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11. 发明授权

US5891631A Methods relating tosterol regulatory element binding proteins 失效
标题翻译：与甾醇调节元件结合蛋白相关的方法
公开(公告)号：US5891631A
公开(公告)日：1999-04-06
申请号：US668123
申请日：1996-06-14
申请人： Joseph L. Goldstein , Michael S. Brown , Michael R. Briggs , Xiaodong Wang
发明人： Joseph L. Goldstein , Michael S. Brown , Michael R. Briggs , Xiaodong Wang
IPC分类号： C07K14/47 , C07K14/525 , C07K14/61 , C12N1/21 , C12N9/72 , C12N15/12 , C12N15/67 , C12N15/85 , C12P21/08 , C12Q1/68 , G01N33/53
CPC分类号： C07K14/525 , C07K14/4702 , C07K14/61 , C12N15/67 , C12N15/85 , C12N9/6459 , C12Y304/21069 , C12N2830/002 , C12N2830/008 , C12N2830/15 , C12N2830/85
摘要： A sterol regulatory element (SRE) binding protein (SREBP) which activates transcription from SREs, such as SRE-1 of the low intensity lipoprotein (LDL) receptor gene, is disclosed, as are DNA segments encoding SREBPs such as an SREBP-1 or SREBP-2. Also described are methods for using SREBP to promote SRE-mediated transcription and LDL receptor production in the presence of sterols, and screening assay for the identification of further agents with such properties. The SREBP and other agents may be used to reduce plasma cholesterol levels and to treat various medical problems associated with hypercholesterolemia.
摘要翻译：还公开了激活SREs的转录的固醇调节元件（SREBP）结合蛋白（SREBP），例如低密度脂蛋白（LDL）受体基因的SRE-1，编码SREBP的DNA片段如SREBP-1或 SREBP-2。还描述了使用SREBP在甾醇存在下促进SRE介导的转录和LDL受体产生的方法，并筛选用于鉴定具有这些性质的其它药剂的测定法。 SREBP和其他药剂可用于降低血浆胆固醇水平并治疗与高胆固醇血症相关的各种医疗问题。

12. 发明申请

US20110184047A1 RNAI MODULATION OF SCAP AND THERAPEUTIC USES THEREOF 有权
标题翻译： RNAI调节SCAP及其治疗方法
公开(公告)号：US20110184047A1
公开(公告)日：2011-07-28
申请号：US13080334
申请日：2011-04-05
申请人： Juergen Soutschek , Pamela Tan , Jay D. Horton , Michael S. Brown , Joseph L. Goldstein , Young-Ah Moon
发明人： Juergen Soutschek , Pamela Tan , Jay D. Horton , Michael S. Brown , Joseph L. Goldstein , Young-Ah Moon
IPC分类号： A61K31/7052 , C07H21/02 , C12N5/00 , C12N15/63 , A61P1/16 , A61P9/00 , A61P3/00
CPC分类号： C12N15/113 , C12N2310/14 , C12N2310/314 , C12N2310/315 , C12N2310/321 , C12N2310/322 , C12N2310/346 , C12N2310/3515 , C12N2310/3521
摘要： The invention relates to a double-stranded ribonucleic acid (dsRNA) for inhibiting the expression of a SCAP gene (Human SCAP gene), comprising an antisense strand having a nucleotide sequence which is less that 30 nucleotides in length, generally 19-25 nucleotides in length, and which is substantially complementary to at least a part of a SCAP gene. The invention also relates to a pharmaceutical composition comprising the dsRNA together with a pharmaceutically acceptable carrier; methods for treating diseases caused by Human SCAP expression and the expression of a SCAP gene using the pharmaceutical composition; and methods for inhibiting the expression of a SCAP gene in a cell.
摘要翻译：本发明涉及用于抑制SCAP基因（人SCAP基因）表达的双链核糖核酸（dsRNA），其包含具有长度小于30个核苷酸的核苷酸序列的反义链，通常为19-25个核苷酸长度，并且其与SCAP基因的至少一部分基本上互补。本发明还涉及包含dsRNA与药学上可接受的载体的药物组合物; 用于治疗由人SCAP表达引起的疾病和使用该药物组合物表达SCAP基因的方法; 以及抑制细胞中SCAP基因表达的方法。

13. 发明授权

US06936431B2 Methods and compositions for inhibiting farnesyl transferase enzyme 失效
标题翻译：抑制法呢基转移酶的方法和组合物
公开(公告)号：US06936431B2
公开(公告)日：2005-08-30
申请号：US10083894
申请日：2002-02-27
申请人： Michael S. Brown , Joseph L. Goldstein , Yuval Reiss
发明人： Michael S. Brown , Joseph L. Goldstein , Yuval Reiss
IPC分类号： A61K38/00 , C07K5/103 , C07K7/06 , C07K14/82 , C12N9/10 , C12Q1/48
CPC分类号： C07K7/06 , A61K38/00 , C07K5/1013 , C07K14/82 , C12N9/1085 , Y10S435/815
摘要： Disclosed are methods and compositions for the identification, characterization and inhibition of farnesyl protein transferases, enzymes involved in the farnesylation of various cellular proteins, including cancer related ras proteins such as p21ras. One farnesyl protein transferase which is disclosed herein exhibits a molecular weight of between about 70,000 and about 100,000 upon gel exclusion chromatography. The enzyme appears to comprise one or two subunits of approximately 50 kDa each. Methods are disclosed for assay and purification of the enzyme, as well as procedures for using the purified enzyme in screening protocols for the identification of possible anticancer agents which inhibit the enzyme and thereby prevent expression of proteins such as p21ras. Also disclosed is a families of compounds which act either as false substrates for the enzyme or as pure inhibitors and can therefore be employed for inhibition of the enzyme. The most potent inhibitors are ones in which phenylalanine occurs at the third position of a tetrapeptide whose amino terminus is cysteine.
摘要翻译：公开了用于鉴定，表征和抑制法呢基蛋白转移酶的方法和组合物，涉及各种细胞蛋白质的法呢基化的酶，包括癌症相关的ras蛋白如p21Ras。本文公开的一种法呢基蛋白转移酶在凝胶排阻色谱上显示约70,000至约100,000的分子量。该酶似乎包含一个或两个约50kDa的亚单位。公开了用于酶的测定和纯化的方法，以及在筛选方案中使用纯化酶鉴定可能的抗癌剂的方法，所述抗癌剂抑制酶，从而阻止蛋白质如p21的表达 >。还公开了作为酶的假底物或纯抑制剂的化合物家族，因此可用于抑制酶。最有效的抑制剂是其氨基末端是半胱氨酸的四肽的第三位发生苯丙氨酸的抑制剂。

14. 发明授权

US06322962B1 Sterol-regulated Site-1 protease and assays of modulators thereof 有权
标题翻译：甾醇调节位点-1蛋白酶及其调节剂的测定
公开(公告)号：US06322962B1
公开(公告)日：2001-11-27
申请号：US09360237
申请日：1999-07-23
申请人： Michael S. Brown , Dong Cheng , Peter J. Espenshade , Joseph L. Goldstein , Robert B. Rawson , Juro Sakai
发明人： Michael S. Brown , Dong Cheng , Peter J. Espenshade , Joseph L. Goldstein , Robert B. Rawson , Juro Sakai
IPC分类号： C12Q100
CPC分类号： C12N9/6454 , A01K2217/05 , C07K2319/00
摘要： The invention provides assays for the identification of modulators of Site-1 protease. Further provided by the invention are expression constructs and the transgenic cells useful for the development of such assays for Site-1 specific protease. The cells allow the implementation of in vitro assays for potential modulators of Site-specific proteases. Still further provided by the invention are in vitro assays employing Site-1 protease which has been isolated from cells.
摘要翻译：本发明提供了用于鉴定Site-1蛋白酶调节剂的测定法。本发明进一步提供的是用于开发Site-1特异性蛋白酶的这种测定的表达构建体和转基因细胞。这些细胞允许对位点特异性蛋白酶的潜在调节剂进行体外测定。本发明进一步提供的是使用已经从细胞中分离出的Site-1蛋白酶的体外测定。

15. 发明授权

US5256545A Sterol Regulatory Elements 失效
标题翻译：甾醇调节元素
公开(公告)号：US5256545A
公开(公告)日：1993-10-26
申请号：US425852
申请日：1989-10-20
申请人： Michael S. Brown , Joseph L. Goldstein , David W. Russell , Thomas C. Sudhof
发明人： Michael S. Brown , Joseph L. Goldstein , David W. Russell , Thomas C. Sudhof
IPC分类号： C12N15/85 , C12N15/11 , C12N5/10 , C12N15/63
CPC分类号： C12N15/85
摘要： Disclosed are discrete functionally translocatable DNA segments, termed Sterol Regulatory Elements (SREs), which are fused to heterologous structural genes to provide sterol regulatory capability to the thus formed hybrid gene. The hybrid genes respond to sterols by decreasing the production of messenger RNA. The SRE segments contain as their primary functional nucleotide sequence, a 16 bp sequence referred to as direct repeat 2, isolated from the 5' regions of the human LDL receptor gene. DNA segments which include this 16 nucleotide long sequence similarly confer sterol regulatory capability to previously known promoters such as the HSV TK promoter. Also disclosed are discrete sequences which confer positive transcription promotion to heterologous structural genes and promoters without conferring sterol responsivity. Methods are disclosed for employing these genetic control elements in a myriad of embodiments which provide for a fine-tune control of heterologous genes. Methods are also disclosed for employing the SRE in a screening assay for drugs capable of stimulating the cell to synthesize LDL receptors.
摘要翻译：公开了离散的功能可转位DNA片段，称为Sterol调节元件（SRE），其与异源结构基因融合以向由此形成的杂合基因提供固醇调节能力。杂交基因通过降低信使RNA的产生来响应甾醇。 SRE片段包含从人LDL受体基因的5'区域分离的作为其主要功能核苷酸序列的16bp序列，称为直接重复序列2。包括该16个核苷酸长序列的DNA片段类似地赋予先前已知的启动子如HSV TK启动子的甾醇调节能力。还公开了对异源结构基因和启动子赋予阳性转录促进剂而不赋予固醇反应性的离散序列。公开了在无数个实施例中使用这些遗传控制元件的方法，其提供异源基因的微调控制。还公开了在能够刺激细胞合成LDL受体的药物的筛选测定中使用SRE的方法。

16. 发明授权

US07919613B2 RNAi modulation of SCAP and therapeutic uses thereof 有权
标题翻译： SCAP的RNAi调节及其治疗用途
公开(公告)号：US07919613B2
公开(公告)日：2011-04-05
申请号：US12749159
申请日：2010-03-29
申请人： Juergen Soutschek , Pamela Tan , Jay D. Horton , Michael S. Brown , Joseph L. Goldstein , Young-Ah Moon
发明人： Juergen Soutschek , Pamela Tan , Jay D. Horton , Michael S. Brown , Joseph L. Goldstein , Young-Ah Moon
IPC分类号： C07H21/04 , C07H21/02 , A61K48/00 , C12N15/63 , C12N15/85
CPC分类号： C12N15/113 , C12N2310/14 , C12N2310/314 , C12N2310/315 , C12N2310/321 , C12N2310/322 , C12N2310/346 , C12N2310/3515 , C12N2310/3521
摘要： The invention relates to a double-stranded ribonucleic acid (dsRNA) for inhibiting the expression of a SCAP gene (Human SCAP gene), comprising an antisense strand having a nucleotide sequence which is less that 30 nucleotides in length, generally 19-25 nucleotides in length, and which is substantially complementary to at least a part of a SCAP gene. The invention also relates to a pharmaceutical composition comprising the dsRNA together with a pharmaceutically acceptable carrier; methods for treating diseases caused by Human SCAP expression and the expression of a SCAP gene using the pharmaceutical composition; and methods for inhibiting the expression of a SCAP gene in a cell.
摘要翻译：本发明涉及用于抑制SCAP基因（人SCAP基因）表达的双链核糖核酸（dsRNA），其包含具有长度小于30个核苷酸的核苷酸序列的反义链，通常为19-25个核苷酸长度，并且其与SCAP基因的至少一部分基本上互补。本发明还涉及包含dsRNA与药学上可接受的载体的药物组合物; 用于治疗由人SCAP表达引起的疾病和使用该药物组合物表达SCAP基因的方法; 以及抑制细胞中SCAP基因表达的方法。

17. 发明授权

US5962243A Methods for the identification of farnesyltransferase inhibitors 失效
标题翻译：鉴定法呢基转移酶抑制剂的方法
公开(公告)号：US5962243A
公开(公告)日：1999-10-05
申请号：US429964
申请日：1995-04-27
申请人： Michael S. Brown , Joseph L. Goldstein , Guy L. James
发明人： Michael S. Brown , Joseph L. Goldstein , Guy L. James
IPC分类号： A61K38/00 , C07K5/103 , C07K7/06 , C07K14/82 , C12N9/10 , C12Q1/48 , C07H21/04
CPC分类号： C07K5/1013 , C07K14/82 , C07K7/06 , C12N9/1085 , C12Q1/48 , A61K38/00
摘要： Disclosed are methods and compositions for the identification of inhibitors of farnesyltransferase enzymes involved in the prenylation of various cellular proteins, including cancer related ras proteins, such as p21.sup.ras, particularly, K-rasB. Enclosed are procedures for using purified farnesyltransferase enzymes and K-rasB proteins in screening protocols for the identification of possible anticancer agents that inhibit the enzyme and thereby prevent prenylation of proteins such as K-RasB.
摘要翻译：公开了用于鉴定参与各种细胞蛋白（包括癌症相关的ras蛋白，例如p21ras，特别是K-rasB）的异戊烯基化的法呢基转移酶的抑制剂的方法和组合物。包括在筛选方案中使用纯化的法呢基转移酶和K-rasB蛋白的程序，用于鉴定抑制酶的可能的抗癌剂，从而防止诸如K-RasB的蛋白质的异戊二酰化。

18. 发明授权

US5843941A Ras farnesyl transferase inhibitors 失效
标题翻译： Ras法呢基转移酶抑制剂
公开(公告)号：US5843941A
公开(公告)日：1998-12-01
申请号：US313068
申请日：1994-09-26
申请人： James C. Marsters, Jr. , Michael S. Brown , Craig W. Crowley , Joseph L. Goldstein , Guy L. James , Robert S. McDowell , David Oare , Thomas E. Rawson , Mark Reynolds , Todd C. Somers
发明人： James C. Marsters, Jr. , Michael S. Brown , Craig W. Crowley , Joseph L. Goldstein , Guy L. James , Robert S. McDowell , David Oare , Thomas E. Rawson , Mark Reynolds , Todd C. Somers
IPC分类号： A61K31/55 , A61K31/551 , A61K38/00 , A61P31/04 , A61P35/00 , C07D223/16 , C07D243/10 , C07D243/14 , C07D243/24 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/06 , C07D409/06 , C07D409/14 , C07D417/12 , C07D417/14 , C07D487/04 , C07D498/04 , C07D513/04 , C07K5/02 , C07K5/06 , C07K5/078 , C07K5/08 , C07K5/083 , C07K5/097 , C07K5/10 , C07K5/103 , C07K5/117
CPC分类号： C07D223/16 , C07D243/10 , C07D243/24 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/06 , C07D409/14 , C07D487/04 , C07D513/04 , C07K5/0207 , C07K5/0606 , C07K5/06139 , C07K5/06191 , C07K5/081 , C07K5/0821 , C07K5/0827 , C07K5/1013 , C07K5/1024 , C07K5/1027 , A61K38/00
摘要： Benzodiazepine derivatives represented by the structure below are disclosed that act as potent inhibitors of ras farnesyl:protein transferase. Pharmaceutical compositions containing these benzodiazepines are provided for treatment of diseases foe which inhibition of the ras farnesyl:protein transferase as indicated. ##STR1##
摘要翻译： PCT No.PCT / US94 / 05157 Sec。 371日期：1994年9月26日 102（e）1994年9月26日PCT PCT 1994年5月10日PCT公布。第WO94 / 26723号公报 1994年11月24日公开了由以下结构表示的苯并二氮杂衍生物，其作为法西诺酯：蛋白转移酶的有效抑制剂。提供含有这些苯并二氮杂的药物组合物，用于治疗如所指出的对法拉西蛋白转移酶的抑制作用的疾病。

19. 发明授权

US5532359A Ras farnesyl transferase inhibitors 失效
标题翻译： Ras法呢基转移酶抑制剂
公开(公告)号：US5532359A
公开(公告)日：1996-07-02
申请号：US328595
申请日：1994-10-25
申请人： James C. Marsters, Jr. , Michael S. Brown , Craig W. Crowley , Joseph L. Goldstein , Guy L. James , Robert S. McDowell , David Oare , Thomas E. Rawson , Mark Reynolds , Todd C. Somers
发明人： James C. Marsters, Jr. , Michael S. Brown , Craig W. Crowley , Joseph L. Goldstein , Guy L. James , Robert S. McDowell , David Oare , Thomas E. Rawson , Mark Reynolds , Todd C. Somers
IPC分类号： A61K31/55 , A61K31/551 , A61K38/00 , A61P31/04 , A61P35/00 , C07D223/16 , C07D243/10 , C07D243/14 , C07D243/24 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/06 , C07D409/06 , C07D409/14 , C07D417/12 , C07D417/14 , C07D487/04 , C07D498/04 , C07D513/04 , C07K5/02 , C07K5/06 , C07K5/078 , C07K5/08 , C07K5/083 , C07K5/097 , C07K5/10 , C07K5/103 , C07K5/117 , C07D223/18
CPC分类号： C07D223/16 , C07D243/10 , C07D243/24 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/06 , C07D409/14 , C07D487/04 , C07D513/04 , C07K5/0207 , C07K5/0606 , C07K5/06139 , C07K5/06191 , C07K5/081 , C07K5/0821 , C07K5/0827 , C07K5/1013 , C07K5/1024 , C07K5/1027 , A61K38/00
摘要： Benzodiazepine derivatives are disclosed that act as potent inhibitors of ras farnesyl:protein transferase. Pharmaceutical compositions containing these benzodiazepines are provided for treatment of diseases for which inhibition of the ras farnesyl:protein transferase is indicated. Also disclosed are benzazepines of the following general formula (II) having similar utility as the aforementioned benzodiazepines: ##STR1##
摘要翻译：公开了苯并二氮杂衍生物，其作为法拉第鞭毛蛋白的有效抑制剂：蛋白质转移酶。提供含有这些苯二氮卓类药物的药物组合物，用于治疗对法拉第法：蛋白转移酶的抑制作用的疾病的治疗。还公开了具有与上述苯并二氮杂类似的效用的以下通式（II）的苯并吖庚因：

20. 发明授权

US5498696A Sterol regulatory element binding proteins and their use in screening assays 失效
标题翻译：甾醇调节元件结合蛋白及其在筛选试验中的应用
公开(公告)号：US5498696A
公开(公告)日：1996-03-12
申请号：US61697
申请日：1993-05-13
申请人： Michael R. Briggs , Michael S. Brown , Joseph L. Goldstein , Xiaodong Wang
发明人： Michael R. Briggs , Michael S. Brown , Joseph L. Goldstein , Xiaodong Wang
IPC分类号： C07K14/47 , C12N15/67
CPC分类号： C12N15/67 , C07K14/4702
摘要： A nuclear protein which binds sterol regulatory elements (SREs), such as SRE-1 of the low density lipoprotein (LDL) receptor gene, and mediates sterol-regulated transcription of the LDL receptor gene is disclosed. Also described are screening assay and methods for the identification of agents capable of promoting LDL receptor gene transcription for use in reducing plasma cholesterol and treating the various medical problems associated therewith.
摘要翻译：公开了结合固醇调节元件（SREs）的核蛋白，例如低密度脂蛋白（LDL）受体基因的SRE-1，并介导LDL受体基因的固醇调节的转录。还描述了用于鉴定能够促进LDL受体基因转录用于降低血浆胆固醇并治疗与其相关的各种医学问题的试剂的筛选测定和方法。

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