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    Recombinant C140 receptor, its agonists and antagonists, and nucleic acids encoding the receptor
    2.
    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，其激动剂和拮抗剂，以及编码受体的核酸

    公开(公告)号：US20030018184A1

    公开(公告)日：2003-01-23

    申请号：US10127691

    申请日：2002-04-23

    申请人： COR THERAPEUTICS, INC.

    发明人： Johan Sundelin ,  Robert M. Scarborough

    IPC分类号： C07K014/715 ,  C07H021/04 ,  C12P021/02 ,  C12N005/06

    CPC分类号： C07K7/06 ,  A61K38/00 ,  A61K48/00 ,  C07K7/08 ,  C07K14/705 ,  C07K14/723 ,  G01N2333/726 ,  G01N2500/00

    摘要： 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.

    摘要翻译： 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。

    Thrombin receptor antagonists
    5.
    发明授权
    Thrombin receptor antagonists 失效
    凝血酶受体拮抗剂

    公开(公告)号：US5866681A

    公开(公告)日：1999-02-02

    申请号：US407468

    申请日：1995-03-20

    申请人： Robert M. Scarborough

    发明人： Robert M. Scarborough

    IPC分类号： A61K38/00 ,  A61P7/02 ,  A61P9/08 ,  A61P9/10 ,  A61P29/00 ,  C07K5/062 ,  C07K5/065 ,  C07K5/083 ,  C07K5/087 ,  C07K5/103 ,  C07K5/107 ,  C07K7/02 ,  C07K7/06 ,  C07K7/08 ,  A61K38/04 ,  C07K5/00

    CPC分类号： C07K7/06 ,  C07K5/06078 ,  C07K5/1016 ,  C07K7/02 ,  A61K38/00

    摘要： Peptide derivatives serving as thrombin receptor antagonists are disclosed, which bear specificity for the cellular thrombin receptor without interfering with the catalytic activities of thrombin. The derivatives generally have the formula ##STR1## in which R.sup.1 and R.sup.3 are amide linkages, N-alkylamide linkages, or isosteric replacements of such linkages; R.sup.2 is either a neutral amino acid side chain or a hydrophobic radical; R.sup.4 is hydrophobic radical; R.sup.5 is CO, CH.sub.2 or SO; X is either of the formula: ##STR2## in which R.sup.6 and R.sup.7 are H, alkyl, cycloalkylalkyl, alkoxyalkyl, alkylthioalkyl or arylalkyl, and R.sup.8 is a hydrophobic radical, or a hydrophobic residue; Y is alkoxy, hydroxy, amino, alkylamino, dialkylamino, in which any of the alkyl groups may be substituted with a basic moiety; Z is an amino acid or peptide residue; and m is zero or one.

    摘要翻译： 公开了用作凝血酶受体拮抗剂的肽衍生物，其对细胞凝血酶受体具有特异性，而不干扰凝血酶的催化活性。 衍生物通常具有式（1）所示的烷基酰胺键或这种键的等位取代; R2是中性氨基酸侧链或疏水基团; R4是疏水基; R5是CO，CH2或SO; X是下式：其中R 6和R 7是H，烷基，环烷基烷基，烷氧基烷基，烷硫基烷基或芳基烷基，R 8是疏水基团或疏水残基; Y是烷氧基，羟基，氨基，烷基氨基，二烷基氨基，其中任何烷基可被碱部分取代; Z是氨基酸或肽残基; m为0或1。

    Platelet aggregation inhibitors
    8.
    发明授权
    Platelet aggregation inhibitors 失效
    血小板聚集抑制剂

    公开(公告)号：US5786333A

    公开(公告)日：1998-07-28

    申请号：US484414

    申请日：1995-06-07

    申请人： Robert M. Scarborough ,  David Lawrence Wolf ,  Israel F. Charo

    发明人： Robert M. Scarborough ,  David Lawrence Wolf ,  Israel F. Charo

    IPC分类号： A61K38/00 ,  A61K38/12 ,  A61K38/17 ,  A61K38/57 ,  C07K14/46 ,  C07K14/75 ,  C07K14/755 ,  C07K14/78 ,  C07K5/00 ,  C07K7/00

    CPC分类号： A61K38/12 ,  A61K38/1703 ,  A61K38/57 ,  C07K14/46 ,  C07K14/75 ,  C07K14/755 ,  C07K14/78

    摘要： An assay for screening snake venom for the presence or absence of platelet aggregation inhibitors (PAIs) based on specific receptor binding is described. Using this assay, the identification and characterization of PAIs in a wide range of snake venom samples was accomplished. The isolated and purified PAI from several of these active snake venoms is described and characterized. In addition, PAIs lacking the Arg-Gly-Asp (RGD) adhesion sequence but containing K*-(G/Sar)-D wherein K* is a modified lysyl residue of the formula R.sup.1.sub.2 N(CH.sub.2).sub.4 CHNHCO-- wherein each R.sup.1 is independently H, alkyl(1-6C) or at most one R.sup.1 is R.sup.2 --C.dbd.NR.sup.3 wherein R.sup.2 is H, alkyl(1-6C), phenyl or benzyl, or is NR.sup.4 .sub.2 in which each R.sup.4 is independently H or alkyl(1-6C) and R.sup.3 is H, alkyl(1-6C), phenyl or benzyl, or R.sup.2 --C.dbd.NR.sup.3 is a radical selected from the group consisting of: ##STR1## where m is an integer of 2-3, and each R.sup.5 is independently H or alkyl(1-6C); and wherein one or two (CH.sub.2) may be replaced by O or S provided said O or S is not adjacent to another heteroatom are prepared and shown to specifically inhibit the binding of fibrinogen or von Willebrand Factor to GP IIb-IIIa.

    摘要翻译： 描述了基于特异性受体结合筛选蛇毒用于存在或不存在血小板聚集抑制剂（PAI）的测定法。 使用该测定，完成了广泛的蛇毒样品中PAIs的鉴定和表征。 描述和表征了来自这些活性蛇毒中的几种的分离和纯化的PAI。 另外，缺乏Arg-Gly-Asp（RGD）粘附序列但含有K * - （G / Sar）-D的PAI，其中K *是式R 12 N（CH 2）4 CHNHCO-的修饰的赖氨酰残基，其中每个R 1独立地为H ，烷基（1-6C）或至多一个R1是R2-C = NR3，其中R2是H，（1-6C）烷基，苯基或苄基，或是NR42，其中每个R4独立地是H或烷基（1- 6C），R3是H，（1-6C）烷基，苯基或苄基，或R2-C = NR3是选自以下的基团：其中m是2-3的整数， 并且每个R 5独立地为H或烷基（1-6C）; 并且其中一个或两个（CH 2）可以被O或S替代，条件是所述O或S不与另一个杂原子相邻，并且显示出特异性抑制纤维蛋白原或血管性血友病因子与GP IIb-IIIa的结合。

    Platelet aggregation inhibitors
    10.
    发明授权
    Platelet aggregation inhibitors 失效
    血小板聚集抑制剂

    公开(公告)号：US5770564A

    公开(公告)日：1998-06-23

    申请号：US465178

    申请日：1995-06-05

    申请人： Robert M. Scarborough ,  David Lawrence Wolf ,  Israel F. Charo

    发明人： Robert M. Scarborough ,  David Lawrence Wolf ,  Israel F. Charo

    IPC分类号： A61K38/00 ,  A61K38/12 ,  A61K38/17 ,  A61K38/57 ,  C07K14/46 ,  C07K14/75 ,  C07K14/755 ,  C07K14/78 ,  A61K38/02 ,  C07K5/00 ,  C07K7/00

    CPC分类号： A61K38/12 ,  A61K38/1703 ,  A61K38/57 ,  C07K14/46 ,  C07K14/75 ,  C07K14/755 ,  C07K14/78

    摘要： An assay for screening snake venom for the presence or absence of platelet aggregation inhibitors (PAIs) based on specific receptor binding is described. Using this assay, the identification and characterization of PAIs in a wide range of snake venom samples was accomplished. The isolated and purified PAI from several of these active snake venoms is described and characterized. In addition, PAIs lacking the Arg-Gly-Asp (RGD) adhesion sequence but containing K*-(G/Sar)-D wherein K* a modified lysyl residue of the formula R.sup.1.sub.2 N(CH.sub.2).sub.4 CHNHCO-- wherein each R.sup.1 is independently H, alkyl(1-6 C) or at most one R.sup.1 is R.sup.2 --C.dbd.NR.sup.3 wherein R.sup.2 is H, alkyl(1-6 C), phenyl or benzyl, or is NR.sup.4.sub.2 in which each R.sup.4 is independently H or alkyl(1-6 C) and R.sup.3 is H, alkyl(1-6 C), phenyl or benzyl, or R.sup.2 --C.dbd.NR.sup.3 is a radical selected from the group consisting of: ##STR1## where m is an integer of 2-3, and each R.sup.5 is independently H or alkyl(1-6 C); and wherein one or two (CH.sub.2) may be replaced by O or S provided said O or S is not adjacent to another heteroatom are prepared and shown to specifically inhibit the binding of fibrinogen or von Willebrand Factor to GP IIb-IIIa.

    摘要翻译： 描述了基于特异性受体结合筛选蛇毒用于存在或不存在血小板聚集抑制剂（PAI）的测定法。 使用该测定，完成了广泛的蛇毒样品中PAIs的鉴定和表征。 描述和表征了来自这些活性蛇毒中的几种的分离和纯化的PAI。 此外，缺少Arg-Gly-Asp（RGD）粘附序列但含有K * - （G / Sar）-D的PAI，其中K *是式R 12 N（CH 2）4 CHNHCO-的修饰的赖氨酰残基，其中每个R 1独立地为H， 烷基（1-6C）或至多一个R1是R2-C = NR3，其中R2是H，烷基（1-6C），苯基或苄基，或是NR42，其中每个R4独立地是H或烷基（1- 6 C），R 3是H，烷基（1-6C），苯基或苄基，或者R 2 -C = NR 3是选自以下的基团：其中m是2-3的整数，以及 每个R 5独立地为H或烷基（1-6C）; 并且其中一个或两个（CH 2）可以被O或S替代，条件是所述O或S不与另一个杂原子相邻，并且显示出特异性抑制纤维蛋白原或血管性血友病因子与GP IIb-IIIa的结合。