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

Publié dansBioorganic & medicinal chemistry, vol. 13, no. 22, p. 6212-6217
Date de publication2005
Résumé

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.

Mots-clés
  • 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
Citation (format ISO)
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. doi: 10.1016/j.bmc.2005.06.043
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ISSN du journal0968-0896
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Informations techniques

Création06/08/2010 13:48:44
Première validation06/08/2010 13:48:44
Heure de mise à jour14/03/2023 16:00:25
Changement de statut14/03/2023 16:00:24
Dernière indexation12/02/2024 19:10:31
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