Glucocorticoid receptor
From Proteopedia
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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>. | ||
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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>. | ||
== Structural highlights == | == Structural highlights == | ||
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<scene name='96/962959/Binding_site/1'>Budesonide binding site</scene>. Water molecule is shown as red sphere. | <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>. | ||
==3D structures of glucocorticoid receptor== | ==3D structures of glucocorticoid receptor== | ||
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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
- ↑ 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
