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Glucocorticoid receptor: Difference between revisions

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*<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=''>
<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 ==
== Function ==


'''Glucocorticoid receptor''' (GCR) is the 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>.
'''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 ==
== 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>.
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>.


== Structural highlights ==
== Disease ==


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.
[[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>.


==3D structures of glucocorticoid receptor==
== Structural highlights ==
[[Glucocorticoid receptor 3D structures]]


</StructureSection>
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]]).
==3D structures of glucocorticoid receptor==


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|


*Glucocorticoid receptor residues 89-158
<scene name='96/962959/Binding_site/1'>Budesonide binding site</scene>. Water molecule is shown as red sphere.


**[[5va7]], [[5va0]] - hGCR + DNA – human<br />
<scene name='97/973067/Overall/1'>Crystal Structure of mometasone furoate-bound glucocorticoid receptor ligand binding domain</scene> ([[4p6w]]).


*Glucocorticoid receptor DBD domain residues 391-480
<scene name='97/973067/Binding_site/1'>Mometasone furoate binding site</scene>.


**[[6cfn]] - hGCR DBD <br />
==3D structures of glucocorticoid receptor==
**[[4hn5]], [[4hn6]], [[5emp]], [[5emq]], [[5emc]], [[5e69]], [[5e6a]], [[5e6b]], [[5e6c]], [[5e6d]], [[5cbx]], [[5cby]], [[5cbz]], [[6bqu]] - hGCR DBD + DNA<br />
[[Glucocorticoid receptor 3D structures]]
**[[5cc1]] - hGCR DBD (mutant) + DNA <br />
**[[1gdc]], [[2gda]], [[1rgd]] – rGCR DBD – NMR – rat<br />
**[[3g9p]], [[3fyl]], [[3g6p]], [[3g6q]], [[3g6r]], [[3g6t]], [[3g6u]], [[3g8u]], [[3g8x]], [[3g97]], [[3g99]], [[3g9i]], [[3g9m]], [[3g9j]], [[3g9o]], [[1glu]], [[1lat]], [[1r4o]], [[1r4r]] - rGCR DBD + DNA<br />


*Glucocorticoid receptor LBD domain residues 500-777 complex with NCOA peptide
</StructureSection>
 
**[[4mdd]] - hGCR LBD (mutant) + NCOA1 peptide + non-steroidal agonist<br />
**[[3h52]] - hGCR LBD (mutant) + NCOA1 peptide + steroid<br />
**[[4udc]], [[4udd]] - hGCR LBD (mutant) + NCOA2 peptide <br />
**[[1m2z]], [[3cld]], [[3bqd]], [[4lsj]], [[4p6w]], [[4p6x]], [[1p93]] - hGCR LBD (mutant) + NCOA2 peptide + steroid <br />
**[[3e7c]], [[4csj]], [[5g3j]], [[5g5w]], [[5g3j]] - hGCR LBD (mutant) + NCOA2 peptide + non-steroidal agonist<br />
**[[3k23]] - hGCR LBD (mutant) + NCOA2 peptide + prolinamide<br />
**[[6el9]], [[6el6]], [[6el7]], [[5nft]] - hGCR LBD + NCOA2 peptide + modulator<br />
**[[5nfp]] - hGCR LBD + NCOA2 peptide + drug<br />
**[[3gn8]] - hGCR LBD + NCOA2 peptide + steroid<br />
**[[4e2j]] - GCR LBD ancestral + NCOA2 peptide + steroid<br />
**[[3mne]], [[3mno]], [[3mnp]] - GCR LBD (mutant) + NCOA2 peptide + steroid – mouse<br />
 
*Glucocorticoid receptor LBD domain other complexes
 
**[[3ry9]] - anGCR LBD ancestral + steroid<br />
**[[1nhz]] – hGCR LBD (mutant) + steroid<br />
**[[5uc3]] - hGCR LBD (mutant) + RU-486<br />
**[[3k22]] - hGCR LBD (mutant) + transcriptional intermediary factor 2  peptide + alaninamide<br />
**[[6dxk]] – hGCR LBD + antagonist<br />
 
*Glucocorticoid receptor 2
 
**[[5ufs]] – anGCR2 LBD + SHP coregulatory + triamcinolone acetonide <br />
**[[4e2j]] – anGCR2 LBD ancestral + NCOA2 peptide + steroid<br />
**[[5uc1]] – GCR2 LBD + RU-486 – ''Heterocephalus glaber''<br />


}}
== References ==
== References ==
<references/>
<references/>
[[Category:Topic Page]]
[[Category:Topic Page]]

Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)

Michal Harel, Alexander Berchansky
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