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公开(公告)号：KR100519693B1
公开(公告)日：2005-10-13
申请号：KR1020030090518
申请日：2003-12-12
Applicant: 한국과학기술연구원
CPC classification number: C07K14/705 , C12N2503/02
Abstract: 본 발명은 레트로바이러스 발현 시스템을 이용하여 α
1G T-형 칼슘 채널이 안정적으로 발현되는 HEK293 세포를 인간 Kir2.1 유전자로 형질전환시킨 세포주에 관한 것이다. 본 발명의 HEK293 세포주는 Kir2.1 (칼륨 내부 정류 채널 (potassium inwardly-rectifying channel))을 영구적으로 추가 발현함으로써 세포 막전압을 과분극쪽으로 더 낮추어 안정적인 막전압을 발현하고, 따라서 전기생리학적 방법 이외에도 고농도의 KCl에 의하여 α
1G 가 활성화된다.-
2.发明公开Ｂ형 간염 바이러스 폴리머라제와 단백질 ｐ１１의 복합체및 ＨｅｐＧ２ 세포에서 상기 복합체의 이동 조절 방법 失效乙型肝炎病毒聚合酶（HBVPOL）和蛋白质P11的复合物和用于控制HEPG2细胞中复合物运动的方法
公开(公告)号：KR1020040020210A
公开(公告)日：2004-03-09
申请号：KR1020020051729
申请日：2002-08-30
Applicant: 한국과학기술연구원
IPC: C07K19/00
CPC classification number: C07K14/005 , A61K38/00 , C07K14/4728 , C12N9/1276 , C12N2730/10122 , C12N2740/16222
Abstract: PURPOSE: A complex of hepatitis B virus polymerase(HBVpol) and protein p11 and a method for controlling movement of the complex in HepG2 cell are provided, thereby detecting a position of the complex in human liver cell and disclosing the carcinogenesis mechanism of liver cancer. CONSTITUTION: A complex of hepatitis B virus polymerase(HBVpol) and a calcium binding protein p11 by noncovalently binding moves to promyelocytic leukemia nuclear body(PMLNB). A method for controlling movement of the complex in HepG2 cell comprises adding a calcium ion concentration regulating agent to the HepG2 cell to increase or decrease the calcium ion concentration in the HepG2 cell.
Abstract translation: 目的：提供乙型肝炎病毒聚合酶（HBVpol）和蛋白质p11的复合物以及控制HepG2细胞复合物运动的方法，从而检测复合物在人肝细胞中的位置，揭示肝癌的致癌机制。 构成：乙型肝炎病毒聚合酶（HBVpol）和非结合结合的钙结合蛋白p11复合物移动到早幼粒细胞白血病核体（PMLNB）。 用于控制HepG2细胞中复合物运动的方法包括向HepG2细胞添加钙离子浓度调节剂以增加或降低HepG2细胞中的钙离子浓度。
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公开(公告)号：KR100379756B1
公开(公告)日：2003-04-11
申请号：KR1020000057916
申请日：2000-10-02
Applicant: 한국과학기술연구원
IPC: C12P41/00
Abstract: PURPOSE: Provided is an effective resolution method of chiral compounds containing hydroxy group or ester group, by using lipase produced by Burkholderia Cocovenenans SY-01I(KFCC 11111). CONSTITUTION: Chiral compounds(formula 1, 2, 3 4 and 5) containing hydroxy group or ester group are resolved by hydrolyzing and trans-esterifying using the solid lipase prepared by dialysis or lyophilizing, wherein the hydrolysis is carried out at 5-35deg.C with by phosphate buffer solution of pH7.09; and the trans-esterification is conducted at 0-55 deg.C with organic solvent and an acylating agent. The organic solvent is selected from n-hexane, ethylacetate, benzene, toluene, THF, diethylether, acetonitrile, dichloroethane, dichloromethane, 1,4-dioxane, methanol, DMSO, DMF and hexane/ethylacetate(9/1 -5/5) and the above acylating agent is chosen from vinylacetate, isopropenylacetate, anhydrous acetic acid, anhydrous propionic acid and anhydrous butyric acid.
Abstract translation: 目的：通过使用由Burkholderia Cocovenenans SY-01I（KFCC 11111）产生的脂肪酶，提供了含有羟基或酯基的手性化合物的有效拆分方法。 构成：含有羟基或酯基的手性化合物（式1,2,3和4）通过使用通过透析或冷冻干燥制备的固体脂肪酶进行水解和酯交换来拆分，其中水解在5-35℃下进行。 C用pH7.09的磷酸盐缓冲溶液; 酯化反应在0-55℃下用有机溶剂和酰化剂进行。 有机溶剂选自正己烷，乙酸乙酯，苯，甲苯，THF，乙醚，乙腈，二氯乙烷，二氯甲烷，1,4-二恶烷，甲醇，DMSO，DMF和己烷/乙酸乙酯（9/1 -5/5） 并且上述酰化剂选自乙酸乙烯酯，异丙烯基乙酸酯，无水乙酸，无水丙酸和无水丁酸。
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4.发明公开
公开(公告)号：KR1020010027211A
公开(公告)日：2001-04-06
申请号：KR1019990038840
申请日：1999-09-11
Applicant: 한국과학기술연구원
IPC: C12P41/00
Abstract: PURPOSE: A method for partitioning racemic alcohol compounds containing quaternary asymmetric carbon and a synthesis method of systhane analog are provided, thereby the produced systhane derivatives can be effectively used for exterminating harmful bacteria in plants. CONSTITUTION: The pure R- and S- isomers are partitioned from (R, S)-alcohol racemate represented by formula (1) by the esterification reaction or hydrolysis reaction of (R, S)-alcohol racemate and lipase, in organic solvents, in the presence of acyl transfer compounds and aldehyde scavenger, at 0 to 60 deg.C, in which R1 is lower alkyl or lower alkoxy-lower alkyl; R2 is linear or branched alcohol represented by -(CH2)nOH, in which n is an integer of 1 to 5; X is substituted halogen or lower alkyl group at ortho, metha and para of a phenyl ring; the lipase is produced from Candida rugosa, Pseudomonas fluorescence, and Pseudomonas cepacia; the acyl transfer compounds are vinylacetate, isopropenylacetate, and acetylenehydride; the organic solvents are normal hexane, cyclo hexane, diisopropyl ether, ethyl acetate, benzene, toluene, tetrahydrofuran, diethyl ether, acetonitrile, dichloroethane, dichloromethane, 1,4-dioxane, methanol, dimethylsulfoxide, dimethylformaldehyde, and hexane/ethylacetate; and the aldehyde scavenger is base such as triethyl amine, pyridine, piperidine, piperazine, diisopropylamine, imidazol, calcium carbonate, sodium acetate, and lithium chloride.
Abstract translation: 目的：提供一种分配含有四元不对称碳的外消旋醇化合物的方法和一种合成方法的合成方法，从而可以有效地利用生成的甲烷衍生物来消除植物中的有害细菌。 构成：通过（R，S） - 醇外消旋物和脂肪酶在有机溶剂中的酯化反应或水解反应将纯R-和S-异构体与式（1）表示的（R，S） - 醇外消旋物分隔开， 在酰基转移化合物和醛清除剂的存在下，在0至60℃，其中R 1是低级烷基或低级烷氧基 - 低级烷基; R2是由 - （CH2）nOH表示的直链或支链醇，其中n为1〜5的整数; X是苯环的邻位，甲基和对位的取代的卤素或低级烷基; 脂肪酶由假丝酵母，假单胞菌荧光和洋葱假单胞菌产生; 酰基转移化合物是乙酸乙烯酯，异丙烯基乙酸酯和乙炔氢化物; 有机溶剂为正己烷，环己烷，二异丙醚，乙酸乙酯，苯，甲苯，四氢呋喃，乙醚，乙腈，二氯乙烷，二氯甲烷，1,4-二恶烷，甲醇，二甲基亚砜，二甲基甲醛和己烷/乙酸乙酯; 醛清除剂为三乙胺，吡啶，哌啶，哌嗪，二异丙胺，咪唑，碳酸钙，乙酸钠，氯化锂等碱。
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5.发明授权
公开(公告)号：KR100478870B1
公开(公告)日：2005-03-25
申请号：KR1020020051729
申请日：2002-08-30
Applicant: 한국과학기술연구원
IPC: C07K19/00
CPC classification number: C07K14/005 , A61K38/00 , C07K14/4728 , C12N9/1276 , C12N2730/10122 , C12N2740/16222
Abstract: 본 발명은 B형 간염에 관련된 B형 간염 바이러스 폴리머라제 (HBVPol)에 비공유결합된 11 kDa의 칼슘 결합 단백질 p11의 복합체에 관한 것이다. HBVPol/p11 복합체는 세포의 핵 안에 존재하는 전골수성 백혈병 핵체 (Promyelocytic Leukemia Nuclear Body, PMLNB)로 이동하며 이 현상은 세포내 칼슘의 영향을 받아 p11이 수행한다. 본 발명은 HBV와 간암 발생 과정을 이해하고 치료의 기초가 될 수 있으며, 칼슘 저해제 스크리닝을 통한 간암치료제 개발에 이용될 수 있다.
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Patent Agency Ranking
公开(公告)号：KR100341255B1
公开(公告)日：2002-06-21
申请号：KR1019990038840
申请日：1999-09-11
Applicant: 한국과학기술연구원
IPC: C12P41/00
Abstract: 본발명은살균제로서우수한아졸화합물인시스탄의비대칭합성에있어화학식 1과같은중간체로적절히고안된 4급비대칭탄소를함유한알콜화합물의라세미체를유기용매중에서아실주게의존재하에 0 ∼ 60 ℃의온도에서리파제로트랜스에스테르화반응또는그 알콜의에스테르에대한가수분해반응을통하여광학적으로순수한각각의 R- 및 S-이성질체로분할하는방법과분할된각 이성질체로부터시스탄과그 유도체의합성방법에관한것이다. 식중, X는수소또는할로겐이며, n은탄소의수를나타내는것으로본 발명에서는 X는수소또는벤젠고리의탄소-4 위치에염소로치환된화합물과히드록시기가있는탄소의수를 1, 2, 3, 4로변환하여합성하였다. 합성한라세미체알콜들을리파제를사용하여 n=1인화합물은완전히분할하여목적화합물인아졸화합물을합성하였다. 사용한리파제들의 4급비대칭탄소에대한인지능력을측정하기위하여 n를증가시켜합성하여트랜스에스테르화반응을수행하였다. 분할을향상시키기위하여반응중 발생하는알데히드를제거할수 있는시약으로아민류를선정하여분할을향상시켰다.
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公开(公告)号：KR1020020026684A
公开(公告)日：2002-04-12
申请号：KR1020000057916
申请日：2000-10-02
Applicant: 한국과학기술연구원
IPC: C12P41/00
Abstract: PURPOSE: Provided is an effective resolution method of chiral compounds containing hydroxy group or ester group, by using lipase produced by Burkholderia Cocovenenans SY-01I(KFCC 11111). CONSTITUTION: Chiral compounds(formula 1, 2, 3 4 and 5) containing hydroxy group or ester group are resolved by hydrolyzing and trans-esterifying using the solid lipase prepared by dialysis or lyophilizing, wherein the hydrolysis is carried out at 5-35deg.C with by phosphate buffer solution of pH7.09; and the trans-esterification is conducted at 0-55 deg.C with organic solvent and an acylating agent. The organic solvent is selected from n-hexane, ethylacetate, benzene, toluene, THF, diethylether, acetonitrile, dichloroethane, dichloromethane, 1,4-dioxane, methanol, DMSO, DMF and hexane/ethylacetate(9/1 -5/5) and the above acylating agent is chosen from vinylacetate, isopropenylacetate, anhydrous acetic acid, anhydrous propionic acid and anhydrous butyric acid.
Abstract translation: 目的：通过使用伯克霍尔德氏菌SY-01I（KFCC 11111）生产的脂肪酶，提供含有羟基或酯基的手性化合物的有效解决方法。 构成：使用通过透析或冻干制备的固体脂肪酶进行水解和酯交换，分解含有羟基或酯基的手性化合物（式1,2,3,4,5），其中水解进行5-35度。 C用磷酸盐缓冲溶液pH7.09; 并且酯交换在0-55℃下与有机溶剂和酰化剂进行。 有机溶剂选自正己烷，乙酸乙酯，苯，甲苯，THF，二乙醚，乙腈，二氯乙烷，二氯甲烷，1,4-二恶烷，甲醇，DMSO，DMF和己烷/乙酸乙酯（9/1 -5/5） 并且上述酰化剂选自乙酸乙烯酯，异丙烯基乙酸酯，无水乙酸，无水丙酸和无水丁酸。
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公开(公告)号：KR1020050058587A
公开(公告)日：2005-06-17
申请号：KR1020030090518
申请日：2003-12-12
Applicant: 한국과학기술연구원
CPC classification number: C07K14/705 , C12N2503/02
Abstract: 본 발명은 레트로바이러스 발현 시스템을 이용하여 α
1G T-형 칼슘 채널이 안정적으로 발현되는 HEK293 세포를 인간 Kir2.1 유전자로 형질전환시킨 세포주에 관한 것이다. 본 발명의 HEK293 세포주는 Kir2.1 (칼륨 내부 정류 채널 (potassium inwardly-rectifying channel))을 영구적으로 추가 발현함으로써 세포 막전압을 과분극쪽으로 더 낮추어 안정적인 막전압을 발현하고, 따라서 전기생리학적 방법 이외에도 고농도의 KCl에 의하여 α
1G 가 활성화된다.-
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10.发明公开
公开(公告)号：KR1020010027210A
公开(公告)日：2001-04-06
申请号：KR1019990038839
申请日：1999-09-11
Applicant: 한국과학기술연구원
IPC: C12P41/00
Abstract: PURPOSE: Provided is a resolution method of racemic acid precursor of verapamil into (R)- and (S)-enantiomers. And a manufacturing method of pure (R)- and (S)-verapamil therefrom is also provided. The verapamil is a calcium antagonist and thus useful for treatment of hypertension. CONSTITUTION: A resolution method of racemic acid precursor of verapamil is characterized by esterifying racemic acid compound of the formula (1), in the presence of a compound containing acyl group, using hydrolase to resolve (R)- and (S)-enantiomers; hydrolyzing the (R)- and (S)-enantiomers with alcohol; and performing these procedures repeatedly. (R)-(+)- and (S)-(-)-verapamils are manufactured by the steps of: reacting (R)- or (S)- enantiomer with methanesulfonyl chloride or toluenesulfonyl chloride to obtain sulfon derivative; reacting the sulfon derivative with 2-(3,4-dimethoxyphenyl)ethylamine to prepare 2-(3,4-dimethoxyphenyl)ethyl-4-cyano-4-diisopropyl-(3,4-dimethoxyphenyl)butylamine; and methylating 2-(3,4-dimethoxyphenyl)ethyl-4-cyano-4-diisopropyl-(3,4-dimethoxyphenyl)butylamine to obtain pure (R)-(+)- and (S)-(-)-veraphil.
Abstract translation: 目的：提供维拉帕米（R） - 和（S） - 对映异构体的外消旋酸前体的分辨方法。 还提供了纯（R） - 和（S） - 维拉帕米的制造方法。 维拉帕米是钙拮抗剂，因此可用于治疗高血压。 构成：维拉帕米的外消旋酸前体的拆分方法的特征在于在含有酰基的化合物的存在下，使用水解酶分解（R） - 和（S） - 对映异构体，酯化式（1）的外消旋酸化合物。 用醇水解（R） - 和（S） - 对映异构体; 并重复执行这些步骤。 （R） - （+） - 和（S） - （ - ） - 维拉帕米通过以下步骤制备：（R） - 或（S） - 对映体与甲磺酰氯或甲苯磺酰氯反应，得到磺酰衍生物; 使磺酰衍生物与2-（3,4-二甲氧基苯基）乙胺反应制备2-（3,4-二甲氧基苯基）乙基-4-氰基-4-二异丙基 - （3,4-二甲氧基苯基）丁胺; 并将2-（3,4-二甲氧基苯基）乙基-4-氰基-4-二异丙基 - （3,4-二甲氧基苯基）丁胺甲基化得到纯的（R） - （+） - 和（S） - （ - ） - 。
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