Abstract:
The present invention relates to a novel preparation method of metabolites from fluvastatin using bacterial cytochrome p450 and a composition therefor, and more specifically, to a composition for manufacturing 5-hydroxyl products and 6-hydroxyl products and a kit from fluvastatin comprising bacterial cytochrome p450 BM3 (CYP102A1), mutants of CYP102A1, and a chimera of mutants of CYP102A1, and to a preparation method thereof.
Abstract:
본 발명은 심바스타틴 또는 로바스타틴의 사람에서의 대사산물을 생산하는 방법에 관한 것이다. 보다 상세하게는, 본 발명은 박테리아 시토크롬 P450 BM3(CYP102A1) 또는 그의 돌연변이체를 이용하여 심바스타틴 또는 로바스타틴으로부터 그의 사람에서의 대사산물을 제조하는 방법 및 이를 위한 조성물 및 키트를 제공한다. 심바스타틴, 로바스타틴, CYP102A1, 돌연변이체
Abstract:
본 발명은 박테리아 시토크롬 P450을 이용한 아토르바스타틴으로부터 대사산물의 신규한 생산방법 및 이를 위한 조성물에 관한 것으로, 보다 상세하게는 박테리아 시토크롬 P450 BM3(CYP102A1), CYP102A1의 돌연변이체(mutant) 및 CYP102A1의 돌연변이체의 카메라(chimera)를 포함하는 아토르바스타틴으로부터 2-히드록실산물 또는 4-히드록실산물제조용 조성물, 키트 및 이의 생산방법에 관한 것이다.
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:
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:
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.