Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 13, Issue 22, Pages 6212-6217Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2005.06.043
Keywords
human recombinant MAO B; human platelet MAO B; inhibitor screening; neurodegenerative diseases
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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.
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