Purification and Characterization of Pranlukast Hydrolase from Rat Liver Microsomes : The Hydrolase is Identical to Carboxylesterase pI 6.2
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概要
- 論文の詳細を見る
Two carboxylesterases with pI 6.0 and 6.2 derived from rat liver microsomes were purified. The two isozymes were remarkably different in substrate specificity, but they had equal enzymatic activity for α-naphthyl acetate and were inhibited equally by phenylmethylsulfonyl fluoride (PMSF) and bis-(4-nitrophenyl) phosphate (BNPP).Carboxylesterases pI 6.0 and 6.2 are identical to the enzymes referred to as hydrolase A and B, respectively, from the results of amino acid sequence analyses. Pranlukast was effectively hydrolyzed by carboxylesterase pI 6.2 but not by the pI 6.0 enzyme, and the difference in the pranlukast metabolism between the human and the rat could be explained by the substrate specificity of carboxylesterase. Furthermore, prodrugs of angiotensin converting enzyme inhibitors were found to be converted to the active drugs after hydrolysis by the carboxylesterases pI 6.0 and 6.2.Carboxylesterases generally catalyze the hydrolysis of ester-type drugs preferentially rather than amide-type drugs.
- 公益社団法人日本薬学会の論文
- 1997-01-15
著者
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平野 和行
岐阜薬科大学 薬剤学
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HIRANO Kazuyuki
Department ofPharmaceutics, Glfu Pharmaceutical University
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KATAGIRI Yoshihiro
Department of Pharmacy, Gifu University Hospital
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SUGIYAMA Tadashi
Department of Pharmacy, Gifu University Hospital
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平野 和行
岐阜薬科大学薬剤学研究室
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USAMI Yoshiko
岐阜薬科大学薬剤学教室
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ADACHI Tetsuo
岐阜薬科大学薬剤学教室
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平野 和行
岐阜薬科大学 薬剤学教室
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Adachi T
Laboratory Of Clinical Pharmaceutics Gifu Pharmaceutical University
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Adachi Tetsuo
Department Of Pharmaceutics Gifu Pharmaceutical University
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Adachi Tetsuo
Department Of Clinical Pharmaceutics Gifu Pharmaceutical University
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Usami Y
Nagoya National Hospital (tokai Area Central Hospital For Aids Treatment And Res.) Aichi Jpn
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TAKAI Satomi
Department of Pharmaceutics, Gifu Pharmaceutical University
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USAMI Yoshiko
Department of Pharmaceutics, Gifu Pharmaceutical University
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Hirano Kazuyuki
Radioisotope Laboratory And Department Of Pharmaceutics Gifu Pharmaceutical University
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Hirano Kazuyuki
Department Of Material Chemistry Graduate School Of Engineering Kyoto University
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Hirano Kazuyuki
Department Of Pharmaceutcs Gifu Pharmaceutical University
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LUAN Libiao
Department of Pharmaceutics, Gifu Pharmaceutical University
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Satoh Takumi
Division Of Protein Biosynthesis Institute For Protein Research Osaka University
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Kizu Hiroto
Department Of Radiology Kanazawa University Hospital
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Katagiri Yoshihiro
Department Of Biochemistry Gifu Pharmaceutical University
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Sugiyama Tadashi
Department Of Applied Chemistry Faculty Of Science Tokyo University Of Science
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HIRANO Kazuyuki
Department of Clinical Chemistry School of Health Sciences, Fujita Health University
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Katagiri Yoshihiro
Deparhnent of Pharmacy Gifu University Hospital
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