title: Human recombinant monoamine oxidase B as reliable and efficient enzyme source for inhibitor screening.
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.
authors.affiliation: LCT-Pharmacochimie, Section des sciences pharmaceutiques, Ecole de Pharmacie Genéve-Lausanne, Université de Genève, 30 Quai Ernest Ansermet, CH-1211 Genève 4, Switzerland.
authors.forename: Laura
authors.initials: L
authors.lastname: Novaroli
authors.forename: Marianne
authors.initials: M
authors.lastname: Reist
authors.forename: Elisabeth
authors.initials: E
authors.lastname: Favre
authors.forename: Angelo
authors.initials: A
authors.lastname: Carotti
authors.forename: Marco
authors.initials: M
authors.lastname: Catto
authors.forename: Pierre-Alain
authors.initials: PA
authors.lastname: Carrupt
mesh_terms: D001792:Blood Platelets / Q000187:drug effects / Q000201:enzymology; D003374:Coumarins / Q000032:analysis / Q000737:chemistry / Q000494:pharmacology; D004353:Drug Evaluation, Preclinical / Q000379:methods; D006801:Humans; D020128:Inhibitory Concentration 50; D008995:Monoamine Oxidase / Q000187:drug effects* / Q000235:genetics* / Q000378:metabolism; D008996:Monoamine Oxidase Inhibitors / Q000032:analysis / Q000737:chemistry / Q000494:pharmacology*; D011724:Pyridazines / Q000032:analysis / Q000145:classification / Q000494:pharmacology; D011994:Recombinant Proteins / Q000235:genetics*
chemical_list: D003374:Coumarins; D008996:Monoamine Oxidase Inhibitors; D011724:Pyridazines; D011994:Recombinant Proteins; C030123:coumarin; D008995:Monoamine Oxidase