Glucocorticoid receptor

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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]] }}
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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=''>
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== Function ==
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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==
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'''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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'''Glucocorticoid receptor DBD domain'''
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See also:
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*[[Glucocorticoids]]
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*[[Intracellular receptors]]
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*[[Steroid Hormones and their receptors]].
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[[1gdc]], [[2gda]], [[1rgd]] – rGCR DBD – NMR – rat<br />
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== Relevance ==
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[[3g9p]], [[3fyl]], [[3g6p]], [[3g6q]], [[3g6r]], [[3g6t]], [[3g6u]], [[3g8u]], [[3g8x]], [[3g97]], [[3g99]], [[3g9i]], [[3g9m]], [[3g9j]], [[3g9o]], [[1glu]], [[1lat]], [[1r4o]], [[1r4r]] - rGCR DBD + DNA
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'''Glucocorticoid receptor LBD domain'''
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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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[[1m2z]], [[3cld]] - hGCR LBD (mutant) + NCOA2 peptide + steroid - human<br />
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== Disease ==
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[[3e7c]] - hGCR LBD (mutant) + NCOA2 peptide + non-steroid<br />al agonist
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[[3k23]] - hGCR LBD (mutant) + NCOA2 peptide + prolinamide<br />
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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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[[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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== Structural highlights ==
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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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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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[[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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<scene name='96/962959/Tert/1'>Glucocorticoid Receptor in complex with budesonide</scene> ([[5nfp]]).
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<scene name='96/962959/Binding_site/1'>Budesonide binding site</scene>. Water molecule is shown as red sphere.
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<scene name='97/973067/Overall/1'>Crystal Structure of mometasone furoate-bound glucocorticoid receptor ligand binding domain</scene> ([[4p6w]]).
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<scene name='97/973067/Binding_site/1'>Mometasone furoate binding site</scene>.
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==3D structures of glucocorticoid receptor==
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[[Glucocorticoid receptor 3D structures]]
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'''Glucocorticoid receptor LBD+hinge domains'''
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</StructureSection>
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[[1nhz]] – hGCR LBD+hinge (mutant) + steroid<br />
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== References ==
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[[1p93]] - hGCR LBD+hinge (mutant) + NCOA2 peptide + steroid<br />
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<references/>
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[[Category:Topic Page]]

Current revision

Rat glucocorticoid receptor DNA-binding domain dimer complex with DNA and Zn+2 ions (grey) (PDB entry 3g6r)

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References

  1. ↑ Lu NZ, Wardell SE, Burnstein KL, Defranco D, Fuller PJ, Giguere V, Hochberg RB, McKay L, Renoir JM, Weigel NL, Wilson EM, McDonnell DP, Cidlowski JA. International Union of Pharmacology. LXV. The pharmacology and classification of the nuclear receptor superfamily: glucocorticoid, mineralocorticoid, progesterone, and androgen receptors. Pharmacol Rev. 2006 Dec;58(4):782-97. PMID:17132855 doi:http://dx.doi.org/10.1124/pr.58.4.9
  2. ↑ Finsterwald C, Alberini CM. Stress and glucocorticoid receptor-dependent mechanisms in long-term memory: from adaptive responses to psychopathologies. Neurobiol Learn Mem. 2014 Jul;112:17-29. doi: 10.1016/j.nlm.2013.09.017. Epub, 2013 Oct 7. PMID:24113652 doi:http://dx.doi.org/10.1016/j.nlm.2013.09.017
  3. ↑ Selroos O, Edsbäcker S, Hultquist C. Once-daily inhaled budesonide for the treatment of asthma: clinical evidence and pharmacokinetic explanation. J Asthma. 2004;41(8):771-90. PMID:15641626 doi:10.1081/jas-200038344

Proteopedia Page Contributors and Editors (what is this?)

Michal Harel, Alexander Berchansky

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