Cell Type-Dependent Divergence of Transactivation by Glucocorticlid Receptor Ligand
スポンサーリンク
概要
- 論文の詳細を見る
The glucocorticoid receptor regulates gene expression mainly by two mechanisms; transactivation and trans-repression. A ligand with strong transrepression and weak transactivation activity is predicted to be a beneficial agent with potent anti-inflammatory activity and minor adverse effects. Recently, the profile of a synthetic steroid, RU24858, has been reported to fulfill this condition in vitro, but others have reported no dissociation between the anti-inflammatory activity and side effects in vivo. To gain further information on the profile of this compound, we evaluated its transactivation ability using a reporter gene analysis both in vitro and in vivo. In the in vitro analysis, RU24858 demonstrated only a weak transactivation activity in HeLa cells, when compared with prednisolone. In CV-1 cells, however, these two glucocorticoids exhibited equivalent transactivation activities. This behavior is independent of whether the reporter gene is regulated by mouse mammary tumor virus promoter or multiple copies of glucocorticoid response element. When the reporter plasmid was inoculated into mouse abdominal skin using a gene gun, followed by orally administration of glucocorticoids, RU24858 induced significantly higher reporter enzyme activity than prednisolone. These results suggest that the profile of RU24858 is divergent and its transactivation ability is comparable to prednisolone depending on the cell-type both in vitro and in vivo.
- 日本薬学会の論文
- 2002-12-01
著者
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Ikizawa Koichi
Pharmacobioregulation Research Laboratory Taiho Pharmaceutical Co. Ltd.
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Ikizawa K
Clinical Research Center For Allergy National Sagamihara Hospital
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Ikizawa Koichi
国立相模原病院
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Ikizawa Koichi
Clinical Research Center For Allergy National Sagamihara Hospital
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Kiniwa Mamoru
大鵬薬品工業
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Kiniwa Mamoru
Pharmacobioregulation Research Laboratory Taiho Pharmaceutical Co. Ltd.
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TANIGAWA Kiyoshi
Pharmacobioregulation Research Laboratory, Taiho Pharmaceutical Co., Ltd.
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TANAKA Katsunao
Pharmacobioregulation Research Laboratory, Taiho Pharmaceutical Co., Ltd.
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NAGASE Hideki
Pharmacobioregulation Research Laboratory, Taiho Pharmaceutical Co., Ltd.
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MIYAKE Hidekazu
Pharmacobioregulation Research Laboratory, Taiho Pharmaceutical Co., Ltd.
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Nagase Hidetaka
Pharmacobioregulation Research Laboratory Taiho Pharmaceutical Co. Ltd.
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Nagase Hidetaka
大鵬薬品工業
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Miyake H
Kitami Inst. Technol. Kitami Jpn
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Miyake Hidekazu
Pharmacobioregulation Research Laboratory Taiho Pharmaceutical Co. Ltd.
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Tanaka Katsunao
Pharmacobioregulation Research Laboratory Taiho Pharmaceutical Co. Ltd.
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Tanaka Katsunao
大鵬薬品工業
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Tanigawa Kiyoshi
大鵬薬品工業
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Tanigawa Kiyoshi
Pharmacobioregulation Research Laboratory Taiho Pharmaceutical Co. Ltd.
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Tanaka K
Chlorella Industry Co. Ltd.
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Miyake H
Department Of Clinical Chemistry Faculty Of Pharmaceutical Sciences Hokuriku University
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Tanigawa Kozo
Pharmacobioregulation Research Laboratory Taiho Pharmaceutical Co. Ltd.
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Nagase H
Pharmacobioregulation Research Laboratory Taiho Pharmaceutical Co. Ltd.
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