4‐Amino‐hex‐5‐enoic Acid, a Selective Catalytic Inhibitor of 4‐Aminobutyric‐Acid Aminotransferase in Mammalian Brain

FEBS Journal - Tập 74 Số 3 - Trang 441-445 - 1977
Bruce Lippert1, Brian W. Metcalf1, Michel J. Jung1, Patrick Casara1
1Centre de Recherche Merrell International, 16, Rue d'Ankara, F-67084 Strasbourg-Cedex, France

Tóm tắt

Incubation of rat brain 4‐aminobutyrate aminotransferase with 4‐amino‐hex‐5‐enoic acid, a substrate analog of 4‐aminobutyric acid, results in a time‐dependent irreversible loss of enzymatic activity. In the presence of 0.1 mM inhibitor the half‐life of the inactivation process is approximately 6 min. Low concentrations of L‐glutamic acid or 4‐aminobutyric acid protect against this inactivation. while 2‐oxoglutarate prevents this protection, suggesting that only the pyridoxal form of the enzyme is susceptible to inhibition by 4‐amino‐hex‐5‐enoic acid.The irreversible inhibition of mammalian 4‐aminobutyrate aminotransferase by 4‐amino‐hex‐5‐enoic acid is selective. There is no inhibition of this enzyme from Pseudomonas fluorescens with the inhibitor at mM concentrations. Even at 10 mM there is no irreversible inhibition of mammalian glutamate decarboxylase or of aspartate aminotransferase, while alanine aminotransferase is inhibited over 500 times more slowly than rat brain 4‐aminobutyrate transaminase.

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Thông tin
Thông tin xuất bản

FEBS Journal

Tập 74 Số 3

441-445

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