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51. 发明授权

US5597705A DNA encoding thyroid hormone receptor compositions and methods 失效
标题翻译：编码甲状腺激素受体组成和方法的DNA
公开(公告)号：US5597705A
公开(公告)日：1997-01-28
申请号：US165708
申请日：1993-12-10
申请人： Ronald M. Evans , Cary A. Weinberger , Stanley M. Hollenberg , Vincent Giguere , Jeffrey Arriza , Catherine C. Thompson , Estelita S. Ong
发明人： Ronald M. Evans , Cary A. Weinberger , Stanley M. Hollenberg , Vincent Giguere , Jeffrey Arriza , Catherine C. Thompson , Estelita S. Ong
IPC分类号： C12N15/09 , C07K14/00 , C07K14/435 , C07K14/575 , C07K14/635 , C07K14/705 , C07K14/71 , C07K14/72 , C12N5/00 , C12N5/10 , C12N15/00 , C12N15/12 , C12N15/67 , C12P21/02 , C12Q1/68 , C12R1/91 , G01N33/50 , C22N15/62
CPC分类号： C12N15/67 , C07K14/721 , C07K14/723 , C12Q1/6897
摘要： The present invention provides a recombinant expression system for production of functional thyroid hormone receptor protein(s). The invention also provides a method to produce thyroid hormone receptor protein(s) by culturing the cells of the invention recombinant expression system. Also provided are thyroid hormone receptor protein(s) produced by the invention method. In addition, the present invention provides recombinant DNAs comprised of sequences which encode proteins having the hormone-binding and/or transcription-activating characteristics of a thyroid hormone receptor. The invention also provides various plasmids containing receptor sequences which exemplify the DNAs of the invention. The invention further provides complementary mRNAs, cells transformed with invention DNAs, and nucleic acid probes derived from invention DNAs.
摘要翻译：本发明提供了用于产生功能性甲状腺激素受体蛋白质的重组表达系统。本发明还提供了通过培养本发明的重组表达系统的细胞产生甲状腺激素受体蛋白的方法。还提供了通过本发明方法产生的甲状腺激素受体蛋白。此外，本发明提供由编码具有甲状腺激素受体的激素结合和/或转录激活特征的蛋白质的序列组成的重组DNA。本发明还提供了含有受体序列的各种质粒，其例证了本发明的DNA。本发明还提供了补体mRNA，用本发明DNA转化的细胞，以及衍生自本发明DNA的核酸探针。

52. 发明授权

US5548063A Retinoic acid receptor alpha proteins 失效
标题翻译：视黄酸受体α蛋白
公开(公告)号：US5548063A
公开(公告)日：1996-08-20
申请号：US179912
申请日：1994-01-11
申请人： Ronald M. Evans , Estelita S. Ong , Prudimar S. Segui , Catherine C. Thompson , Kazuhiko Umesono , Vincent Giguere
发明人： Ronald M. Evans , Estelita S. Ong , Prudimar S. Segui , Catherine C. Thompson , Kazuhiko Umesono , Vincent Giguere
IPC分类号： C07K14/705 , C12Q1/68
CPC分类号： C12Q1/6897 , C07K14/70567 , C07K2319/00 , C07K2319/61 , C07K2319/715 , C07K2319/81
摘要： A human retinoic acid receptor alpha protein is disclosed. The receptor is encoded by the cDNA insert of plasmid phRAR1, which has been deposited with ATCC. Methods employing chimeric receptors derived from the retinoic acid receptor are illustrated which demonstrate that the ligand for the new receptor is the retinoid, retinoic acid.
摘要翻译：公开了人视黄酸受体α蛋白。受体由已经保藏于ATCC的质粒phRAR1的cDNA插入片段编码。示出了使用衍生自视黄酸受体的嵌合受体的方法，其表明新受体的配体是类视黄醇维甲酸。

53. 发明授权

US5312732A Hormone receptor compositions and methods 失效
标题翻译：激素受体组合物和方法
公开(公告)号：US5312732A
公开(公告)日：1994-05-17
申请号：US667602
申请日：1991-03-07
申请人： Ronald M. Evans , Cary A. Weinberger , Stanley M. Hollenberg , Vincent Giguere , Jeffrey Arriza , Catherine C. Thompson , Estelita S. Ong
发明人： Ronald M. Evans , Cary A. Weinberger , Stanley M. Hollenberg , Vincent Giguere , Jeffrey Arriza , Catherine C. Thompson , Estelita S. Ong
IPC分类号： C12N15/09 , C07K14/00 , C07K14/435 , C07K14/575 , C07K14/635 , C07K14/705 , C07K14/71 , C07K14/72 , C12N5/00 , C12N5/10 , C12N15/00 , C12N15/12 , C12N15/67 , C12P21/02 , C12Q1/68 , C12R1/91 , G01N33/50 , C12N15/63
CPC分类号： C12N15/67 , C07K14/721 , C07K14/723 , C12Q1/6897
摘要： The present invention provides substantially pure DNA's comprised of sequences which encode proteins having the hormone-binding and/or transcription-activating characteristics of a glucocorticoid receptor, a mineralocorticoid receptor, or a thyroid hormone receptor. The invention also provides various plasmids containing receptor sequences which exemplify the DNA's of the invention. The invention further provides receptor proteins, including modified functional forms thereof, expressed from the DNA's (or mRNA's) of the invention. In addition to the novel receptor DNA, RNA and protein compositions, the present invention involves a bioassay for determining the functionality of a receptor protein. By using our bioassay system we have discovered that a necessary and sufficient condition for activation of transcription of a gene (G), whose transcription is activated by hormones complexed with receptors, is the presence of the hormone and its receptor in the cell (C) where (G) is located. As a result of that discovery we have also invented new methods for producing desired proteins in genetically engineered cells. Two of these methods are methods of the present invention. The first is a method for inducing transcription of a gene whose transcription is activated by hormones complexed with the receptors. The second is a method for engineering a cell and increasing and controlling production of a protein encoded by a gene whose transcription is activated by hormones complexed with receptor proteins.
摘要翻译：本发明提供了基本上纯的DNA，其由编码具有糖皮质激素受体，盐皮质激素受体或甲状腺激素受体的激素结合和/或转录激活特征的蛋白质的序列组成。本发明还提供了含有受体序列的各种质粒，其例证了本发明的DNA。本发明还提供了从本发明的DNA（或mRNA）表达的受体蛋白，包括其修饰的功能形式。除了新的受体DNA，RNA和蛋白质组合物之外，本发明涉及用于测定受体蛋白质的功能的生物测定。通过使用我们的生物测定系统，我们已经发现，激活基因（G）的转录的必要和充分条件（G），其转录由与受体复合的激素激活，是细胞中激素及其受体的存在（C）其中（G）位于。作为这一发现的结果，我们还发明了用于在遗传工程细胞中产生所需蛋白质的新方法。这些方法中的两个是本发明的方法。第一种是诱导转录由与受体复合的激素激活的基因的转录的方法。第二种是用于工程化细胞并增加和控制由受体与受体蛋白质复合的激素激活转录的基因编码的蛋白质的产生的方法。

54. 发明授权

US5298429A Bioassay for identifying ligands for steroid hormone receptors 失效
标题翻译：用于鉴定类固醇激素受体配体的生物测定
公开(公告)号：US5298429A
公开(公告)日：1994-03-29
申请号：US807135
申请日：1991-12-10
申请人： Ronald M. Evans , Stanley M. Hollenberg , Vincent Giguere
发明人： Ronald M. Evans , Stanley M. Hollenberg , Vincent Giguere
IPC分类号： C12N15/09 , C07K14/00 , C07K14/435 , C07K14/575 , C07K14/635 , C07K14/705 , C07K14/71 , C07K14/72 , C12N5/00 , C12N5/10 , C12N15/00 , C12N15/12 , C12N15/67 , C12P21/02 , C12Q1/68 , C12R1/91 , G01N33/50 , G01N30/00
CPC分类号： C12N15/67 , C07K14/721 , C07K14/723 , C12Q1/6897
摘要： Bioassays are disclosed which are useful for determining whether a compound is a hormone receptor agonist (i.e., is capable of promoting the transcription-activation activities of such receptors) or a hormone receptor antagonist (i.e., is capable of blocking the transcription-activation activities of such receptors). The invention bioassay is conducted by culturing test cells in the presence of at least one compound whose ability to function as a ligand for said receptor protein (or functional engineered or modified forms thereof) is sought to be determined. Alternatively, test cells are cultured in medium containing increasing concentrations of at least one compound whose ability to inhibit the transcription activation activity of hormone receptor agonists is sought to be determined, and a fixed concentration of at least one agonist for the receptor protein. Test cells employed in the practice of the present invention contain non-endogenous DNA which expresses hormone receptor (or functional modified forms thereof) and a DNA sequence encoding a hormone response element operatively linked to a reporter gene. The cultured cells are monitored for evidence of transcription of the reporter gene as a function of the concentration of test compound in the culture medium. The variation in transcription levels of the reporter gene as a function of concentration of test compound indicates the ability of test compound to promote or inhibit activation of transcription.
摘要翻译：公开了可用于确定化合物是激素受体激动剂（即能够促进此类受体的转录激活活性）还是激素受体拮抗剂的生物测定（即，能够阻断化合物的转录活化活性这样的受体）。本发明生物测定通过在至少一种化合物的存在下培养测试细胞来进行，该化合物的功能是用作所述受体蛋白质的配体（或其功能性工程化或修饰形式）。或者，将测试细胞在含有增加浓度的至少一种其抑制激素受体激动剂的转录激活活性的能力的化合物的培养基中培养，并测定受体蛋白质的至少一种激动剂的固定浓度。在本发明的实践中使用的测试细胞含有表达激素受体（或其功能性修饰形式）的非内源性DNA和编码与报告基因有效连接的激素应答元件的DNA序列。监测培养的细胞作为培养基中测试化合物浓度的函数的报告基因转录的证据。作为测试化合物浓度的函数的报告基因的转录水平的变化表明测试化合物促进或抑制转录激活的能力。

55. 发明授权

US5274077A Retinoic acid receptor composition 失效
标题翻译：视黄酸受体组成
公开(公告)号：US5274077A
公开(公告)日：1993-12-28
申请号：US975777
申请日：1992-11-13
申请人： Ronald M. Evans , Estelita S. Ong , Prudimar S. Segui , Catherine C. Thompson , Kazuhiko Umesono , Vincent Giguere
发明人： Ronald M. Evans , Estelita S. Ong , Prudimar S. Segui , Catherine C. Thompson , Kazuhiko Umesono , Vincent Giguere
IPC分类号： C07K14/705 , C12N15/12 , C12Q1/68 , C07K13/00
CPC分类号： C07K14/70567 , C12Q1/6897 , C07K2319/61 , C07K2319/715 , C07K2319/81
摘要： A novel retinoic acid receptor is disclosed. The novel receptor is encoded for by CDNA carried on plasmid phRAR1, which has been deposited with the American Type Culture Collection for patent purposes. Chimeric receptor proteins are also disclosed. The chimera are constructed by exchanging functional domains between the glucocorticoid, the mineralocorticoid, the estrogen-related, the thyroid and the retinoic acid receptors. In addition, a novel method for identifying functional ligands for receptor proteins is disclosed. The method, which takes advantage of the modular structure of the hormone receptors and the idea that the functional domains may be interchangeable, replaces the DNA-binding domain of a putative novel receptor with the DNA-binding domain of a known receptor such as the glucocorticoid receptor. The resulting chimeric construction, when expressed in cells, produces a hybrid receptor whose activation of a ligand--(e.g., glucocorticoid) inducible promoter is dependent on the presence of the new ligand. The novel method is illustrated in part by showing that the ligand for the new receptor protein is the retinoid, retinoic acid.
摘要翻译：公开了一种新型视黄酸受体。新型受体由携带在质粒phRAR1上的CDNA编码，其已经用美国典型培养物保藏中心专利保藏。还公开了嵌合受体蛋白。通过在糖皮质激素，盐皮质激素，雌激素相关，甲状腺和视黄酸受体之间交换功能结构来构建嵌合体。另外，公开了用于鉴定受体蛋白质的功能性配体的新方法。利用激素受体的模块化结构的方法和功能域可以互换的想法将已知受体的DNA结合结构域（例如糖皮质激素）替代推定的新受体的DNA结合结构域受体。当在细胞中表达时，产生的嵌合构型产生杂合受体，其配体（例如，糖皮质激素）诱导型启动子的活化取决于新配体的存在。该新方法部分地通过显示新受体蛋白质的配体是类视黄醇，视黄酸来说明。

56. 发明授权

US5262300A Receptors: their identification, characterization, preparation and use 失效
标题翻译：用于鉴定类固醇/甲状腺超家族受体拮抗剂的生物测定
公开(公告)号：US5262300A
公开(公告)日：1993-11-16
申请号：US797546
申请日：1991-11-25
申请人： Ronald M. Evans , Stanley M. Hollenberg
发明人： Ronald M. Evans , Stanley M. Hollenberg
IPC分类号： C07K14/72 , C12N15/85 , C12Q1/68 , G01N33/566 , G01N33/574 , G01N33/74 , A61K37/24 , C07K13/00 , C12P21/06
CPC分类号： C12N15/85 , C07K14/721 , C12Q1/6897 , G01N33/566 , G01N33/574 , G01N33/743 , C07K2319/61 , C07K2319/715 , C07K2319/81 , C12N2830/002 , G01N2333/723 , G01N2500/00
摘要： The present invention relates to bioassays for evaluating compounds as potential antagonists for members of the steroid hormone superfamily of receptor protein(s). The invention bioassay comprises culturing test cells expressing steroid receptor protein in the presence of increasing concentrations of at least one compound whose ability to inhibit the action of agonists on members of the steroid hormone superfamily of receptors is sought to be determined, and a fixed concentration of at least one agonist for said steroid hormone receptor protein(s). Test cells employed in the practice of the present invention contain DNA which expresses a member of the steroid hormone superfamily of receptor protein(s) in a form having improved trans-activation transcription activity, relative to wild-type receptor, and a DNA sequence comprising a response element for said hormone receptor protein operatively linked to a reporter gene. Improved trans-activation transcription activity is provided by receptor having a plurality of at least one parental receptor trans-activation domain selected from .tau..sub.1 or .tau..sub.2, located outside the DNA-binding and ligand-binding domains of the receptor protein. The invention assay is completed by monitoring the level of expression of reporter gene product as a function of the concentration of potential antagonist compound in the culture medium, thereby indicating the ability of potential antagonist compound(s) to inhibit activation of members of the steroid hormone superfamily of receptors.
摘要翻译：本发明涉及用于评估化合物作为受体蛋白类固醇激素超家族成员的潜在拮抗剂的生物测定法。本发明生物测定包括在增加浓度的至少一种化合物的存在下培养表达类固醇受体蛋白的测试细胞，其寻求抑制激动剂对类固醇激素超家族成员的作用的能力，并确定固定浓度至少一种用于所述类固醇激素受体蛋白的激动剂。在本发明实践中使用的测试细胞包含相对于野生型受体具有改善的反式激活转录活性形式的表达受体蛋白质的类固醇激素超家族成员的DNA，以及包含所述激素受体蛋白质与报道基因可操作地连接的反应元件。改善的反式激活转录活性由位于受体蛋白的DNA结合和配体结合结构域之外的多个至少一个选自tau1或tau2的亲本受体反式激活结构域的受体提供。通过监测报道基因产物的表达水平作为潜在的拮抗剂化合物在培养基中的浓度的函数的程度来完成本发明测定，从而表明潜在的拮抗剂化合物抑制类固醇激素成员的活化的能力受体超家族。

57. 发明授权

US5071773A Hormone receptor-related bioassays 失效
标题翻译：激素受体相关生物多样性
公开(公告)号：US5071773A
公开(公告)日：1991-12-10
申请号：US108471
申请日：1987-10-20
申请人： Ronald M. Evans , Cary A. Weinberger , Stanley M. Hollenberg , Vincent Giguere , Jeffrey Arriza , Catherine C. Thompson , Estelita S. Ong
发明人： Ronald M. Evans , Cary A. Weinberger , Stanley M. Hollenberg , Vincent Giguere , Jeffrey Arriza , Catherine C. Thompson , Estelita S. Ong
IPC分类号： C12N15/09 , C07K14/00 , C07K14/435 , C07K14/575 , C07K14/635 , C07K14/705 , C07K14/71 , C07K14/72 , C12N5/00 , C12N5/10 , C12N15/00 , C12N15/12 , C12N15/67 , C12P21/02 , C12Q1/68 , C12R1/91 , G01N33/50
CPC分类号： C12N15/67 , C07K14/721 , C07K14/723 , C12Q1/6897
摘要： The present invention discloses two hormone receptor-related bioassays. The first bioassay is useful for determining whether a protein suspected of being a hormone receptor has transcription-activating properties of a hormone receptor. The second bioassay is useful for evaluating whether compounds are functional ligands for receptor proteins. According to the first bioassay, cells that contain non-endogenous DNA which expresses a protein suspected of being a hormone receptor and which contain a DNA sequence encoding an operative hormone responsive promoter/enhancer element linked to an operative reporter gene, are cultured, the culturing being conducted in a culture medium containing a known hormone, or an analog thereof. The cultured cells are then monitored for induction of the product of the reporter gene as an indication of functional transcription-activating binding between the hormone or hormone analog and the protein suspected of being a hormone receptor. According to the second bioassay, cells that contain non-endogenous DNA which expresses hormone receptor or a functional engineered or modified form thereof, and which also contain a DNA sequence encoding an operative hormone responsive promoter/enhancer element linked to an operative reporter gene, are cultured, the culturing being conducted in culture medium containing at least one compound whose ability to functionally bind the receptor protein is sought to be determined. The cultured cells are then monitored for induction of the product of the report gene as an indicator of functional binding between the compound and the receptor.
摘要翻译：本发明公开了两种与激素受体相关的生物测定。第一种生物测定可用于确定怀疑是激素受体的蛋白质是否具有激素受体的转录激活特性。第二个生物测定可用于评估化合物是否是受体蛋白质的功能性配体。根据第一生物测定法，培养含有表达怀疑是激素受体的蛋白质并含有编码与操作性报告基因连接的操作性激素反应性启动子/增强子元件的DNA序列的非内源性DNA的细胞，培养在含有已知激素或其类似物的培养基中进行。然后监测培养的细胞以诱导报告基因的产物，作为激素或激素类似物与怀疑是激素受体的蛋白质之间的功能性转录激活结合的指示。根据第二生物测定，含有表达激素受体的非内源性DNA或其功能性工程化或修饰形式的细胞，并且还包含编码与有效的报告基因连接的操作性激素反应性启动子/增强子元件的DNA序列的细胞是培养时，寻求在含有至少一种能够与受体蛋白质功能结合的化合物的培养基中进行培养。然后监测培养的细胞以诱导报告基因的产物，作为化合物和受体之间功能性结合的指标。

58. 发明授权

US4870009A Method of obtaining gene product through the generation of transgenic animals 失效
标题翻译：通过产生转基因动物获得基因产物的方法
公开(公告)号：US4870009A
公开(公告)日：1989-09-26
申请号：US561644
申请日：1983-12-15
申请人： Ronald M. Evans , Richard D. Palmiter , Ralph L. Brinster
发明人： Ronald M. Evans , Richard D. Palmiter , Ralph L. Brinster
IPC分类号： C07K14/61 , C12N15/16 , C12N15/85 , C12N15/89
CPC分类号： C07K14/61 , C12N15/85 , C12N15/89
摘要： Mammalian genes that encode hormones are cloned and linked to strong promoter DNA sequences. The linked sequences are inserted in plasmids for amplification in prokaryotic cells, and multiple copies of the linked sequences are excised therefrom. Linked sequences are subsequently microinjected into fertilized eggs and the fertilized eggs are implanted into pseudo-pregnent females of the same species. As a result, transgenic animals are born having the linked sequences incorporated into their genomes and expressing the gene-encoded hormone. Because multiple copies of the linked sequences are frequently inserted and because production of the hormone is not limited to certain organs, as is the case with most endogenous hormones, the transgenic animals produce substantial amounts of the hormone. Hormone can be harvested from the living animal (and from its hormone-producing progeny) by extracting fluid, such as blood serum or ascites fluid, on a regular basis.
摘要翻译：编码激素的哺乳动物基因被克隆并与强启动子DNA序列连接。将连接的序列插入质粒用于在原核细胞中扩增，并从其中切除连接序列的多个拷贝。随后将连锁序列显微注射到受精卵中，将受精卵植入相同物种的假怀孕女性。结果，转基因动物出生后将连锁序列并入其基因组并表达基因编码的激素。由于连锁序列的多个拷贝经常插入，因为激素的产生不限于某些器官，如大多数内源激素的情况，转基因动物产生大量的激素。通过定期地提取液体，如血清或腹水，可以从活的动物（以及来自其激素产生的后代）中收获激素。

59. 发明申请

US20110018866A1 STRUCTURE OF THE FARNESOID X RECEPTOR LIGAND BINDING DOMAIN AND METHODS OF USE THEREFOR 失效
标题翻译： FARNESOID X受体配体结合域的结构及其使用方法
公开(公告)号：US20110018866A1
公开(公告)日：2011-01-27
申请号：US12686347
申请日：2010-01-12
申请人： Michael R. Downes , Mark A. Verdicia , Joseph P. Noel , Ronald M. Evans , Lindsey J. Bowman , Marianne Bowman
发明人： Michael R. Downes , Mark A. Verdicia , Joseph P. Noel , Ronald M. Evans , Lindsey J. Bowman , Marianne Bowman
IPC分类号： C07C229/44 , C07K14/72 , A61K38/16 , A61K31/216 , C07D317/58 , A61K31/36 , C07J9/00 , A61K31/575 , C07D261/08 , A61K31/42 , G06G7/58 , G06T15/00
CPC分类号： C07K14/70567 , C07K2299/00 , G01N33/743 , G01N2500/00 , G06F19/16 , G06F19/706
摘要： The present invention provides compositions comprising the ligand binding domain (LBD) of a farnesoid X receptor (FXR) in crystalline form. In alternative embodiments, the LBD of FXR is complexed with a ligand therefor. There are provided high resolution structures of FXR complexed with a novel high affinity agonist fexaramine. The discovered structure of a FXR LBD provides the first three-dimensional view of the structural basis for FXR ligand binding. The present invention further provides a computer for producing a time-dimensional representation of FXR or a complex thereof, and a computer for determining at least a portion of the structure coordinates of FXR or a complex thereof. The present invention further provides methods of using this structural information to predict molecules capable of binding to FXR; to identify compounds with agonist, antagonist or partial agonist activity for FXR; and to determine whether a test compound is capable of binding to the LBD of FXR. The present invention further provides compositions comprising compounds identified by such invention methods.
摘要翻译：本发明提供了包含结晶形式的法呢甾X受体（FXR）的配体结合结构域（LBD）的组合物。在替代实施方案中，FXR的LBD与其配体复合。提供了与新型高亲和力激动剂福沙康胺复合的FXR的高分辨率结构。所发现的FXR LBD的结构提供了FXR配体结合的结构基础的第一个三维视图。本发明还提供一种用于产生FXR或其复数的时间维度表示的计算机，以及用于确定FXR或其复数的结构坐标的至少一部分的计算机。本发明还提供使用该结构信息来预测能够结合FXR的分子的方法; 识别FXR激动剂，拮抗剂或部分激动剂活性的化合物; 并确定测试化合物是否能够结合FXR的LBD。本发明还提供包含通过本发明方法鉴定的化合物的组合物。

60. 发明授权

US07413853B2 Modulation of metabolism of steroids and xenobiotics 失效
标题翻译：调节类固醇和异生素的代谢
公开(公告)号：US07413853B2
公开(公告)日：2008-08-19
申请号：US10482555
申请日：2002-07-09
申请人： Ronald M. Evans , Wen Xie
发明人： Ronald M. Evans , Wen Xie
IPC分类号： C12Q1/68 , C12Q1/48 , C12Q1/34 , G01N33/53
CPC分类号： A01K67/0275 , A01K67/0276 , A01K2207/15 , A01K2217/00 , A01K2217/072 , A01K2217/075 , A01K2227/105 , A01K2267/03 , C12N9/12 , C12N15/8509 , C12Q1/26 , G01N33/573 , G01N2333/70567 , G01N2333/90245 , G01N2333/91091 , G01N2500/00
摘要： In accordance with the present invention, there are provided methods for modulating Phase II conjugating enzymes such as, for example, UGTs. Phase II conjugating enzymes such as UGTs function in concert with Phase I monooxygenase enzymes such as cytochrome P450 enzymes (CYPs) to eliminate steroids and xenobiotics. Nuclear receptors SXR/PXR and CAR are xenosensors regulating expression of CYP genes such as CYP3A and 2B. The ability of this group of receptors to regulate expression of UGT in response to steroids and/or xenobiotics provides novel approaches for direct regulation/activation of a glucuronidation pathway, thereby providing methods to achieve physiologic homeostasis with respect to steroids and/or xenobiotics. SXR/PXR and CAR regulation/activation of UGT represents the first evidence of receptors that can transduce/transactivate both Phase I and Phase II adaptive hepatic response. In another aspect, the present invention also provides transgenic rodents expressing one or more of SXR, CAR or PXR.
摘要翻译：根据本发明，提供了调节II期缀合酶的方法，例如UGT。 II型缀合酶如UGT与I期单加氧酶如细胞色素P450酶（CYPs）协同作用，以消除类固醇和异种生物。核受体SXR / PXR和CAR是调节CYP3A和2B等CYP基因表达的异种传感器。该组受体调节UGT响应于类固醇和/或异种生物体的表达的能力提供了用于直接调节/激活葡糖苷酸化途径的新方法，从而提供了相对于类固醇和/或异生物获得生理平衡的方法。 UGT的SXR / PXR和CAR调节/活化代表可以转导/反式激活I期和II期适应性肝反应的受体的第一个证据。另一方面，本发明还提供表达SXR，CAR或PXR中的一种或多种的转基因啮齿动物。

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