박테리아 시토크롬 P450을 이용한 아토르바스타틴으로부터 대사산물의 신규한 생산방법 및 이를 위한 조성물
    5.
    发明公开
    박테리아 시토크롬 P450을 이용한 아토르바스타틴으로부터 대사산물의 신규한 생산방법 및 이를 위한 조성물 有权
    使用细菌细胞色素P450的ATORVASTATIN代谢物的新方法及其组成

    公开(公告)号:KR1020130055511A

    公开(公告)日:2013-05-28

    申请号:KR1020120094935

    申请日:2012-08-29

    CPC classification number: C12N9/0071 C12P17/10 C12Y114/14001

    Abstract: PURPOSE: A composition, a kit, and a method for preparing a 2-hydroxyl product or a 4-hydroxyl product from atorvastatin, are provided to cheaply, efficiently, and selectively produce a large amount of the 2-hydroxyl products or the 4-hydroxyl products, and to develop a novel drug using an atorvastatin metabolite. CONSTITUTION: A composition for preparing a 2-hydroxyl product or a 4-hydroxyl product from atorvastatin contains one or more enzymes selected from the group consisting of wild type CYP102A1, mutant CYP102A1, and a chimera of mutant CYP102A1. A method for preparing the 2-hydroxyl product or the 4-hydroxyl product from atorvastatin comprises a step of reacting the enzymes with atorvastatin. A kit for preparing the 2-hydroxyl product or the 4-hydroxyl product from atorvastatin contains the enzymes and an NADPH-generation system.

    Abstract translation: 目的:提供一种组合物,试剂盒和从阿托伐他汀制备2-羟基产物或4-羟基产物的方法,以便廉价,高效地选择性地生产大量的2-羟基产物或4-羟基产物, 羟基产物,并使用阿托伐他汀代谢物开发新药。 构成:用于从阿托伐他汀制备2-羟基产物或4-羟基产物的组合物含有一种或多种选自野生型CYP102A1,突变CYP102A1和突变型CYP102A1嵌合体的酶。 从阿托伐他汀制备2-羟基产物或4-羟基产物的方法包括使酶与阿托伐他汀反应的步骤。 用于制备2-羟基产物或来自阿托伐他汀的4-羟基产物的试剂盒含有酶和NADPH生成系统。

    박테리아 사이토크롬 피450을 이용한 심바스타틴 또는 로바스타틴의 사람에서의 대사산물의 신규한 생산방법 및 이를 위한 조성물
    6.
    发明公开
    박테리아 사이토크롬 피450을 이용한 심바스타틴 또는 로바스타틴의 사람에서의 대사산물의 신규한 생산방법 및 이를 위한 조성물 有权
    使用细菌细胞色素P450的辛伐他汀或LOVASTATIN的人代谢产物的新方法及其组合物

    公开(公告)号:KR1020110020525A

    公开(公告)日:2011-03-03

    申请号:KR1020090078181

    申请日:2009-08-24

    CPC classification number: C12P17/06 C12N9/0071 C12Y114/14001

    Abstract: PURPOSE: A method for selective producing human metabolite from simvastatin or lovastatin is provided. CONSTITUTION: A composition for catalysis for producing human metabolite from simvastatin or lovastatin contains wild type CYP102A1 and/or CYP102A1 mutant. The CYP102A1 mutant has 47th amino acid, arginin substituted with leucine; 51th amino acid, tyrosine substituted with phenylalanine; 64th amino acid, glytamic acid substituted with glycine; 74th amino acid, alanine substituted with glycine, 81th amino acid, phenylalanine substituted with isoleucine, 86th amino acid, leucine substituted with isoleucine; 87th amino acid, phenylalanine substituted with valine; 143th amino acid, gluamic acid substituted with glycine; 188th amino acid, leucine substituted with glutamine; and 267th amino acid glutamic acid substituted with valine.

    Abstract translation: 目的:提供从辛伐他汀或洛伐他汀选择性生产人类代谢物的方法。 构成:用于从辛伐他汀或洛伐他汀生产人代谢物的催化组合物含有野生型CYP102A1和/或CYP102A1突变体。 CYP102A1突变体具有第47位氨基酸,精氨酸被亮氨酸取代; 第51位氨基酸,被苯丙氨酸取代的酪氨酸; 第64位氨基酸,甘氨酸取代的甘氨酸; 第74位氨基酸,被甘氨酸取代的丙氨酸,第81位氨基酸,被异亮氨酸取代的苯丙氨酸,第86位氨基酸,被异亮氨酸取代的亮氨酸; 第87位氨基酸,用缬氨酸取代的苯丙氨酸; 第143位氨基酸,被甘氨酸取代的谷氨酸; 第188位氨基酸,用谷氨酰胺取代的亮氨酸; 和用缬氨酸取代的第267位氨基酸谷氨酸。

    박테리아 사이토크롬 피450을 이용한 심바스타틴 또는 로바스타틴의 사람에서의 대사산물의 신규한 생산방법 및 이를 위한 조성물
    8.
    发明公开
    박테리아 사이토크롬 피450을 이용한 심바스타틴 또는 로바스타틴의 사람에서의 대사산물의 신규한 생산방법 및 이를 위한 조성물 无效
    使用细菌细胞色素P450的辛伐他汀或LOVASTATIN的人代谢产物的新方法及其组合物

    公开(公告)号:KR1020110086686A

    公开(公告)日:2011-07-29

    申请号:KR1020110071078

    申请日:2011-07-18

    Abstract: PURPOSE: A method for preparing human metabolites of simvastatin or lovastatin using bacterial cytochrome p450 is provided to selectively produce metabolic protucts. CONSTITUTION: A composition for preparing human metabolites of simvastatin or lovastatin has: 47th amino acid arginin(R) of wild type CYP102A1, which is substituted with alanine, valine, leucine, isoleucine, proline, methionine, phenylalanine, or tryptopane; 87th amino acid, phenylalaine(F) which is substituted with alanine, valine, leucine, isoleucine, proline, methionine, or tryptopane; 143th amino acid, gluamic acid(E), which is substituted with glycine, serine, threonine, cysteine, tyrosine, asparagine, or glutamine; and 188th amino acid, leucine(L), which is substituted with glycine, serine, threonine, cysteine, tyrosine, asparagine, or glutamine.

    Abstract translation: 目的:提供使用细菌细胞色素p450制备辛伐他汀或洛伐他汀的人代谢产物的方法,以选择性地产生代谢产物。 构成:用于制备辛伐他汀或洛伐他汀的人代谢物的组合物具有:用丙氨酸,缬氨酸,亮氨酸,异亮氨酸,脯氨酸,甲硫氨酸,苯丙氨酸或三苯甲烷取代的野生型CYP102A1的第47位氨基酸精氨酸(R) 第八十八氨基酸,被丙氨酸,缬氨酸,亮氨酸,异亮氨酸,脯氨酸,甲硫氨酸或三苯甲烷取代的苯丙氨酸(F); 由甘氨酸,丝氨酸,苏氨酸,半胱氨酸,酪氨酸,天冬酰胺或谷氨酰胺取代的第143位氨基酸,葡萄糖酸(E) 和第188位氨基酸,其被甘氨酸,丝氨酸,苏氨酸,半胱氨酸,酪氨酸,天冬酰胺或谷氨酰胺取代的亮氨酸(L)。

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