Human recombinant monoamine oxidase B as reliable and efficient enzyme source for inhibitor screening

被引：115

作者：

Novaroli, L

Reist, M

Favre, E

Carotti, A

Catto, M

Carrupt, PA

机构：

[1] Univ Geneva, Ecole Pharm Geneve Lausanne, Sect Sci Pharmaceut, LCT Pharmacochim, CH-1211 Geneva, Switzerland

[2] Univ Bari, Dipartimento Farmacochim, I-70125 Bari, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2005年 / 13卷 / 22期

关键词：

human recombinant MAO B; human platelet MAO B; inhibitor screening; neurodegenerative diseases;

D O I：

10.1016/j.bmc.2005.06.043

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Interest in inhibitors of monoamine oxidase type B (MAO B) has grown in recent years, due to their therapeutic potential in aging-related neurodegenerative diseases, such as Parkinson's disease and Alzheimer's disease. This study is devoted to the use of human recombinant MAO B obtained from a Baculovirus expression system (Supersomes (TM) MAO B, BD Gentest, MA, USA) as reliable and efficient enzyme source for MAO B inhibitor screening. Comparison of inhibition potencies (pIC(50) values) determined with human cloned and human platelet MAO B for the two series of MAO B inhibitors, coumarin and 5H-indeno[1,2-c]pyridazin-5-one derivatives, showed that the difference between pIC(50) values obtained with the two enzyme sources was not significant (P > 0.05, Student's t-test). Hence, recombinant enzyme is validated as convenient enzyme source for MAO B inhibitor screening. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：6212 / 6217

页数：6

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