Glucocorticoid receptor
From Wikipedia, the free encyclopedia
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Nuclear receptor subfamily 3, group C, member 1 (glucocorticoid receptor)
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| Identifiers | |
| Symbol | NR3C1 GCR, GCCR, GRL |
| HUGO | 7978 |
| Entrez | 2908 |
| OMIM | 138040 |
| RefSeq | NM_000176 |
| UniProt | P04150 |
| Other data | |
| Locus | Chr. 5 q31-32 |
The glucocorticoid receptor (GR) or nuclear receptor subfamily 3, group C, member 1 is a ligand-activated intracytoplasmatic transcription factor that interacts with high affinity to cortisol and other glucocorticoids.
The GR is controlled by gene NR3Cl on chromosome 5 (5q31).
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[edit] Structure
Like the other steroid receptors the structure of the GR consists of a variable domain, the DNA-binding domain with zinc fingers, a hinge region, and the hormone-binding domain with a final carboxy terminal.
[edit] Binding and response
Cortisol diffuses through the cell membrane into the cytoplasm and binds to the glucocorticoid receptor (GR) forming a GR-hormone complex. Initially the GR includes the heat shock protein 90 (hsp90), the heat shock protein 70 (hsp70) and the protein FKBP52 (FK506-binding protein 52). Dissociation of the GR complex releases the heat shock chaperones and yields the free cortisol-receptor subunits that link up as homodimers. These are translocated via nucleopores into the nucleus and bind with zinc fingers to the specific DNA responsive elements activating gene transcription. The biologic response depends on the cell type.
[edit] Agonists and antagonists
Relaxin is an agonist, and RU486 and cyproterone are antagonists of the GR. Also, progesterone and DHEA have antagonist effects on the GR.
The GR is abnormal in familial glucocorticoid resistance.[1]
[edit] References
- ^ Mendonca B, Leite M, de Castro M, Kino T, Elias L, Bachega T, Arnhold I, Chrousos G, Latronico A (2002). "Female pseudohermaphroditism caused by a novel homozygous missense mutation of the GR gene". J Clin Endocrinol Metab 87 (4): 1805-9. PMID 11932321.
[edit] External links
(A07EA, C05AA, D07, D10AA, H02, R01AD, R03BA, S01BA, S02B, and S03B)
Alclometasone, Aldosterone, Amcinonide, Beclometasone, Betamethasone, Budesonide, Ciclesonide, Clobetasol, Clobetasone, Clocortolone, Cloprednol, Cortisone, Cortivazol, Deflazacort, Deoxycorticosterone, Desonide, Desoximetasone, Desoxycortone, Dexamethasone, Diflorasone, Diflucortolone, Difluprednate, Fluclorolone, Fludrocortisone, Fludroxycortide, Flumetasone, Flunisolide, Fluocinolone acetonide, Fluocinonide, Fluocortin, Fluocortolone, Fluorometholone, Fluperolone, Fluprednidene, Fluticasone, Formocortal, Halcinonide, Halometasone, Hydrocortisone/cortisol, Hydrocortisone aceponate, Hydrocortisone buteprate, Hydrocortisone butyrate, Loteprednol, Medrysone, Meprednisone, Methylprednisolone, Methylprednisolone aceponate, Mometasone furoate, Paramethasone, Prednicarbate, Prednisone, Prednisolone, Prednylidene, Rimexolone, Tixocortol, Triamcinolone, Ulobetasol
CAP - CBF - E2F - KlF - Nanog - NF-kB - Oct-4 - P300/CBP - PIT-1 - Rho/Sigma - R-SMAD - Sox2 - Sp1 - STAT (STAT1, STAT3, STAT5)
Basic-helix-loop-helix: AhR - HIF - MYC - Twist - Myogenic regulatory factors (MyoD, Myogenin, MYF5, MYF6)
Basic leucine zipper: C/EBP - CREB - AP-1
Basic helix-loop-helix leucine zipper: MITF - SREBP
Nuclear receptors: subfamily 1 (Thyroid hormone, RAR, PPAR, LXR, FXR, Calcitriol, PXR, CAR) - subfamily 2 (HNF4, RXR) - subfamily 3/Steroid hormone (Estrogen, Estrogen related, Glucocorticoid, Mineralocorticoid, Progesterone, Androgen) - subfamily 0 (NR0B1)
