-
- 山田 良平
- 京都府立医科大学生化学教室
書誌事項
- タイトル別名
-
- Slow-Binding Inhibition and Slow, Tight-Binding Inhibition of Aspartate Aminotransferase by Hydrazinosuccinate
- ヒドラジノコハク類によるアスパラギン酸アミノ基転移酵素のSlow-binding inhibition及びSlow,tight-binding inhibition
- ヒドラジノコハクルイ ニ ヨル アスパラギンサン アミノキ テンイ コウソ ノ
この論文をさがす
抄録
Administration of isoniazid to mice induced a remarkable inhibition of liver cytosolic aspartate aminotransferase. Experimental findings indicated that the inhibitor was not isoniazid itself but probably its metabolite. DL-Hydrazinosuccinate, a model compound of the metabolite, was synthesized since the metabolite was not successfully isolated. The compound was found to be even more inhibitory. The inhibition by the compound proceeded time-dependently and was not readily released. D- and L-Hydrazinosuccinate were synthesized, respectively, for further analyses of the inhibition mechanisms. D-Hydrazinosuccinate was found to behave as a slow-binding inhibitor via a single-step reaction mechanism and gave Ki of approx. 3 nM. L-Hydrazinosuccinate was a more powerful inhibitor with Ki of approx. 0.2 nM, and was found to be a slow, tight-binding inhibitor and interact with the enzyme through consecutive reversible steps. Administration of L-hydrazinosuccinate to mice produced in vivo a potent and long lasting inhibition of cytosolic aspartate aminotransferase in the liver and kidney in a relatively specific manner. The administration of this compound also caused a remarkable accumulation of citrulline in the liver and plasma, which was explained as a result of both specific and non-specific effects of the inhibitor.
収録刊行物
-
- ビタミン
-
ビタミン 62 (3), 117-127, 1988
公益社団法人 日本ビタミン学会
- Tweet
キーワード
詳細情報 詳細情報について
-
- CRID
- 1390001205832675840
-
- NII論文ID
- 110002847540
-
- NII書誌ID
- AN00207833
-
- ISSN
- 2424080X
- 0006386X
-
- NDL書誌ID
- 3175383
-
- 本文言語コード
- ja
-
- データソース種別
-
- JaLC
- NDL
- CiNii Articles
-
- 抄録ライセンスフラグ
- 使用不可