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Human recombinant monoamine oxidase B as reliable and efficient enzyme source for inhibitor screening
|Published in||Bioorganic & Medicinal Chemistry. 2005, vol. 13, no. 22, p. 6212-6217|
|Abstract||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 MAO B, BD Gentest, MA, USA) as reliable and efficient enzyme source for MAO B inhibitor screening. Comparison of inhibition potencies (pIC50 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 pIC50 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.|
|Keywords||Blood Platelets/drug effects/enzymology — Coumarins/analysis/chemistry/pharmacology — Drug Evaluation, Preclinical/methods — Humans — Inhibitory Concentration 50 — Monoamine Oxidase/*drug effects/*genetics/metabolism — Monoamine Oxidase Inhibitors/analysis/chemistry/*pharmacology — Pyridazines/analysis/classification/pharmacology — Recombinant Proteins/*genetics|
|NOVAROLI, L. et al. Human recombinant monoamine oxidase B as reliable and efficient enzyme source for inhibitor screening. In: Bioorganic & Medicinal Chemistry, 2005, vol. 13, n° 22, p. 6212-6217. https://archive-ouverte.unige.ch/unige:10616|