PLATELET GLYCOPROTEIN V GENE AND USES
    21.
    发明申请
    PLATELET GLYCOPROTEIN V GENE AND USES 审中-公开
    PLATELET GLYCOPROTEIN V基因和用途

    公开(公告)号:WO1995002054A2

    公开(公告)日:1995-01-19

    申请号:PCT/US1994007644

    申请日:1994-07-07

    CPC classification number: C07K14/705 A61K38/00

    Abstract: This invention relates to the glycoprotein v gene. Specifically, this invention discloses the sequence and structure of the glycoprotein v gene and the amino acid sequence of the glycoprotein v polypeptide. In addition, the evolutionary relationship of the glycoprotein v gene with other glycoproteins is described and several uses of the isolated glycoprotein v gene are shown.

    Abstract translation: 本发明涉及糖蛋白v基因。 具体地,本发明公开了糖蛋白v基因的序列和结构以及糖蛋白v多肽的氨基酸序列。 此外,描述了糖蛋白v基因与其他糖蛋白的进化关系,并显示了分离的糖蛋白v基因的几种用途。

    MODULATION OF INTERACTIONS BETWEEN MYOSIN AND INTEGRINS
    24.
    发明申请
    MODULATION OF INTERACTIONS BETWEEN MYOSIN AND INTEGRINS 审中-公开
    MYOSIN和INTEGRINS之间相互作用的调节

    公开(公告)号:WO1998022500A2

    公开(公告)日:1998-05-28

    申请号:PCT/US1997022422

    申请日:1997-11-21

    CPC classification number: C07K14/70546 A61K38/00 C07K14/70557

    Abstract: The present invention describes a direct interaction between myosin and the cytoplasmic domain of membrane proteins, particularly the phosphorylated cytoplasmic domains of the beta -subunit of integrins. The invention provides methods of identifying agents which block integrin binding to myosin, methods of using agents which block integrin binding to myosin to modulate biological and pathological processes, and provides agents that block integrin mediated binding to myosin and thereby modulate related cellular or cellular component movement.

    Abstract translation: 本发明描述了肌球蛋白和膜蛋白的细胞质结构域之间的直接相互作用,特别是整联蛋白β亚单位的磷酸化胞质结构域。 本发明提供鉴定阻断整合素与肌球蛋白结合的试剂的方法,使用阻断整合素结合肌球蛋白以调节生物学和病理学过程的试剂的方法,以及提供阻断整合素介导的结合肌球蛋白从而调节相关细胞或细胞成分运动的试剂 。

    PHARMACEUTICAL PYRAZOLE COMPOSITIONS USEFUL AS INHIBITORS OF PROTEIN KINASES
    26.
    发明申请
    PHARMACEUTICAL PYRAZOLE COMPOSITIONS USEFUL AS INHIBITORS OF PROTEIN KINASES 审中-公开
    用作蛋白激酶抑制剂的药用吡唑组合物

    公开(公告)号:WO1996014843A2

    公开(公告)日:1996-05-23

    申请号:PCT/US1995014723

    申请日:1995-11-09

    CPC classification number: A61K31/455 A61K31/415 A61K31/4155 A61K31/4439

    Abstract: A method for selectively inhibiting a kinase is disclosed, which comprises contacting a composition containing a kinase with a compound of formula (I), wherein: R1 is lower alkyl, lower hydrocarbyl, aryl lower alkyl, heteroaryl lower alkyl, 5- or 6-membered heterocyclic aromatic, polyaromatic, polyaromatic carbonyl, polyheteroaromatic or polyheteroaromatic carbonyl; R2 is lower alkyl, lower hydrocarbyl, aryl lower alkyl, heteroaryl lower alkyl, 5- or 6-membered heterocyclic aromatic, lower hydrocarboyl, 5- or 6-membered heterocyclic aromatic carbonyl, polyaromatic or polyheteroaromatic; R3 is H or lower alkyl; R5 is H, lower alkyl, lower hydrocarbyl, aryl lower alkyl, heteroaryl lower alkyl, 5- or 6-membered heterocyclic aromatic, halogen, or cyano; and R6 is H or lower hydrocarboyl.

    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)化合物接触,其中:R 1是低级烷基,低级烃基,芳基低级烷基,杂芳基低级烷基,5-或6- 多芳基,多芳基羰基,多杂芳基或多杂芳基羰基; R 2是低级烷基,低级烃基,芳基低级烷基,杂芳基低级烷基,5-或6-元杂环芳族,低级烃基,5-或6-元杂环芳族羰基,多芳族或多杂芳族; R3是H或低级烷基; R5是H,低级烷基,低级烃基,芳基低级烷基,杂芳基低级烷基,5-或6-元杂环芳族,卤素或氰基; R6为H或低级烃基。

    PROCESS FOR PRODUCTION OF INHIBITED FORMS OF ACTIVATED BLOOD FACTORS
    27.
    发明申请
    PROCESS FOR PRODUCTION OF INHIBITED FORMS OF ACTIVATED BLOOD FACTORS 审中-公开
    生产激活血液因子抑制形式的方法

    公开(公告)号:WO1996013274A1

    公开(公告)日:1996-05-09

    申请号:PCT/US1995013940

    申请日:1995-10-27

    CPC classification number: C12N9/6432 C07K14/75 C12Y304/21006 Y10S530/829

    Abstract: A process, as shown in the figure, for producing a highly purified preparation of an inhibited form of an activated blood factor entails providing a partially purified preparation containing the blood factor of interest, treating the partially purified preparation to convert the blood factor to an inhibited activated form in a single step, and then purifiying the resulting inhibited activated blood factor.

    Abstract translation: 如图所示,用于生产抑制形式的活化血液因子的高度纯化的制剂的方法需要提供含有目标血液因子的部分纯化的制剂,处理部分纯化的制剂以将血液因子转化为抑制 活化形式,然后净化所得的抑制的活化血液因子。

    RECEPTOR FUNCTION ASSAYS
    29.
    发明申请
    RECEPTOR FUNCTION ASSAYS 审中-公开
    受体功能测定

    公开(公告)号:WO1995004136A1

    公开(公告)日:1995-02-09

    申请号:PCT/US1994008571

    申请日:1994-07-29

    CPC classification number: G01N33/5008 G01N2333/9121

    Abstract: Methods are provided for assaying the function (e.g., activation) of signal-transducing receptors on cells. The methods are useful for identifying compounds that are agonists or antagonists of receptor function. The assays utilize a two-antibody sandwich assay employing an immobilized first antibody that specifically binds and captures the receptor of interest along with any tightly associated proteins or polypeptides and a second antibody directed against (i) an epitope of the receptor that is characteristic of the activated but not the unactivated state, (ii) an epitope of a protein or molecule characteristically bound to activated receptor but not to unactivated receptor, or (iii) an epitope of the receptor that is characteristic of the unactivated but not the activated state. In one embodiment, the level of binding of the second antibody is determined and correlated with the presence of activated receptor, and thus with activation in response to the treatment received by the cells. The methods provided by the invention will find particular use for detecting activation of tyrosine kinase growth factor receptors.

    Abstract translation: 提供了用于测定细胞上信号转导受体的功能(例如激活)的方法。 该方法可用于鉴定作为受体功能的激动剂或拮抗剂的化合物。 该测定法利用采用固定化的第一抗体的双抗体夹心测定法,其特异性结合并捕获感兴趣的受体以及任何紧密相关的蛋白质或多肽,以及针对(i)受体表位的第二抗体,其特征在于 活化但不是未活化状态,(ii)特征性结合活化受体但不结合未活化受体的蛋白质或分子的表位,或(iii)受体的表位,其是未活化但不是活化状态的特征。 在一个实施方案中,确定第二抗体的结合水平并与活化受体的存在相关,并因此响应于由细胞接受的治疗而激活。 本发明提供的方法将特别用于检测酪氨酸激酶生长因子受体的活化。

    RECOMBINANT THROMBIN RECEPTOR AND RELATED PHARMACEUTICALS
    30.
    发明申请
    RECOMBINANT THROMBIN RECEPTOR AND RELATED PHARMACEUTICALS 审中-公开
    重组血红蛋白受体和相关药物

    公开(公告)号:WO1992014750A1

    公开(公告)日:1992-09-03

    申请号:PCT/US1992001312

    申请日:1992-02-19

    Abstract: The DNA encoding the cell surface receptor for thrombin has been cloned and sequenced. The availability of this DNA permits the recombinant production of thrombin receptor which can be produced at cell surfaces and is useful in assay systems both for the detection of thrombin and for the evaluation of candidate thrombin agonists and antagonists. Further, the elucidation of the structure of the thrombin receptor permits the design of agonist and antagonist compounds which are useful diagnostically and therapeutically. The availability of the thrombin receptor also permits production of antibodies specifically immunoreactive with the receptor per se or with specific regions thereof which are also useful diagnostically or therapeutically.

    Abstract translation: 编码凝血酶细胞表面受体的DNA已被克隆并测序。 该DNA的可用性允许重组产生可在细胞表面产生的凝血酶受体,并且可用于检测凝血酶和用于评价候选凝血酶激动剂和拮抗剂的测定系统。 此外,阐明凝血酶受体的结构允许设计在诊断和治疗上有用的激动剂和拮抗剂化合物。 凝血酶受体的可用性还允许产生与受体本身或其特异性区域特异性免疫反应的抗体,其在诊断或治疗上也是有用的。

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