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Post-Translational Regulation of Catalytic Activities of Cytochrome P450 46A1 and Uses Thereof

机译:翻译后调控的细胞色素P450 46A1的催化活性及其用途

摘要

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.
机译:本文提供了用于脑和视网膜中细胞色素P450 46A1(CYP46A1)酶活性的翻译后调节的方法和化合物。另外,提供了一种使用该酶的晶体结构鉴定CYP46A1酶的潜在调节剂的方法,以及一种用于在CYP46A1酶存在下筛选调节活性的后续方法。另外,提供了通过CYP46A1酶抑制或刺激胆固醇羟基化的调节剂化合物。还提供了使用刺激性化合物治疗与脑和视网膜中胆固醇水平升高相关的病理神经疾病的方法。

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