利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

83 条记录 (耗时 0.033 秒)

    Single-molecule platform for drug discovery: methods and apparatuses for drug discovery, including discovery of anticancer and antiviral agents
    1.
    发明授权
    Single-molecule platform for drug discovery: methods and apparatuses for drug discovery, including discovery of anticancer and antiviral agents 有权

    公开(公告)号：US09862984B2

    公开(公告)日：2018-01-09

    申请号：US11790071

    申请日：2007-04-23

    申请人： Anita Goel

    发明人： Anita Goel

    IPC分类号： C12Q1/00 ,  C12Q1/48

    CPC分类号： C12Q1/00 ,  C12Q1/48 ,  G01N2333/16 ,  G01N2333/91245 ,  G01N2500/02

    摘要： The present application discloses methods and apparatuses for single molecule drug screening, discovery and validation. These methods and apparatuses allow a user to detect rapidly, using observation of single molecules, whether and how a drug candidate interferes with a target enzyme involved in a particular disease pathway. The methods and apparatuses described herein utilize single molecule manipulation and detection technologies (e.g., optical or magnetic tweezers) to directly detect whether the characteristic dynamics, or “mechanical signature,” of the target enzyme-substrate interaction are substantially altered or modulated by a drug candidate. Furthermore, the methods and apparatuses are useful for analyzing the modulation of the mechanical signature in order to identify potential interference mechanisms of a drug candidate. In one aspect of the invention, the methods and apparatuses disclosed herein relate to monitoring the real-time dynamic mechanical signatures of individual polymerase molecules (e.g. DNA polymerases, RNA polymerases, and reverse transcriptases) along a polynucleotide substrate in the presence of drug candidates that either inhibit or otherwise modulate the polymerization process. Identification and analysis of such drug candidates is critical for anti-viral, anti-cancer, and antibiotic drug development.

    Method for Identifying a Compound That Modulates Telomerase Activity
    5.
    发明申请
    Method for Identifying a Compound That Modulates Telomerase Activity 有权
    鉴定调节端粒酶活性的化合物的方法

    公开(公告)号：US20100216150A1

    公开(公告)日：2010-08-26

    申请号：US12701801

    申请日：2010-02-08

    申请人： Emmanuel Skordalakes

    发明人： Emmanuel Skordalakes

    IPC分类号： C12Q1/68 ,  G01N33/573

    CPC分类号： C12Q1/48 ,  G01N2333/91245

    摘要： The present invention embraces methods for identifying compounds that modulate the activity of telomerase. Compounds of the invention are identified by designing or screening for a compound which binds to at least one amino acid residue of the TRBD, “thumb,” “finger,” and/or “palm” domain; or FP-pocket, PT-pocket or Th-pocket of telomerase and testing the compound for its ability to modulate the activity of telomerase.

    摘要翻译： 本发明包括用于鉴定调节端粒酶活性的化合物的方法。 通过设计或筛选与TRBD，“拇指”，“手指”和/或“手掌”结构域的至少一个氨基酸残基结合的化合物来鉴定本发明化合物; 或FP-pocket，PT-pocket或Th-pocket端粒酶，并测试该化合物调节端粒酶活性的能力。

    Screening and selection methods for statin drug combinations
    7.
    发明授权
    Screening and selection methods for statin drug combinations 失效
    他汀类药物组合的筛选方法

    公开(公告)号：US07407772B2

    公开(公告)日：2008-08-05

    申请号：US10490462

    申请日：2002-09-20

    申请人： Thomayant Prueksaritanont

    发明人： Thomayant Prueksaritanont

    IPC分类号： C12Q1/48

    CPC分类号： C12Q1/48 ,  A61K31/19 ,  A61K31/366 ,  A61K31/40 ,  G01N2333/90245 ,  G01N2333/91245 ,  G01N2500/04 ,  A61K2300/00

    摘要： A method for screening statins in their open acid form to determine the susceptibility of each tested statin to metabolic glucuronidation is provided. Also provided is a method for determining if a non-statin pharmaceutical drug co-administered with a statin that is susceptible to metabolic glucuronidation in its open acid form, will inhibit the glucuronidation of the statin and thereby increase the risk of an adverse drug interaction.

    摘要翻译： 提供了以开放酸形式筛选他汀类药物以确定每种被测他汀类药物对代谢葡萄糖醛酸化的敏感性的方法。 还提供了一种用于确定与其开放酸形式易于代谢葡糖醛酸化的他汀类药物共同施用的非他汀类药物是否将抑制他汀类药物葡糖醛酸化，从而增加不良药物相互作用的风险的方法。

    IgY antibodies to human telomerase reverse transcriptase
    8.
    发明申请
    IgY antibodies to human telomerase reverse transcriptase 审中-公开
    人类端粒酶逆转录酶的IgY抗体

    公开(公告)号：US20080131442A1

    公开(公告)日：2008-06-05

    申请号：US11474452

    申请日：2006-06-26

    申请人： Yan Xiao

    发明人： Yan Xiao

    IPC分类号： A61K39/395 ,  G01N33/53 ,  C07K16/40

    CPC分类号： C07K16/02 ,  C07K16/40 ,  C07K2317/23 ,  G01N2333/91245 ,  G01N2333/9125

    摘要： IgY antibodies which specifically bind to human telomerase reverse transcriptase (hTERT) can be used to detect hTERT and thereby diagnose cancer. Preparations of the antibodies can be used to reduce hTERT reverse transcriptase activity in in vitro assays and can be used as in vivo therapeutics to treat cancer.

    摘要翻译： 特异性结合人端粒酶逆转录酶（hTERT）的IgY抗体可用于检测hTERT，从而诊断癌症。 抗体的制备可用于在体外测定中降低hTERT逆转录酶活性，并且可以用作体内治疗剂来治疗癌症。

    Test system for determining the activity of cyclo-nucleotide-dependent protein kinases and vasp phosphatases
    10.
    发明申请
    Test system for determining the activity of cyclo-nucleotide-dependent protein kinases and vasp phosphatases 审中-公开
    用于测定环核苷酸依赖性蛋白激酶和磷脂酶活性的测试系统

    公开(公告)号：US20030166005A1

    公开(公告)日：2003-09-04

    申请号：US10311093

    申请日：2003-04-01

    发明人： Peter Druckes ,  Thomas Jarchau ,  Ulrich Walter ,  Benjamin Bader

    IPC分类号： G01N033/53 ,  C12M001/34

    CPC分类号： C12Q1/485 ,  G01N2333/91245

    摘要： The invention relates to an HTS-appropriate test system for detecting the activity of cyclo-nucleotide-dependent protein kinases (cNPK) containing: a) at least one test compound; b) at least one appropriate cNPK substrate; c) at least one composition, which is to be incubated and which contains cNPK and ATP, optionally, phosphorylation reaction stoppers, and; d) an appropriate detection system for quantifying the phosphorylation of the cNPK substrate. The invention also relates to an HTS-appropriate test system for detecting the activity of VASP phosphatases containing: e) at least one test compound; f) at least one appropriate VASP phosphatase substrate; g) at least one composition, which is to be incubated and which contains VASP phosphatase, and; h) an appropriate detection system for quantifying the dephosphorylation of the VASP phosphatase substrate. The described test systems can be used for locating compounds, which modulate the activity of a cNPK or of a VASP phosphatase, from chemical or natural substance libraries.

    摘要翻译： 本发明涉及用于检测环核苷酸依赖性蛋白激酶（cNPK）的活性的HTS合适的测试系​​统，其包含：a）至少一种测试化合物; b）至少一种适当的cNPK底物; c）至少一种待孵育的组合物，其中含有cNPK和ATP，任选的磷酸化反应阻断剂;和 d）用于量化cNPK底物磷酸化的适当检测系统。 本发明还涉及用于检测VASP磷酸酶的活性的HTS合适的测试系​​统，其包含：e）至少一种测试化合物; f）至少一种合适的VASP磷酸酶底物; g）至少一种待孵育并且含有VASP磷酸酶的组合物，和 h）用于量化VASP磷酸酶底物去磷酸化的适当检测系统。 所描述的测试系统可用于从化学或天然物质文库中定位调节cNPK或VASP磷酸酶的活性的化合物。