Nucleic acid modulators of glycoprotein VI
    2.
    发明授权
    Nucleic acid modulators of glycoprotein VI 有权
    糖蛋白VI的核酸调节剂

    公开(公告)号:US08318923B2

    公开(公告)日:2012-11-27

    申请号:US12793572

    申请日:2010-06-03

    IPC分类号: C07H21/04

    摘要: The present invention relates, in general, to a pharmacologic system to modulate the biology of platelets based upon a nucleic acid ligand that can interact with and modulate the activity of platelet glycoprotein GPVI to regulate platelet function. These nucleic acid ligands are also actively reversible using a modulator that inhibits the activity of the nucleic acid ligand to neutralize this pharmacologic effect and thereby restore GPVI function, including collagen binding, platelet adhesion, collagen-induced platelet activation, and collagen-induced platelet aggregation. The invention further relates to compositions comprising the nucleic acid ligand, the ligand and a modulator, methods to generate the nucleic acid ligand and its modulator, as well as methods of using these agents and compositions in medical therapeutic and diagnostic procedures.

    摘要翻译: 本发明一般涉及基于可与血小板糖蛋白GPVI相互作用并调节血小板糖蛋白GPVI的活性以调节血小板功能的核酸配体调节血小板生物学的药理学系统。 这些核酸配体也可以使用抑制核酸配体的活性来中和这种药理作用并由此恢复GPVI功能的调节剂,包括胶原结合,血小板粘附,胶原诱导的血小板活化和胶原诱导的血小板聚集 。 本发明还涉及包含核酸配体,配体和调节剂的组合物,产生核酸配体及其调节剂的方法,以及在医学治疗和诊断程序中使用这些试剂和组合物的方法。

    Administration of the REG1 anticoagulation system
    3.
    发明申请
    Administration of the REG1 anticoagulation system 审中-公开
    管理REG1抗凝系统

    公开(公告)号:US20090048193A1

    公开(公告)日:2009-02-19

    申请号:US11805950

    申请日:2007-05-25

    IPC分类号: A61K31/7088

    CPC分类号: A61K49/00 A61K31/00

    摘要: An improved method of administration of an aptamer and antidote system to regulate blood coagulation in a host is provided based on weight adjusted or body mass index-adjusted dosing of the components of the system to provide a desired pharmacodynamic response. In addition, a method of reversing activity of the aptamer to a desired extent is provided where an antidote dose is based solely on its relationship to the aptamer dose.

    摘要翻译: 基于体重调节或体重指数调整的系统组分的给药提供改善的适配体和解毒剂系统的调节方法以调节宿主中的血液凝固,以提供期望的药效学响应。 此外,提供将适配体的活性逆转到所需程度的方法,其中解毒剂剂量仅基于其与适体剂量的关系。

    Focused libraries, functional profiling, laser SELEX, and DESELEX
    4.
    发明授权
    Focused libraries, functional profiling, laser SELEX, and DESELEX 有权
    专注图书馆,功能剖析,激光SELEX和DESELEX

    公开(公告)号:US08367627B2

    公开(公告)日:2013-02-05

    申请号:US11992125

    申请日:2006-09-15

    IPC分类号: C07H21/02

    摘要: Focused aptamer libraries are constructed in accordance with a proteome (i.e., complex mixture of native biomolecules). The libraries may be screened to identify one or more candidate aptamers with desired biological activities other than specific binding to a target. Aptamers which are selected or derivatives thereof may be used for those specific activities in biological systems. Any combination of deconvoluting a focused library (functional profiling), increasing frequencies of particular aptamers in a focused library (Laser SELEX), and decreasing frequencies of particular aptamers in a focused library (DeSELEX) may be performed prior to assaying biological activity.

    摘要翻译: 根据蛋白质组(即天然生物分子的复杂混合物)构建聚焦的适体文库。 可以筛选文库以鉴定具有除特异性结合靶标以外的所需生物活性的一种或多种候选适体。 选择的适体或其衍生物可用于生物系统中的那些特定活性。 在分析生物活性之前,可以进行解卷积聚焦库(功能分析),聚焦库(Laser SELEX)中特定适体的频率增加以及聚焦文库(DeSELEX)中特定适体的频率降低的任何组合。

    MODULATORS OF PHARMACOLOGICAL AGENTS
    6.
    发明申请
    MODULATORS OF PHARMACOLOGICAL AGENTS 有权
    药物代谢调节剂

    公开(公告)号:US20100249217A1

    公开(公告)日:2010-09-30

    申请号:US12637467

    申请日:2009-12-14

    IPC分类号: A61K31/7052 A61P7/00

    摘要: The biological activity of nucleic acid ligand is regulated (i.e. enhanced or inhibited) in vivo to produce a desired biological effect. This is accomplished through the administration of a modulator, or regulator, that changes the binding of the nucleic acid ligand for its target or that degrades or otherwise cleaves, metabolizes or breaks down the nucleic acid ligand while the ligand is still exerting its effect. Modulators of the present invention can be administered in real time as needed based on various factors, including the progress of the patient, as well as the physician's discretion in how to achieve optimal therapy. Thus, this invention provides for the first time a regulatable therapeutic regime in the course of nucleic acid ligand therapy.

    摘要翻译: 核酸配体的生物活性在体内被调节(即增强或抑制)以产生所需的生物效应。 这通过施用调节剂或调节剂来实现,该调节剂或调节剂改变核酸配体对其靶的结合,或者在配体仍然发挥作用的同时降解或以其它方式切割,代谢或分解核酸配体。 本发明的调节剂可以根据各种因素,包括患者的进展以及医师在如何达到最佳治疗方面的酌处权,根据需要实时施用。 因此,本发明在核酸配体治疗过程中首次提供可调节的治疗方案。