Glucocorticoid receptor binding

Tonner LE, Katz DI, Heiman AS. 1997. The acute effect of lead acetate on glucocorticoid receptor binding in C6 glioma cells. Toxicology 116 109-122. 

Sunahara Gl, Chiesa A. 1992. Phorone (diisopropylidene acetone), a glutathione depletor, decreases rat glucocorticoid receptor binding in vivo. Carcinogenesis 13(7) 1083-1089. 

Chen Y, Ferguson SS, Negishi M, Goldstein JA. Identification of constitutive androstane receptor and glucocorticoid receptor binding sites in the CYP2C19 promoter. Mol Pharmacol 2003 64(2) 316-324. 

Beclometasone (as dipropionate) is a pro-drug with weak glucocorticoid receptor-binding activity. It is hydrolysed via esterase enzymes to the active metabolite beclometasone-17-monopropionate (B-17-MP), which has high topical anti-inflammatory activity. 

The 18F-containing steroid 328 exhibits high in vitro GR (glucocorticoid receptor) binding affinity318. 

Copik AJ, Webb MS, Miller AL, Wang Y, Kumar R, Thompson EB. Activation function 1 of glucocorticoid receptor binds TATA-binding protein in vitro and in vivo. Mol. Endocrinol. 2006 20 1218-1230. 

Lee, P.C. and M. Struve. Unsaturated fatty acids inhibit glucocorticoid receptor binding of trout hepatic cytosol. Comp. Biochem. Physiol. 102B 707-711, 1992. 

Nimmagadda SR, Szefler SJ, Spahn JD, Surs W, Leung DY Allergen exposure decreases glucocorticoid receptor binding affinity and steroid responsiveness in atopic asthmatics. Am J Respir Crit Care Med 1997 155 87-93. (Ill)... 

Kam J, Szefler SJ, Surs W, Sher E, Leung DYM Combinations of IL-2 and IL-4 reduces glucocorticoid receptor-binding affinity and T cell response to glucocorticoids. J Immunol 1993 151 3460-3466. 

Both 19a,b inhibited dexamethasone-glucocorticoid receptor binding in a dose dependent manner (IC50=1.5 x 10 5 M and 1.0 x 10 5 M, respectively). [114]. Collismycins A and B were found to be cytotoxic against L1210 murine leukemia cells (IC50= 0.08 pg/ml and 0.12 pg/ml, respectively), and to display antimicrobial activity [114]. 

Huss, J.M., S.I. Wang, A. Astrom, P. McQuiddy, and C.B. Kasper (1996). Dexamethasone responsiveness of a major glucocorticoid-inducible CYP3A gene is mediated by elements unrelated to a glucocorticoid receptor binding motif. Proc. Natl. Acad. Sci. USA 93,4666-4670. 

Blackhurst G, McElroy P K, et al. (2001). Seasonal variation in glucocorticoid receptor binding characteristics in human mononuclear leukocytes. Clin. Endocrinol. (Oxf.) 55 683-686. 

Smith CL, Kreutner W. In vitro glucocorticoid receptor binding and transcriptional activation by topically active glucocorticoids. Arzneimittelforschung 1998 48 956-960. 

Prod, by Streptomyces sp. MQ22 and S. sp. SF 2738. Inhibitor of dexamethasone-glucocorticoid receptor binding. Antimicrobial and antitumour agent. Cryst. 

Payvar F, Wrange 0, Carlstedt-Duke J, Okret S, Gustafsson J-A, Yamamoto KR (1981) Purified glucocorticoid receptors bind selectively in vitro to a cloned DNA fragment whose transcription is regulated by glucocorticoids in vivo. Proc Natl Acad Sci USA 78 6628-6632... 

Scheidereit C, Geisse S, Westphal HM, Beato M (1983) The glucocorticoid receptor binds to defined nucleotide sequences near the promoter of mouse mammary tumour virus. Nature (London) 304 749-752... 

Williams GT, Morimoto RI (1990) Maximal stress-induced transcription from the human HSP70 promoter requires interactions with the basal promoter elements independent of rotational alignment. Mol Cell Biol 10 3125-3136 Willmann T, Beato M (1986) Steroid-free glucocorticoid receptor binds specifically to mouse mammary tumour virus DNA. Nature 324 688-691 Winkler H, Adam G, Mattes E, Schanz M, Hartig A, Ruis H (1988) Co-ordinate control of synthesis of mitochondrial and non-mitochondrial hemoproteins a binding site for the HAP-1 (CYPl) protein in the UAS region of the yeast catalase T gene. EMBO J 7 1799-1804... 

There are patients for whom currently available medical regimens are ineffective. Persistently uncontrolled asthma is associated with reduced glucocorticoid receptor binding on the inflammatory cells (60) anti-IgE may offer additional hope for these patients. Frequent exacerbations of asthma have been documented in patients who do not adhere to their treatment regimen (61). Indeed, studies show that only one half of the medication prescribed for asthma is ever used (62,63). For other patients, imperfect effort and technique limit the benefit of inhaled medication. Thus, the introduction of an effective therapy administered parenterally at 4-week intervals offers a fresh approach to improve the care of many patients. 

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