Characterization of a Binding Site of UCN-01,a Novel Anticancer Drug on α_1-Acid Glycoprotein
スポンサーリンク
概要
- 論文の詳細を見る
The binding site of 7-hydroxystaurosporine (UCN-01) on α_1-acid glycoprotein (AGP) was studied by fluorescence and ultracentrifugation experiments. Three ligands, propranolol, warfarin and progesterone were employed as marker ligands and quinaldine red was employed as a fluorescent probe. The persence of UCN-01,propranolol, warfarin and progesterone resulted in a significant quenching of the fluorescence of quinaldine red, when bound to AGP, depending upon the potency of the binding to AGP. The construction of Klotz plots indicated that the displacement effects of propranolol, warfarin and progesterone on UCN-01-AGP binding were competitive in nature. These data suggest that the binding site of UCN-01 on the AGP partly overlaps and binding site for basic drugs, acidic drugs, as well as steroid hormones.
- 公益社団法人日本薬学会の論文
- 2000-07-01
著者
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小林 智
協和発酵工業株式会社 医薬開発本部非臨床開発部
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OTAGIRI MASAKI
Faculty of Pharmaceutical Science, Kumamoto University
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西 勝英
熊本大学医学薬学研究部生体機能薬理学教室
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KOBAYASHI Satoshi
Pharmaceuticals Research and Development Division, Kyowa Hakko Kogyo Co., Ltd.
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SUENAGA Ayaka
Faculty of Pharmaceutical Science, Kumamoto University
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Suenaga A
Graduate School Of Pharmaceutical Sciences Kumamoto University
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Suenaga Ayaka
Graduate School Of Pharmaceutical Sciences Kumamoto University
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Suenaga Ayaka
Faculty Of Pharmaceutical Science Kumamoto University
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Otagiri M
Graduate School Of Pharmaceutical Sciences Kumamoto University
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Watanabe Hiroshi
Super-fine Sr Lithography Laboratory Association Of Super-advanced Electronics Technologies(aset) At
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NISHI Koji
Faculty of Pharmaceutical Sciences, Kumamoto University
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KURATA Noriaki
Pharmaceutical Research Institute, Kyowa Hakko Kogyo Co., Ltd.,
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MATSUSHITA Sadaharu
Faculty of Pharmaceutical Sciences, Kumamoto University
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WATANABE Hiroshi
Faculty of Pharmaceutical Sciences, Kumamoto University
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Kurata Noriaki
Pharmaceutical Research Institute Kyowa Hakko Kogyo Co. Ltd.
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Otagiri M
Kumamoto Univ. Kumamoto Jpn
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Watanabe H
Tokyo Univ. Pharmacy And Life Sci. Tokyo Jpn
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Katagiri S
Faculty Of Engineering Niigata University
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Kobayashi Satoshi
Analytical And Pharmacokinetic Department Pharmaceutical Research Laboratories Kyowa Hakko Kogyo Co.
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Kobayashi Satoshi
Pharmaceutical Research Institute Kyowa Hakko Kogyo Co. Ltd.
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Matsushita S
Faculty Of Pharmaceutical Sciences Kumamoto University
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Otagiri Masaki
Faculty Of Pharmaceutical Science Kumamoto University
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Kobayashi Satoshi
Analytical & Pharmacokinetic Laboratories Pharmaceutical Research Institute Kyowa Hakko Hagyo Co
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Kobayashi Satoshi
Drug Development Research Laboratories Pharmaceutical Research Institute Kyowa Hakko Kogyo Co. Ltd.
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Nishi Katsuhide
Department Of Biopharmaceutics Graduate School Of Pharmaceutical Sciences Kumamoto University
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