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    TRANSGENIC MAMMALS EXPRESSING MUTANT GP IIIa
    5.
    发明公开
    TRANSGENIC MAMMALS EXPRESSING MUTANT GP IIIa 审中-公开
    转基因哺乳动物而言突变的GPIIIa表达

    公开(公告)号：EP1071751A1

    公开(公告)日：2001-01-31

    申请号：EP99918586.1

    申请日：1999-04-15

    申请人： COR THERAPEUTICS, INC.

    发明人： LAW, Deborah, Ann ,  PHILLIPS, David, R.

    IPC分类号： C12N5/10 ,  A01K67/027 ,  C07K14/705 ,  A61K49/00

    CPC分类号： C12N15/8509 ,  A01K67/0275 ,  A01K2217/072 ,  A01K2227/105 ,  A01K2267/03 ,  C07K14/70557 ,  C12N2800/30

    摘要： The present invention relates to mammals into which foreign DNA has been introduced or in which various modifications or substitutions have been made to an integrin β subunit, thereby generating transgenic or genetically-engineered non-human mammals. In particular, the present invention provides a transgenic mammal in which the endogenous GP IIIa gene has been replaced with an altered or mutant GP IIIa gene in which one or all of the phosphorylatable cytoplasmic tyrosine residues have been replaced with non-tyrosine residues such as phenylalanine. Since the platelets in the blood of the resultant transgenic mammals expressing the altered or mutant GP IIIa cannot undergo tyrosine phosphorylation to the extent that it occurs in wild-type mammals, these genetically-engineered animals provide a critical tool for assessing the importance of the phosphorylation reaction for platelet function. The invention is also useful for studying the effect of the mutant GP IIIa integrin subunit on biological processes other than platelet formation.

    THROMBIN RECEPTOR ANTAGONISTS
    7.
    发明授权
    THROMBIN RECEPTOR ANTAGONISTS 失效
    拮抗剂反对凝血酶

    公开(公告)号：EP0656008B1

    公开(公告)日：2000-03-15

    申请号：EP93917028.8

    申请日：1993-07-08

    申请人： COR THERAPEUTICS, INC.

    发明人： SCARBOROUGH, Robert M.

    IPC分类号： C07K5/06 ,  C07K5/10 ,  C07K7/06

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

    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 formula (I) in which R?1 and R3¿ are amide linkages, N-alkylamide linkages, or isosteric replacements of such linkages; R2 is either a neutral amino acid side chain or a hydrophobic radical; R4 is hydrophobic radical; R5 is CO, CH¿2? or SO; X is either of formula (II) in which R?6 and R7¿ are H, alkyl, cycloalkylalkyl, alkoxyalkyl, alkylthioalkyl or arylalkyl, and R8 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.