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

Bioorg Med Chem. 2005 Nov 15;13(22):6212-7. doi: 10.1016/j.bmc.2005.06.043. Epub 2005 Jul 27.

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.

Publication types

  • Validation Study

MeSH terms

  • Blood Platelets / drug effects
  • Blood Platelets / enzymology
  • Coumarins / analysis
  • Coumarins / chemistry
  • Coumarins / pharmacology
  • Drug Evaluation, Preclinical / methods
  • Humans
  • Inhibitory Concentration 50
  • Monoamine Oxidase / drug effects*
  • Monoamine Oxidase / genetics*
  • Monoamine Oxidase / metabolism
  • Monoamine Oxidase Inhibitors / analysis
  • Monoamine Oxidase Inhibitors / chemistry
  • Monoamine Oxidase Inhibitors / pharmacology*
  • Pyridazines / analysis
  • Pyridazines / classification
  • Pyridazines / pharmacology
  • Recombinant Proteins / genetics*

Substances

  • Coumarins
  • Monoamine Oxidase Inhibitors
  • Pyridazines
  • Recombinant Proteins
  • coumarin
  • Monoamine Oxidase