Receptor-Fluticasone propionate-complex (PDB ID: 3CLD) Reference: Biggadike, K.; et al. J. Med. Chem. 2008, 51, 3349. Navigation: < Last Page | Main Page | Next Page > |
This is the structure of the naturally occuring hormone, cortisol. When this binds to a glucocorticoid receptor it causes anti-inflammatory responces in the body. The non-polar structure of steriods give them the ability to diffuse directly though the cellular membrane and into cells. Fluticasone Propionate, chemically know as S-(fluoromethyl)6a,9-difluoro-11ß-17-dihydroxy-16a-methyl-3-oxoandrosta-1,4-diene-17ß-carbothioate is a drug that mimics the naturally occure hormomne cortisol. Glucocorticoid receptor are a type of nuclear receptors found within the interior cytoplasm of cell. These receptors work by binding with a ligand, Cortisol or Fluticasone Propionate, which form a receptor-glucorticoid complex. The receptor-glucorticoid complex then binds directly to DNA in order regulates multiple genes that control the transcription and expression of immune responses. The receptor-glucorticoid complex up-regulates the expression of anti-inflammatory proteins and represses the expression of pro-inflammatory proteins in the cell. Fluticasone Propionate binds to the 570 GLN side chain of the alpha helix of the receptor. The binding induce a conformational change to change the structure of the receptor protein.
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