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MR Vol.14 No.5 indexに戻る
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MODERN RHEUMATOLOGY Vol.14 No.5 |
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Selective modulation of glucocorticoid receptor function toward development of novel antiinflammation: lessons from a phenylpyrazolosteroid cortivazol |
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| Hirotoshi Tanaka1, Noritada Yoshikawa1, Noriaki Shimizu1 and Chikao Morimoto1 |
(1) Division of Clinical Immunology, The Advanced Clinical Research Center, The Institute of Medical Science, The University of Tokyo, 4-6-1 Shirokanedai, Minato-ku, Tokyo 108-8639, Japan |
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| Abstract |
| A Frequent association of side effects has been a long-standing dilemma in clinical glucocorticoid therapy. Recent progress in molecular biology of glucocorticoid hormone action, however, has prompted researchers to tackle the dissociation of side effects and therapeutic effects based on the assumption that selective modulation of its receptor function could be achieved by as yet unknown compounds. Already a number of selective modulators of the glucocorticoid receptor (SGRMs) have been reported, and certain compounds have dissociating characteristics in vivo. We have addressed ligand-dependent modular recruitment of AF-1 function using a phenylpyrazologlucocorticoid cortivazol, suggesting the possibility of developing tissue-specific SGRMs. It should also be emphasized that SGRMs do not always have a steroid structure. |
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| Key words |
| Co-activator - Conformation - Glucocorticoid receptor (GR) - Ligand binding domain (LBD) - Transcription |
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