Inactivation of GABA transaminase by 3-chloro-1-(4-hydroxyphenyl)propan-1-one |
| |
| Authors: | Yun-Hai Tao Hui-Bi Xu Xiang-Liang Yang |
| |
| Affiliation: | 1. College of Life Science and Technology, Huazhong University of Science and Technology, 1037 Luoyu Road, Wuhan 430074, China;2. Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry of Education, School of Chemical Science and Technology, Yunnan University, Kunming 650091, China |
| |
| 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 is irreversible. This study provides a novel strategy for the design of more effective inhibitors. |
| |
| Keywords: | |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
