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US 2013/0217595 A1Published application
Method for the identification of catechol o-methyltransferase modulators
AssigneeHoffman-La Roche Inc.
InventorsThilo Enderle, Doris Roth
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Abstract
The present invention relates to a method for the identification of modulators of catechol O-methyltransferase enzyme activity (COMT).
Claims15
A method for the identification of a modulator of the activity of a catechol O-methyl transferase enzyme (COMT) comprising the steps of:
- a) providing a COMT substrate covalently linked to a fluorescence dye,
- b) contacting the molecule of step a) with a catechol O-methyl transferase enzyme (COMT), a S-adenosylmethionine (SAM) and a candidate compound and
- c) measuring the fluorescence readout of the mixture of step b), wherein an altered fluorescence readout in presence of the candidate compound compared to a blank is indicative for a modulator of a catechol O-methyl transferase enzyme (COMT).
A method for the identification of a substrate of a catechol O-methyl transferase enzyme (COMT) comprising the steps of:
- a) providing a mixture comprising a COMT substrate covalently linked to a fluorescence dye and S-adenosylmethionine (SAM),
- b) contacting the mixture of step a) with different concentrations of a candidate compound,
- c) contacting the mixtures of step b) with a catechol O-methyl transferase enzyme (COMT) and
- d) measuring the kinetic fluorescence readout of the mixtures of step c), wherein a decreasing fluorescence readout plateau as a function of an increasing concentration of the candidate compound is indicative for a substrate of a catechol —O-methyl transferase enzyme (COMT).
1 more element
Dependencies are inferred from the claim text.