会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 4. 发明授权
    • Steroid-activated nuclear receptors and uses therefor
    • 类固醇激活的核受体及其用途
    • US07972782B2
    • 2011-07-05
    • US11495263
    • 2006-07-27
    • Ronald M. EvansBruce Blumberg
    • Ronald M. EvansBruce Blumberg
    • C12Q1/68
    • A01K67/0275A01K2217/05A01K2227/105A01K2267/03A61K38/00C07K14/70567C07K2319/71C12N15/8509C12N2830/008C12Q1/6897G01N33/743G01N2333/90245G01N2500/00
    • A novel nuclear receptor, termed the steroid and xenobiotic receptor (SXR), a broad-specificity sensing receptor that is a novel branch of the nuclear receptor superfamily, has been discovered. SXR forms a heterodimer with RXR that can bind to and induce transcription from response elements present in steroid-inducible cytochrome P450 genes in response to hundreds of natural and synthetic compounds with biological activity, including therapeutic steroids as well as dietary steroids and lipids. Instead of hundreds of receptors, one for each inducing compound, the invention SXR receptors monitor aggregate levels of inducers to trigger production of metabolizing enzymes in a coordinated metabolic pathway. Agonists and antagonists of SXR are administered to subjects to achieve a variety of therapeutic goals dependent upon modulating metabolism of one or more endogenous steroids or xenobiotics to establish homeostasis. An assay is provided for identifying steroid drugs that are likely to cause drug interaction if administered to a subject in therapeutic amounts. Transgenic animals are also provided which express human SXR, thereby serving as useful models for human response to various agents which potentially impact P450-dependent metabolic processes.
    • 已经发现了一种称为类固醇和异种生物受体(SXR)的新型核受体,作为核受体超家族的新分支的广泛特异性感受器受体。 SXR与RXR形成异源二聚体,其可以结合并诱导存在于类固醇诱导细胞色素P450基因中的响应元件的转录,以响应数百种具有生物活性的天然和合成化合物,包括治疗类固醇以及膳食类固醇和脂质。 代替数百个受体,每个诱导化合物一个,本发明SXR受体监测诱导剂的总体水平以引发协同代谢途径中代谢酶的产生。 SXR的激动剂和拮抗剂被施用于受试者以实现依赖于调节一种或多种内源性类固醇或异种生物的代谢以建立体内平衡的多种治疗目标。 提供了用于鉴定如果以治疗量施用给受试者的可能引起药物相互作用的类固醇药物的测定。 还提供了表达人SXR的转基因动物,从而作为人类对各种可能影响P450依赖性代谢过程的药物的反应的有用模型。
    • 5. 发明申请
    • Novel steroid-activated nuclear receptors and uses therefor
    • 新型类固醇激活的核受体及其用途
    • US20070026445A1
    • 2007-02-01
    • US11495263
    • 2006-07-27
    • Ronald EvansBruce Blumberg
    • Ronald EvansBruce Blumberg
    • C12Q1/68G01N33/567G01N33/53
    • A01K67/0275A01K2217/05A01K2227/105A01K2267/03A61K38/00C07K14/70567C07K2319/71C12N15/8509C12N2830/008C12Q1/6897G01N33/743G01N2333/90245G01N2500/00
    • A novel nuclear receptor, termed the steroid and xenobiotic receptor (SXR), a broad-specificity sensing receptor that is a novel branch of the nuclear receptor superfamily, has been discovered. SXR forms a heterodimer with RXR that can bind to and induce transcription from response elements present in steroid-inducible cytochrome P450 genes in response to hundreds of natural and synthetic compounds with biological activity, including therapeutic steroids as well as dietary steroids and lipids. Instead of hundreds of receptors, one for each inducing compound, the invention SXR receptors monitor aggregate levels of inducers to trigger production of metabolizing enzymes in a coordinated metabolic pathway. Agonists and antagonists of SXR are administered to subjects to achieve a variety of therapeutic goals dependent upon modulating metabolism of one or more endogenous steroids or xenobiotics to establish homeostasis. An assay is provided for identifying steroid drugs that are likely to cause drug interaction if administered to a subject in therapeutic amounts. Transgenic animals are also provided which express human SXR, thereby serving as useful models for human response to various agents which potentially impact P450-dependent metabolic processes.
    • 已经发现了一种称为类固醇和异种生物受体(SXR)的新型核受体,作为核受体超家族的新分支的广泛特异性感受器受体。 SXR与RXR形成异源二聚体,其可以结合并诱导存在于类固醇诱导细胞色素P450基因中的响应元件的转录,以响应数百种具有生物活性的天然和合成化合物,包括治疗类固醇以及膳食类固醇和脂质。 代替数百个受体,每个诱导化合物一个,本发明SXR受体监测诱导剂的总体水平以引发协同代谢途径中代谢酶的产生。 SXR的激动剂和拮抗剂被施用于受试者以实现依赖于调节一种或多种内源性类固醇或异种生物的代谢以建立体内平衡的多种治疗目标。 提供了用于鉴定如果以治疗量施用给受试者的可能引起药物相互作用的类固醇药物的测定。 还提供了表达人SXR的转基因动物,从而作为人类对各种可能影响P450依赖性代谢过程的药物的反应的有用模型。
    • 6. 发明授权
    • High throughput functional screening of cDNAs
    • cDNA的高通量功能筛选
    • US06274321B1
    • 2001-08-14
    • US09454704
    • 1999-12-03
    • Bruce Blumberg
    • Bruce Blumberg
    • C12Q168
    • C12N15/1086
    • Methods for screening cDNAs that express a product interacting with a target molecule. Individual cDNAs are pooled and the cDNA pools are expressed to obtain expression products, for example by coupled in vitro transcription/translation. The interaction of the products with the target molecule is then assayed, for example by scintillation proximity assay (SPA), to identify pools of interest. By selectively re-pooling the cDNAs and repeating the expression and assay steps, individual cDNAs of interest can be rapidly identified. This method is readily automated in a computer-controlled device for high throughput screening. The invention also provides methods of transfecting a cell with a cDNA identified by the screening method to confer a desired property to a cell or identifying cDNAs from a pool of cDNAs by transfection into cells to confer a desired property.
    • 用于筛选表达与靶分子相互作用的产物的cDNA的方法。 汇集单个cDNA并且表达cDNA库以获得表达产物,例如通过偶联的体外转录/翻译。 然后测定产物与靶分子的相互作用,例如通过闪烁近邻测定(SPA),以鉴定感兴趣的池。 通过选择性重新汇集cDNA并重复表达和测定步骤,可以快速鉴定感兴趣的各个cDNA。 该方法在用于高通量筛选的计算机控制装置中容易自动化。 本发明还提供了通过筛选方法鉴定的cDNA转染细胞的方法,以通过转染细胞以赋予细胞所需的性质来赋予细胞所需的性质或从cDNA库鉴定cDNA。
    • 8. 发明授权
    • Human peroxisome proliferator activated receptor &ggr; compositions and methods
    • 人类过氧化物酶体增殖物激活受体γ组合物和方法
    • US06815168B1
    • 2004-11-09
    • US09587549
    • 2000-06-01
    • Marianne E. GreeneBruce Blumberg
    • Marianne E. GreeneBruce Blumberg
    • G01N3353
    • C07K14/70567
    • The invention relates generally to compositions of and methods for obtaining peroxisome proliferator-activated receptors. The invention relates as well to the DNA sequences encoding peroxisome proliferator-activated receptors, the recombinant vectors carrying those sequences, the recombinant host cells including either the sequences or vectors, and recombinant peroxisome proliferator-activated receptor polypeptides. By way of example, the invention discloses the cloning and functional expression of a peroxisome proliferator-activated receptor, designated PPAR-&ggr;, obtained from a human source. The invention includes as well, methods for using the isolated, recombinant peroxisome proliferator-activated receptor polypeptides in assays designed to select and improve substances capable of interacting with peroxisome proliferator-activated receptor polypeptides for use in diagnostic, drug design and therapeutic applications.
    • 本发明一般涉及获得过氧化物酶体增殖物激活受体的组合物和方法。 本发明还涉及编码过氧化物酶体增殖物激活受体的DNA序列,携带这些序列的重组载体,包含序列或载体的重组宿主细胞以及重组过氧化物酶体增殖物激活的受体多肽。 举例来说,本发明公开了从人源获得的称为PPAR-γ的过氧化物酶体增殖物激活受体的克隆和功能表达。 本发明还包括在测定中使用分离的重组过氧化物酶体增殖物激活受体多肽的方法,其设计用于选择和改善能够与用于诊断,药物设计和治疗应用的能够与过氧化物酶体增殖物激活受体多肽相互作用的物质。
    • 9. 发明授权
    • Method, polypeptides, nucleotide sequence of XOR-6, a vitamin D-like receptor from xenopus
    • 使用XOR-6的方法,一种来自砧木的维生素D样受体
    • US06391847B1
    • 2002-05-21
    • US08875082
    • 1997-07-17
    • Ronald M. EvansBruce BlumbergKazuhiko Umesono
    • Ronald M. EvansBruce BlumbergKazuhiko Umesono
    • A01N3718
    • C07K14/463A01K2217/05A61K38/00C07K14/70567C07K14/721
    • In accordance with the present invention, there are provided new members of the steroid receptor superfamily of receptors, a representative member of which has been designated XOR-6. Invention receptors are responsive to hydroxy, mercapto or amino benzoates, and are expressed, for example, in Xenopus laevis embryos. XOR-6 is most closely, although distantly, related to the vitamin D3 receptor (VDR). The proteins are about 73% identical in amino acid sequence in the DNA-binding domains and about 42% identical in the ligand binding domain. Like VDR, XOR-6 has an extended D region between the DNA and ligand binding domains. Notably, the region amino-terminal to the XOR-6 DNA-binding domain is extremely acidic. This may influence its ability to activate target genes. XOR-6 is not restricted to Xenopus because southern blots show the presence of XOR-6-related sequences in a variety of other vertebrates. Indeed, a human genomic clone for an XOR-6 related gene has recently been isolated. In accordance with a particular aspect of the present invention, there are also provided nucleic acid sequences encoding the above-identified receptor, as well as constructs and cells containing same, and probes derived therefrom. Furthermore, we have also discovered that hydroxy, mercapto or amino benzoates modulate the transcription activating effects of invention receptors.
    • 根据本发明,提供了类固醇受体超家族受体的新成员,其代表性成员被称为XOR-6。 发明受体对羟基,巯基或氨基苯甲酸酯有反应,并且例如在非洲爪蟾胚胎中表达。 XOR-6与维生素D3受体(VDR)有密切的关系。 蛋白质在DNA结合结构域中的氨基酸序列约为73%,配体结合域约为42%。 像VDR一样,XOR-6在DNA和配体结合域之间具有扩展的D区。 值得注意的是,XOR-6 DNA结合结构域的氨基末端区域是极酸性的。 这可能会影响其激活靶基因的能力。 XOR-6不仅限于非洲爪蟾,因为南部印迹显示在各种其他脊椎动物中存在XOR-6相关序列。 事实上,最近已经分离了XOR-6相关基因的人基因组克隆。 根据本发明的特定方面,还提供了编码上述受体的核酸序列,以及含有该受体的构建体和细胞,以及由其衍生的探针。 此外,我们还发现羟基,巯基或氨基苯甲酸酯调节本发明受体的转录激活作用。