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| {{STRUCTURE_3g6r| PDB=3g6r | SIZE=400| SCENE= |right| CAPTION= Rat glucocorticoid receptor DNA-binding domain dimer complex with DNA and Zn+2 ions (grey), [[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=''> |
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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. | |
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| ==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>. |
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| | See also: |
| | *[[Glucocorticoids]] |
| | *[[Intracellular receptors]] |
| | *[[Steroid Hormones and their receptors]]. |
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| | == Relevance == |
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| | 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>. |
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| | == Disease == |
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| | [[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>. |
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| | == Structural highlights == |
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| | 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]]). |
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| Updated on {{REVISIONDAY2}}-{{MONTHNAME|{{REVISIONMONTH}}}}-{{REVISIONYEAR}}
| | <scene name='96/962959/Tert/1'>Glucocorticoid Receptor in complex with budesonide</scene> ([[5nfp]]). |
| {{#tree:id=OrganizedByTopic|openlevels=0|
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| *Glucocorticoid receptor DBD domain
| | <scene name='96/962959/Binding_site/1'>Budesonide binding site</scene>. Water molecule is shown as red sphere. |
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| **[[1gdc]], [[2gda]], [[1rgd]] – rGCR DBD – NMR – rat<br />
| | <scene name='97/973067/Overall/1'>Crystal Structure of mometasone furoate-bound glucocorticoid receptor ligand binding domain</scene> ([[4p6w]]). |
| **[[3g9p]], [[3fyl]], [[3g6p]], [[3g6q]], [[3g6r]], [[3g6t]], [[3g6u]], [[3g8u]], [[3g8x]], [[3g97]], [[3g99]], [[3g9i]], [[3g9m]], [[3g9j]], [[3g9o]], [[1glu]], [[1lat]], [[1r4o]], [[1r4r]] - rGCR DBD + DNA<br />
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| **[[4hn5]], [[4hn6]] - hGCR DBD + DNA – human<br />
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| *Glucocorticoid receptor LBD domain
| | <scene name='97/973067/Binding_site/1'>Mometasone furoate binding site</scene>. |
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| **[[1m2z]], [[3cld]], [[3bqd]], [[4lsj]], [[4p6w]], [[4p6x]] - hGCR LBD (mutant) + NCOA2 peptide + steroid <br />
| | ==3D structures of glucocorticoid receptor== |
| **[[3e7c]], [[4csj]] - hGCR LBD (mutant) + NCOA2 peptide + non-steroidal agonist<br />
| | [[Glucocorticoid receptor 3D structures]] |
| **[[4mdd]] - hGCR LBD (mutant) + NCOA1 peptide + non-steroidal agonist<br />
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| **[[3k23]] - hGCR LBD (mutant) + NCOA2 peptide + prolinamide<br />
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| **[[3k22]] - hGCR LBD (mutant) + transcriptional intermediary factor 2 peptide + alaninamide<br />
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| **[[3h52]] - hGCR LBD (mutant) + NCOA1 peptide + steroid<br />
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| **[[3gn8]] - hGCR LBD + NCOA2 peptide + steroid<br />
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| **[[3ry9]] - GCR LBD ancestral + steroid<br />
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| **[[4e2j]] - GCR LBD ancestral + NCOA2 peptide + steroid<br />
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| **[[3mne]], [[3mno]], [[3mnp]] - GCR LBD (mutant) + NCOA2 peptide + steroid<br /> – mouse
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| *Glucocorticoid receptor LBD+hinge domains
| | </StructureSection> |
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| **[[1nhz]] – hGCR LBD+hinge (mutant) + steroid<br />
| | == References == |
| **[[1p93]] - hGCR LBD+hinge (mutant) + NCOA2 peptide + steroid<br />
| | <references/> |
| }}
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| [[Category:Topic Page]] | | [[Category:Topic Page]] |