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 == | ||
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{{#tree:id=OrganizedByTopic|openlevels=0| | {{#tree:id=OrganizedByTopic|openlevels=0| | ||
*Glucocorticoid receptor DBD domain | *Glucocorticoid receptor residues 89-158 | ||
**[[5va7]], [[5va0]] - hGCR + DNA – human<br /> | |||
*Glucocorticoid receptor DBD domain residues 391-480 | |||
**[[1gdc]], [[2gda]], [[1rgd]] – rGCR DBD – NMR – rat<br /> | **[[1gdc]], [[2gda]], [[1rgd]] – rGCR DBD – NMR – rat<br /> | ||
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**[[5cc1]] - hGCR DBD (mutant) + DNA <br /> | **[[5cc1]] - hGCR DBD (mutant) + DNA <br /> | ||
*Glucocorticoid receptor LBD domain | *Glucocorticoid receptor LBD domain residues 500-777 complex with NCOA peptide | ||
**[[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 /> | **[[4udc]], [[4udd]] - hGCR LBD (mutant) + NCOA2 peptide <br /> | ||
**[[1m2z]], [[3cld]], [[3bqd]], [[4lsj]], [[4p6w]], [[4p6x]] - hGCR LBD (mutant) + NCOA2 peptide + steroid <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 /> | **[[3e7c]], [[4csj]], [[5g3j]], [[5g5w]], [[5g3j]] - hGCR LBD (mutant) + NCOA2 peptide + non-steroidal agonist<br /> | ||
**[[3k23]] - hGCR LBD (mutant) + NCOA2 peptide + prolinamide<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 /> | **[[3gn8]] - hGCR LBD + NCOA2 peptide + steroid<br /> | ||
**[[4e2j]] - GCR LBD ancestral + NCOA2 peptide + steroid<br /> | **[[4e2j]] - GCR LBD ancestral + NCOA2 peptide + steroid<br /> | ||
**[[3mne]], [[3mno]], [[3mnp]] - GCR LBD (mutant) + 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 /> | |||
*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]] | ||
Revision as of 09:43, 30 May 2018
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[1].
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)[2].
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.
Rat glucocorticoid receptor DNA-binding domain dimer complex with DNA and Zn+2 ions (grey) (PDB entry 3g6r)
Drag the structure with the mouse to rotate 3D structures of glucocorticoid receptor
3D structures of glucocorticoid receptor Updated on 30-May-2018
References
References - ↑ 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
- ↑ 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
