Effects of Active-Site Modification and Quaternary Structure on the Regioselectivity of Catechol- O -Methyltransferase
Effects of Active-Site Modification and Quaternary Structure on the Regioselectivity of Catechol- O -Methyltransferase
复制标题
活性位点修饰和四级结构对儿茶酚-O-甲基转移酶区域选择性的影响
DOI：
10.1002/ange.201508287
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发表时间：
2016
影响因子：
--
通讯作者：
Law B
中科院分区：
文献类型：
--
作者：
Law B
Catechol‐O‐methyltransferase (COMT), an important therapeutic target in the treatment of Parkinson's disease, is also being developed for biocatalytic processes, including vanillin production, although lack of regioselectivity has precluded its more widespread application. By using structural and mechanistic information, regiocomplementary COMT variants were engineered that deliver eithermeta‐ orpara‐methylated catechols. X‐ray crystallography further revealed how the active‐site residues and quaternary structure govern regioselectivity. Finally, analogues of AdoMet are accepted by the regiocomplementary COMT mutants and can be used to prepare alkylated catechols, including ethyl vanillin.
