Characteristics of ethacrynic acid highly sensitive Mg2+-ATPase in microsomal fractions of the rat brain : Functional molecular size, inhibition by SITS and stimulation by Cl-.
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概要
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Studies were performed to characterize ethacrynic acid (EA) highly sensitive Mg<SUP>2+</SUP>-ATPase isolated from microsomal fractions of the rat brain. The functional molecular sizes of the EA highly sensitive and EA less sensitive Mg<SUP>2+</SUP>-ATPases, estimated by a radiation inactivation method, were 480 and 80 kDa, respectively. An anion transport inhibitor, 4-acetamido-4'-isothiocyanostilbene2, 2'-disulfonic acid (SITS) inhibited the EA highly sensitive Mg<SUP>2+</SUP>-ATPase activity. The type of inhibition was uncompetitive with respect to ATP, and the inhibition was suppressed by anions such as Cl<SUP>-</SUP>, Br<SUP>-</SUP> and I<SUP>-</SUP>. Chloride ions stimulated enzyme activity with an increase in V<SUB>max</SUB>, but not in K<SUB>m</SUB>, for ATP. Anions tested also increased the enzyme activity in the following order of decreasing potency: Cl<SUP>-</SUP> >Br<SUP>-</SUP>>CH<SUB>3</SUB>COO<SUP>-</SUP>=I<SUP>-</SUP>>SO<SUB>4</SUB><SUP>2-</SUP>=HCO<SUB>3</SUB><SUP>-</SUP>>SO<SUB>3</SUB><SUP>2-</SUP>. These results suggest that EA highly sensitive Mg<SUP>2+</SUP>-ATPase is a relatively large molecule with anion-sensitive sites that affect the ATP hydrolyzing activity and the SITS binding capacity through anions, with Cl<SUP>-</SUP> being the most potent.
- 公益社団法人 日本薬理学会の論文
著者
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Takaori Shuji
Department Of Pharmacology Shimane Medical University
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Tanaka Toshizo
Department Of Pharmacology Faculty Of Medicine Kyoto University
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Matsuda Koji
Osaka Laboratories Japanese Association For Radiation Research On Polymers
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INAGAKI Chiyoko
Departmctit of Pharmacology, Faculty of Medicine, Kyoto University
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