Post-translational regulation of catalytic activities of cytochrome P450 46A1 and uses thereof
OwnerIrina A. Pikuleva, Natalia V. Mastinventors
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Abstract
Provided herein are methods and compounds for post-translational regulation of cytochrome P450 46A1 (CYP46A1) enzyme activity in the brain and retina. Also, a method for identifying a potential regulator of a CYP46A1 enzyme using crystal structures of the enzyme and a subsequent method for screening for a regulatory activity in the presence of CYP46A1 enzyme are provided. In addition, the regulator compounds that either inhibit or stimulate cholesterol hydroxylation by the CYP46A1 enzyme are provided. Further provided is a method of treating a pathoneurological condition associated with increased cholesterol levels in the brain and retina using the stimulatory compounds.
Claims28
A method for controlling an activity of a cytochrome P450 46A1 (CYP46A1) enzyme, comprising:
- contacting the CYP46A1 enzyme with a compound that binds within the CYP46A1 active site such that cholesterol hydroxylation is effectively inhibited or stimulated thereby controlling the CYP46A1 activity.
A method for designing a potential regulator compound of a post-translational CYP46A1 activity, comprising:
- identifying a test compound that interacts within the active site of CYP46A1, said identification based at least in part on the crystal structure of CYP46A1.
Dependencies are inferred from the claim text.