Structures of Human Monoamine Oxidase B Complexes with Selective Noncovalent Inhibitors: Safinamide and Coumarin Analogs
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- 作者：Claudia Binda ; Jin Wang ; Leonardo Pisani ; Carla Caccia ; Angelo Carotti ; Patricia Salvati ; Dale E. Edmondson ; Andrea Mattevi
- 刊名：Journal of Medicinal Chemistry
- 出版年：2007
- 出版时间：November 15, 2007
- 年：2007
- 卷：50
- 期：23
- 页码：5848 - 5852
- 全文大小：216K
- 年卷期：v.50,no.23(November 15, 2007)
- ISSN：1520-4804
文摘
Structures of human monoamine oxidase B (MAO B) in complex with safinamide and two coumarinderivatives, all sharing a common benzyloxy substituent, were determined by X-ray crystallography. Thesecompounds competitively inhibit MAO B with Ki values in the 0.1-0.5 M range that are 30-700-foldlower than those observed with MAO A. The inhibitors bind noncovalently to MAO B, occupying both theentrance and the substrate cavities and showing a similarly oriented benzyloxy substituent.