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Inactivation of GABA transaminase by 4-acryloylphenol
Yun-Hai Tao1, Hui-Bi Xu, Xiang-Liang Yang
1Institute of Materia Medica, College of Life Science and Technology, Huazhong University of Science and Technology, 430074 Wuhan, China.
Abstract:
Previous study showed that 4-hydroxybenzaldehyde is a competitive inhibitor of GABA transaminase. As a result, 4-acryloylphenol was synthesized as a 4-hydroxybenzaldehyde analogue, and shown to inactivate potently the enzyme in a time-dependent manner. The inactivation was protected by alpha-ketoglutarate, indicating that it occurs at the active site of the enzyme. Beta-mercaptoethanol also prevented the enzyme from inactivation. The possible mechanism involving a Michael addition was proposed to rationalize the inactivation.
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