RECOMBINANT C140 RECEPTOR, ITS AGONISTS AND ANTAGONISTS, AND NUCLEIC ACIDS ENCODING THE RECEPTOR
    88.
    发明申请
    RECOMBINANT C140 RECEPTOR, ITS AGONISTS AND ANTAGONISTS, AND NUCLEIC ACIDS ENCODING THE RECEPTOR 审中-公开
    重组C140受体,其激素和拮抗剂以及编码受体的核酸

    公开(公告)号:WO1996023225A1

    公开(公告)日:1996-08-01

    申请号:PCT/US1996001179

    申请日:1996-01-25

    CPC classification number: C07K14/723 A61K38/00 A61K48/00

    Abstract: Nucleic acid molecules encoding the C140 cell surface receptor have been cloned and sequenced. The availability of C140 receptor DNA permits the recombinant production of the C140 receptor which can be produced on the surface of a cell, including an oocyte. The nucleic acid molecules are useful in an assay for detecting a substance which affects C140 receptor activity, either receptor agonists or antagonists. Further, the elucidation of the structure of the C140 receptor permits the design of agonist and antagonist compounds which are useful in such assays. The availability of the C140 receptor also permits production of antibodies specifically immunoreactive with one or more antigenic epitopes of the C140 receptor.

    Abstract translation: 编码C140细胞表面受体的核酸分子已被克隆并测序。 C140受体DNA的可用性允许重组产生可在细胞表面(包括卵母细胞)上产生的C140受体。 核酸分子可用于检测影响C140受体活性的物质,即受体激动剂或拮抗剂。 此外,阐明C140受体的结构允许设计可用于此类测定中的激动剂和拮抗剂化合物。 C140受体的可用性还允许产生与C140受体的一个或多个抗原表位特异性免疫反应的抗体。

    METHOD AND COMPOSITIONS FOR INHIBITING PROTEIN KINASES
    89.
    发明申请
    METHOD AND COMPOSITIONS FOR INHIBITING PROTEIN KINASES 审中-公开
    抑制蛋白激酶的方法和组合物

    公开(公告)号:WO9613259A2

    公开(公告)日:1996-05-09

    申请号:PCT/US9513882

    申请日:1995-10-26

    CPC classification number: A61K31/366 A61K31/365

    Abstract: A method for selectively inhibiting a kinase is disclosed, which comprises contacting a composition containing a kinase with a molecule of formula (I) wherein R1 is H, lower alkyl, or lower alkanoyl; R2 is H, lower alkyl, or lower alkanoyl; R3 and R4 together represent a cis double bond or -O- or each of R3 and R4 independently represents H or OR; R5 is =O, =S, or -H, -OR; R6 and R7 together represent a double bond or -O- or each of R6 and R7 independently represents H or OR; R8 and R9 together represent a double bond or -O- or each of R8 and R9 independently represents H or OR; and each R independently represents H, lower alkyl, or lower alkanoyl.

    Abstract translation: 公开了选择性抑制激酶的方法,其包括将含有激酶的组合物与式(I)分子(其中R 1为H,低级烷基或低级烷酰基)接触; R2是H,低级烷基或低级烷酰基; R3和R4一起表示顺式双键或-O-或R 3和R 4各自独立地表示H或OR; R5为= O,= S或-H,-OR; R6和R7一起表示双键或-O-或R6和R7各自独立地表示H或OR; R8和R9一起表示双键或-O-或R8或R9各自独立地表示H或OR; 并且每个R独立地表示H,低级烷基或低级烷酰基。

    GLYCOSYLATION-MEDIATED INHIBITION OF FACTOR X
    90.
    发明申请
    GLYCOSYLATION-MEDIATED INHIBITION OF FACTOR X 审中-公开
    糖基化介导的因子X的抑制

    公开(公告)号:WO1993018782A1

    公开(公告)日:1993-09-30

    申请号:PCT/US1993002203

    申请日:1993-03-11

    Abstract: Reagents that specifically bind a carbohydrate target wherein sialic acid is linked at the nonreducing terminus of a glycoside to a galactose or galactosamine residue through an alpha 2-6 linkage are able to inhibit the conversion of human Factor X to human Factor Xa. These reagents (SA/Gal/GalNAc binding reagents) as well as other strategies for inhibiting the conversion of Factor X to Factor Xa are useful in treating thrombosis, inflammation and other conditions associated with excess thrombin activity.

    Abstract translation: 特异性结合碳水化合物靶标的试剂能够抑制人因子X向人因子Xa的转化,其中唾液酸在糖苷的非还原性末端通过α2-6键连接到半乳糖或半乳糖胺残基。 这些试剂(SA / Gal / GalNAc结合试剂)以及抑制因子X转化成因子Xa的其它策略可用于治疗血栓形成,炎症和与过量凝血酶活性相关的其它病症。

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