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MR Vol.11 No.4 indexに戻る
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MODERN RHEUMATOLOGY
Vol.11 No.4 |
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Molecular pharmacology of glucocorticoids: recent
advances and future perspectives |
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| H. Tanaka1 |
| (1) Division of Clinical Immunology, Advanced
Clinical Research Center, Institute of Medical Science,University
of Tokyo, 4-6-1 Shirokanedai, Minato-ku, Tokyo 108-8639, Japan |
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| Abstract |
| Abstract Glucocorticoids are one of the most
widely used bullets for the treatment of inflammatory and immune
disorders. They act by binding to their specific intracellular
receptor, the glucocorticoid receptor (GR), which is a transcription
factor belonging to the nuclear receptor superfamily. It is believed
that the GR, upon binding ligand, elicits transcriptional regulation
of target gene expression via orchestrated interaction with DNA,
coregulators, other transcription factors, and chromatin. This
model has raised the possibility that a certain class of ligand
might variably modulate GR-mediated intracellular signals. Moreover,
crystallographic analysis of the ligand-binding domain of the nuclear
receptor has given structural insight into the ligand-dependent
modularity of the receptor function. This advanced technology would
allow the molecular pharmacologic development of a ligand that
could dissociate therapeutic actions from the undesirable metabolic
effects of glucocorticoids in the near future. |
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| Key words |
| Key words Antiinflammation ・ Glucocorticoid
・ Glucocorticoid receptor ・ Immunosuppression ・ Transcription factor |
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