Novel arylpyrazole compounds selectively modulate glucocorticoid receptor regulatory activity

Article Abstract:

A series of arylpyrazole compounds, which specifically bind the glucocorticoid receptor (GR), selectively modulates GR-regulated biological functions in preadipocyte, preosteoblast, and lung epithelial cell lines. Subtle differences in ligand chemistry can profoundly influence the transcriptional regulatory activity of GR, and that endogenous genes bearing natural glucocortidcoid receptor elements (GREs) are especially sensitive detectors of these differences.

Ligand binding (Biochemistry), Chemical properties, Pyrazoles

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The glucocorticoid receptor blocks P-TEFb recruitment by NFkappaB to effect promoter-specific transcriptional repression

Article Abstract:

The composition and function of regulatory complexes at two NFkappaB-responsive genes is compared to investigate the determinants of promoter-specific gene regulation by the glucocorticoid receptor (GR). Proinflamatory genes such as IL-8 mRNA synthesis was repressed by GR at a post-initiation step, demonstrating that promoter proximal regulatory sequences assemble complexes that impact early and late stages of mRNA synthesis.

Gene mutations, Gene mutation, Nucleotide sequence, Base sequence, Messenger RNA

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Identification of C. elegans DAF-12-binding sites, response elements, and target genes

Article Abstract:

Intracellular receptor DAF -12 regulates dauer formation and development age and affects Caenorhabditis elegans life span. A procedure for multiple rounds of selection and amplification that yielded fragments bearing DAF-12-binding sites is developed beginning with C. elegans genomic DNA.

Biological Product (except Diagnostic) Manufacturing, Drugs, Deoxyribonucleic Acid, DNA, Caenorhabditis elegans, Binding sites (Biochemistry), Active sites (Biochemistry)

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