].  GCR regulates genes involved in development, metabolism and immune response.  GCR interacts with nuclear receptor coactivator 2 (NCOA2) which promotes DNA transcription by acylating histones<ref>PMID:17132855</ref>.
+See also:
+*[[Glucocorticoids]]
+*[[Intracellular receptors]]
+*[[Steroid Hormones and their receptors]].
+== Relevance ==
+The glucocorticoid-bound GCR can either up-regulate the expression of anti-inflammatory proteins (transactivation) or repress the expression of pro-inflammatory proteins (transrepression)<ref>PMID:24113652</ref>.
+== Disease ==
+[[Budesonide]] is an agonist of GCR and is used as medication for asthma and inflammatory bowel diseases like chronic obstructive pulmonary disease<ref>PMID:15641626</ref>.
+== Structural highlights ==
+GCR contains 5 domains: N terminal regulatory domain; DNA-binding domain (DBD) residues 417-506; hinge region; ligand-binding domain (LBD) residues 521-777 and C terminal domain. <scene name='89/895670/Cv/4'>Human glucocorticoid receptor ligand-binding domain bound to dexamethasone</scene> ([[1m2z]]).
-'''Glucocorticoid receptor DBD domain'''
+<scene name='96/962959/Tert/1'>Glucocorticoid Receptor in complex with budesonide</scene> ([[5nfp]]).
-[[1gdc]], [[2gda]], [[1rgd]] – rGCR DBD – NMR – rat<br />
+<scene name='96/962959/Binding_site/1'>Budesonide binding site</scene>. Water molecule is shown as red sphere.
-[[3g9p]], [[3fyl]], [[3g6p]], [[3g6q]], [[3g6r]], [[3g6t]], [[3g6u]], [[3g8u]], [[3g8x]], [[3g97]], [[3g99]], [[3g9i]], [[3g9m]], [[3g9j]], [[3g9o]], [[1glu]], [[1lat]], [[1r4o]], [[1r4r]] - rGCR DBD + DNA
-'''Glucocorticoid receptor LBD domain'''
+<scene name='97/973067/Overall/1'>Crystal Structure of mometasone furoate-bound glucocorticoid receptor ligand binding domain</scene> ([[4p6w]]).
-[[1m2z]], [[3cld]] - hGCR LBD (mutant) + NCOA2 peptide + steroid - human<br />
+<scene name='97/973067/Binding_site/1'>Mometasone furoate binding site</scene>.
-[[3e7c]] - hGCR LBD (mutant) + NCOA2 peptide + non-steroid<br />al agonist
-[[3k23]] - hGCR LBD (mutant) + NCOA2 peptide + prolinamide<br />
-[[3k22]] - hGCR LBD (mutant) + transcriptional intermediary factor 2  peptide + alaninamide<br />
-[[3h52]] - hGCR LBD (mutant) + NCOA1 peptide + steroid<br />
-[[3gn8]] - hGCR LBD + NCOA2 peptide + steroid<br />
-[[3ry9]] - GCR LBD ancestral + steroid<br />
-[[4e2j]] - GCR LBD ancestral + NCOA2 peptide + steroid<br />
-[[3mne]], [[3mno]], [[3mnp]] - GCR LBD (mutant) + NCOA2 peptide + steroid<br /> – mouse
-'''Glucocorticoid receptor LBD+hinge domains'''
+==3D structures of glucocorticoid receptor==
+[[Glucocorticoid receptor 3D structures]]
-[[1nhz]] – hGCR LBD+hinge (mutant) + steroid<br />
+</StructureSection>
-[[1p93]] - hGCR LBD+hinge (mutant) + NCOA2 peptide + steroid<br />
+== References ==
+<references/>
 [[Category:Topic Page]]