Bioorganic & medicinal chemistry letters

Inactivation of GABA transaminase by 3-chloro-1-(4-hydroxyphenyl) propan-1-one

YH Tao, HB Xu, XL Yang

Index: Tao, Yun-Hai; Xu, Hui-Bi; Yang, Xiang-Liang Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 3 p. 731 - 734

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Abstract

Previously it was found that 4-hydroxybenzaldehyde is a competitive inhibitor of GABA transaminase. Here 3-chloro-1-(4-hydroxyphenyl) propan-1-one (9), a 4- hydroxybenzaldehyde analogue, was found to inactivate potently the enzyme in a time- dependent manner. α-Ketoglutarate prevented the enzyme from inactivation, suggesting that the inactivation occurs in its active site. Several experiments indicated that the inactivation ...