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51 条记录 (耗时 0.069 秒)

    Human n-methyl-d-aspartate receptor type 1 subunits, DNA encoding same and uses therefor
    31.
    发明授权
    Human n-methyl-d-aspartate receptor type 1 subunits, DNA encoding same and uses therefor 失效
    人类N-甲基-D-天冬氨酸受体1型亚基，编码相同的DNA并用于其中

    公开(公告)号：US6033865A

    公开(公告)日：2000-03-07

    申请号：US480474

    申请日：1995-06-06

    申请人： Lorrie P. Daggett ,  Steven B. Ellis ,  Chen Wang Liaw

    发明人： Lorrie P. Daggett ,  Steven B. Ellis ,  Chen Wang Liaw

    IPC分类号： C12N15/09 ,  A61K38/00 ,  C07K14/705 ,  C07K16/28 ,  C12N5/10 ,  C12N15/12 ,  C12P21/02 ,  C12P21/08 ,  C12Q1/02 ,  C12Q1/68 ,  C12R1/91 ,  G01N33/50 ,  G01N33/68 ,  C12N15/10 ,  C07K1/00 ,  G01N33/566

    CPC分类号： G01N33/5008 ,  C07K14/70571 ,  G01N33/502 ,  G01N33/5041 ,  G01N33/5058 ,  G01N33/5091 ,  G01N33/6872 ,  A01K2217/05 ,  A61K38/00 ,  G01N2333/70571

    摘要： In accordance with the present invention, there are provided nucleic acids encoding human NMDA receptor protein subunits and the proteins encoded thereby. The NMDA receptor subunits of the invention comprise components of NMDA receptors that have cation-selective channels and bind glutamate and NMDA. In one aspect of the invention, the nucleic acids encode NMDAR1 and NMDAR2 subunits of human NMDA receptors. In a preferred embodiment, the invention nucleic acids encode NMDAR1, NMDAR2A and NMDAR2C subunits of human NMDA receptors. In addition to being useful for the production of NMDA receptor subunit proteins, these nucleic acids are also useful as probes, thus enabling those skilled in the art, without undue experimentation, to identify and isolate related human receptor subunits. Functional glutamate receptors can be assembled, in accordance with the present invention, from a plurality of one type of NMDA receptor subunit protein (homomeric) or from a mixture of two or more types of subunit proteins (heteromeric). In addition to disclosing novel NMDA receptor protein subunits, the present invention also comprises methods for using such receptor subunits to identify and characterize compounds which affect the function of such receptors, e.g., agonists, antagonists, and modulators of glutamate receptor function. The invention also comprises methods for determining whether unknown protein(s) are functional as NMDA receptor subunits.

    摘要翻译： 根据本发明，提供了编码人NMDA受体蛋白质亚基的核酸和由此编码的蛋白质。 本发明的NMDA受体亚基包含具有阳离子选择性通道并结合谷氨酸和NMDA的NMDA受体的组分。 在本发明的一个方面，核酸编码人NMDA受体的NMDAR1和NMDAR2亚基。 在优选的实施方案中，本发明核酸编码人NMDA受体的NMDAR1，NMDAR2A和NMDAR2C亚基。 除了可用于产生NMDA受体亚基蛋白之外，这些核酸也可用作探针，因此使得本领域技术人员无需过多的实验来鉴定和分离相关的人受体亚单位。 功能性谷氨酸受体可以根据本发明从多种一种NMDA受体亚基蛋白（同源性）或两种或更多种亚基蛋白（异聚体）的混合物组装。 除了公开新的NMDA受体蛋白质亚基之外，本发明还包括使用这些受体亚基来鉴定和表征影响这些受体功能的化合物的方法，例如激动剂，拮抗剂和谷氨酸受体功能的调节剂。 本发明还包括用于确定未知蛋白质是否用作NMDA受体亚基的方法。

    Automated analysis equipment and assay method for detecting cell surface protein and/or cytoplasmic receptor function using same
    38.
    发明授权
    Automated analysis equipment and assay method for detecting cell surface protein and/or cytoplasmic receptor function using same 失效
    使用其自动分析设备和检测细胞表面蛋白质和/或细胞质受体功能的测定方法

    公开(公告)号：US5670113A

    公开(公告)日：1997-09-23

    申请号：US244985

    申请日：1994-06-20

    申请人： Michael Anthony Akong ,  Michael Miller Harpold ,  Gonul Velicelebi ,  Paul Brust

    发明人： Michael Anthony Akong ,  Michael Miller Harpold ,  Gonul Velicelebi ,  Paul Brust

    IPC分类号： G01N33/48 ,  G01N33/50 ,  G01N33/68 ,  G01N35/02 ,  G01N35/04 ,  G01N35/10 ,  G01N21/64 ,  G01J3/42

    CPC分类号： G01N33/6872 ,  G01N21/6452 ,  G01N33/5008 ,  G01N33/502 ,  G01N33/5058 ,  G01N35/028 ,  G01N2035/042 ,  G01N21/6428 ,  G01N2333/705 ,  G01N2500/00 ,  G01N35/109 ,  Y10S436/80 ,  Y10S436/807 ,  Y10S436/809 ,  Y10T436/11 ,  Y10T436/115831

    摘要： Automated measurement apparatus and methods for automated drug screening and for studying ion channel and cell surface receptor activity are provided. The apparatus is designed to initiate and measure rapid or transient events, such as cell receptor and/or ion channel activity. The apparatus can effect measurements of transient reactions in or more samples in a multi-well container, initiate the reaction with reagent addition and measure a resulting attribute of the sample for a period of time. The apparatus is capable of substantially continuously measuring and recording data corresponding to the measured attribute before, during and after initiation of the reaction so that a time course of the rapid or transient event is determined. Automated drug screening methods and methods for studying receptor and ion channel activity using the apparatus are also provided. The drug screening assays identify compounds that activate, inhibit or potentiate cellular ion channel or receptor activity.

    摘要翻译： PCT No.PCT / US92 / 11090 Sec。 371日期：1994年6月20日 102（e）日期1994年6月20日PCT提交1992年12月13日PCT公布。 出版物WO93 / 13423 日期1993年7月8日提供自动化药物筛选和研究离子通道和细胞表面受体活性的自动测量装置和方法。 该装置被设计为启动和测量诸如细胞受体和/或离子通道活性的快速或瞬时事件。 该装置可以实现多孔容器中或多个样品中的多个样品中的瞬态反应的测量，通过加入试剂启动反应并测量样品的结果属性一段时间。 该装置能够在反应开始之前，期间和之后基本上连续地测量和记录对应于测量属性的数据，从而确定快速或瞬态事件的时间过程。 还提供了使用该装置研究受体和离子通道活性的自动药物筛选方法和方法。 药物筛选试验鉴定激活，抑制或增强细胞离子通道或受体活性的化合物。

    Peptide and peptide analog protease inhibitors
    39.
    发明授权
    Peptide and peptide analog protease inhibitors 失效
    肽和肽类似物蛋白酶抑制剂

    公开(公告)号：US6015879A

    公开(公告)日：2000-01-18

    申请号：US442662

    申请日：1995-05-17

    申请人： Ian Alexander McDonald ,  Elisabeth Albrecht ,  Benito Munoz

    发明人： Ian Alexander McDonald ,  Elisabeth Albrecht ,  Benito Munoz

    IPC分类号： A61K38/00 ,  A61K31/00 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  C07C237/22 ,  C07K5/02 ,  C07K5/06 ,  C07K5/065 ,  C07K5/078 ,  C07K5/08 ,  C07K5/083 ,  A61K38/06

    CPC分类号： C07K5/0808 ,  C07C237/22 ,  C07K5/0202 ,  C07K5/0205 ,  C07K5/06043 ,  C07K5/06078 ,  C07K5/06139 ,  C07K5/06165 ,  C07K5/06191 ,  A61K38/00

    摘要： Methods of use of compounds and compounds for the treatment of disorders characterized by the cerebral deposition of amyloid are provided Among the compounds are those of formulae I and II: ##STR1## in which R.sub.1 is preferably 2-methyl propene, 2-butene, cyclohexyl or cyclohexylmethyl; R.sub.2, R.sub.4, and R.sub.8 are each independently methyl or ethyl; R.sub.3 is preferably iso-butyl or phenyl; R.sub.5 is preferably iso-butyl; R.sub.6 is H or methyl; R.sub.7 --(Q).sub.n is preferably benzyloxycarbonyl or acetyl; Q is preferably --C(O)--; R.sub.B is preferbly iso-butyl; --R.sub.A =--(T).sub.m --(D).sub.m --R.sub.1, is which T is preferably oxygen or carbon, and D is preferably a mono-unsaturated C.sub.3-4 alkenyl being more preferred; and X is preferably an .alpha.-ketoester or .alpha.-ketoamide or aldehyde.

    摘要翻译： 提供化合物和化合物用于治疗以沉淀淀粉样蛋白为特征的疾病的方法在这些化合物中是式I和II的化合物：其中R 1优选为2-甲基丙烯，2-丁烯，环己基或环己基甲基; R2，R4和R8各自独立地是甲基或乙基; R3优选为异丁基或苯基; R5优选为异丁基; R6是H或甲基; R7-（Q）n优选为苄氧羰基或乙酰基; Q优选为-C（O） - ; RB优选为异丁基; -RA = - （T）m-（D）m -R 1，其中T优选为氧或碳，D优选为单不饱和C 3-4烯基为更优选的; 并且X优选为α-酮酯或α-酮酰胺或醛。