Glucocorticoid receptors structure

The individual domains of the two receptors both have structures similar to that of the glucocorticoid receptor, and they bind to DNA in a similar way, with their recognition helices in the major groove. The dimer contacts are, however, totally different. In the glucocorticoid receptor, which binds to a palindromic DNA sequence like the 434 repressor described in Chapter 8, the domains interact symmetrically in a head-to-head fashion equivalent... 

Hard, T., et al. Solution structure of the glucocorticoid receptor DNA-binding domain. Science 249 157-160, 1990. 

Hollenberg SM, Weinberger C, Ong ES et al (1985) Primary structure and expression of a functional human glucocorticoid receptor cDNA. Nature 318 635-641... 

Arriza, J. L., Weinberger, C., Cerelli, G. et al. Cloning of the human mineralocorticoid receptor complementary DNA Structural and functional kinship with the glucocorticoid receptor. Science 237 268-275,1987. 

Encio IJ, Detera-Wadleigh SD. (1991) The genomic structure of the human glucocorticoid receptor. J Biol Chem. 266, 7182-7188. 

Glucocorticoid receptors are present in a high density in the amygdala and neuroimaging studies have shown that the amygdala is the only structure in which the regional blood flow and glucose metabolism consistently correlate positively with the severity of depression. This... 

The slight conformational modification of the cycle A (revealed by X-ray diffraction), which probably comes from an interaction between the fluorine at C-9 and the axial OH at C-1, could contribute to the change in affinity [131]. However X-ray structure of the fluorocortisol co-crystallised with the glucocorticoid receptor does not clearly explain the impact of fluorine on the increased affinity for the receptor (cortisol, Ki=0.67pM vs 9a-fluorocortisol K,=0.027 pM) [132,133],... 

J. L. Arriza, C. Weinberger, G. Cerelli, T. M. Glaser, B. L. Handelin, D. E. Housman, R. E. Evans (1987). Cloning of human mineralocorticoid receptor c-DNA structural and functional kinship with the glucocorticoid receptor. Science 227 268-275. 

The HREs of the steroid hormone receptors posses a palindromic structure, comparable to the DNA binding elements of procaryotic repressors (see fig. 4.7a). The glucocorticoid receptor, for example, binds as a homodimer to the two-fold symmetrical recognition sequence, whereby the receptor is already dimerized in solution. In complex with the DNA each subimit of the dimer contacts one half-site of the HRE. As a consequence of the two-fold repeat of the recognition sequence, a high affinity binding of the receptor dimer results (compare 1.2.4). 

Lewis, D.F.V. et al. (2002) Molecular modelling of the human glucocorticoid receptor (hGR) ligand-binding domain (LBD) by homology with the human estrogen receptor a (hERa) LBD quantitative structure-activity... 

Receptor Structures for Glucocorticoids and Mineralocorticoids. The effects of adrenal-cortical steroids are thought to result from... 

The mineralocorticoid receptor (MR) mediates the sodium-retaining effects of aldosterone in the kidney, salivary glands, sweat glands, and colon. The human MR gene was cloned in 1987 and bears structural and functional kinships to the glucocorticoid receptor (11). It consists of 984 amino acids, spans 60 90 kb on chromosome 4q31.2 (50,51) and contains 10 exons including two exons (la and 1 p) that encode different 5 untranslated sequences whose expression is controlled by two different promoters (52). 

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