公开(公告)号：US20100298200A1

公开(公告)日：2010-11-25

申请号：US12454765

申请日：2009-05-22

申请人： Dakai Liu ,  Xiaofeng Li ,  Richard Jin ,  Yuaxin Liang ,  Wei Cheng ,  Riddhi Bhattacharyya ,  Guangrong Zhang

发明人： Dakai Liu ,  Xiaofeng Li ,  Richard Jin ,  Yuaxin Liang ,  Wei Cheng ,  Riddhi Bhattacharyya ,  Guangrong Zhang

IPC分类号： A61K38/02 ,  C07D265/38 ,  C07C309/53 ,  C07C235/56 ,  C07D251/70 ,  C07C229/66 ,  A61K31/538 ,  A61K31/196 ,  A61K31/185 ,  A61K31/277 ,  A61K31/53 ,  A61K31/245 ,  A61K31/366 ,  A61K31/12 ,  A61K31/165 ,  A61K31/167 ,  A61K31/505 ,  A61K31/122 ,  A61K31/235 ,  A61K31/05 ,  A61K31/365 ,  A61K31/343 ,  A61P31/12 ,  A61P25/00 ,  A61P19/00 ,  A61P35/00 ,  A61P3/08 ,  A61P3/06 ,  G01N33/00 ,  C12Q1/02 ,  C12Q1/68 ,  G01N33/53 ,  G01N33/542 ,  C40B30/04 ,  C40B30/02 ,  C12N5/10 ,  C12Q1/66

CPC分类号： G01N33/6845 ,  A61K31/536 ,  A61K31/538 ,  C07D265/28 ,  C07D265/34 ,  C07D265/38 ,  C40B30/02 ,  G01N2800/36

摘要： The present invention relates to the field of therapeutic methods to screen for compounds on the basis of their ability to influence Wnt activity. The screening process is applied to both a physical library of a series of compounds and a virtual library of compounds that affect Wnt activity. In one aspect, the virtual screening process could be carried out where a permutational library of small peptides is substituted for the small organic molecules. The inventive methods may be used to empirically test for effects on Wnt activity and may also be applied to any pair of proteins involved in protein-protein interactions.

摘要翻译： 本发明涉及根据其影响Wnt活性的能力筛选化合物的治疗方法领域。 筛选过程适用于一系列化合物的物理文库和影响Wnt活性的化合物的虚拟文库。 在一个方面，虚拟筛选过程可以在小肽的置换文库替代小有机分子的地方进行。 本发明的方法可用于经验性地测试对Wnt活性的影响，并且还可以应用于涉及蛋白质 - 蛋白质相互作用的任何一对蛋白质。

公开(公告)号：US09052324B2

公开(公告)日：2015-06-09

申请号：US12454765

申请日：2009-05-22

申请人： Dakai Liu ,  Xiaofeng Li ,  Richard Jin ,  Yuaxin Liang ,  Wei Cheng ,  Riddhi Bhattacharyya ,  Guangrong Zhang

发明人： Dakai Liu ,  Xiaofeng Li ,  Richard Jin ,  Yuaxin Liang ,  Wei Cheng ,  Riddhi Bhattacharyya ,  Guangrong Zhang

IPC分类号： A61K31/538 ,  G01N33/68 ,  C40B30/02 ,  C07D265/28 ,  C07D265/38 ,  C07D265/34 ,  A61K31/536

CPC分类号： G01N33/6845 ,  A61K31/536 ,  A61K31/538 ,  C07D265/28 ,  C07D265/34 ,  C07D265/38 ,  C40B30/02 ,  G01N2800/36

摘要： The present invention relates to the field of therapeutic methods to screen for compounds on the basis of their ability to influence Wnt activity. The screening process is applied to both a physical library of a series of compounds and a virtual library of compounds that affect Wnt activity. In one aspect, the virtual screening process could be carried out where a permutational library of small peptides is substituted for the small organic molecules. The inventive methods may be used to empirically test for effects on Wnt activity and may also be applied to any pair of proteins involved in protein-protein interactions.

摘要翻译： 本发明涉及根据其影响Wnt活性的能力筛选化合物的治疗方法领域。 筛选过程适用于一系列化合物的物理文库和影响Wnt活性的化合物的虚拟文库。 在一个方面，虚拟筛选过程可以在小肽的置换文库替代小有机分子的地方进行。 本发明的方法可用于经验性地测试对Wnt活性的影响，并且还可以应用于涉及蛋白质 - 蛋白质相互作用的任何一对蛋白质。

公开(公告)号：US20120322717A9

公开(公告)日：2012-12-20

申请号：US12454765

申请日：2009-05-22

申请人： Dakai Liu ,  Xiaofeng Li ,  Richard Jin ,  Yuaxin Liang ,  Wei Cheng ,  Riddhi Bhattacharyya ,  Guangrong Zhang

发明人： Dakai Liu ,  Xiaofeng Li ,  Richard Jin ,  Yuaxin Liang ,  Wei Cheng ,  Riddhi Bhattacharyya ,  Guangrong Zhang

IPC分类号： A61K38/02 ,  C07C309/53 ,  C07C235/56 ,  C07D251/70 ,  C07C229/66 ,  A61K31/538 ,  A61K31/196 ,  A61K31/185 ,  A61K31/277 ,  A61K31/53 ,  A61K31/245 ,  A61K31/366 ,  A61K31/12 ,  A61K31/165 ,  A61K31/167 ,  A61K31/505 ,  A61K31/122 ,  A61K31/235 ,  A61K31/05 ,  A61K31/365 ,  A61K31/343 ,  A61P31/12 ,  A61P25/00 ,  A61P19/00 ,  A61P35/00 ,  A61P3/08 ,  A61P3/06 ,  G01N33/00 ,  C12Q1/02 ,  C12Q1/68 ,  G01N33/53 ,  G01N33/542 ,  C40B30/04 ,  C40B30/02 ,  C12N5/10 ,  C12Q1/66 ,  C07D265/38

CPC分类号： G01N33/6845 ,  A61K31/536 ,  A61K31/538 ,  C07D265/28 ,  C07D265/34 ,  C07D265/38 ,  C40B30/02 ,  G01N2800/36

摘要： The present invention relates to the field of therapeutic methods to screen for compounds on the basis of their ability to influence Wnt activity. The screening process is applied to both a physical library of a series of compounds and a virtual library of compounds that affect Wnt activity. In one aspect, the virtual screening process could be carried out where a permutational library of small peptides is substituted for the small organic molecules. The inventive methods may be used to empirically test for effects on Wnt activity and may also be applied to any pair of proteins involved in protein-protein interactions.

摘要翻译： 本发明涉及根据其影响Wnt活性的能力筛选化合物的治疗方法领域。 筛选过程适用于一系列化合物的物理文库和影响Wnt活性的化合物的虚拟文库。 一方面，虚拟筛选过程可以在小肽的置换文库替代小有机分子的地方进行。 本发明的方法可用于经验性地测试对Wnt活性的影响，并且还可以应用于涉及蛋白质 - 蛋白质相互作用的任何一对蛋白质。

公开(公告)号：US20110105606A1

公开(公告)日：2011-05-05

申请号：US12221863

申请日：2008-08-07

申请人： Elazar Rabbani ,  Xiaofeng Li ,  Dakai Liu ,  Yazhou Zhang ,  Richard Jin ,  Riddhi Bhattacharyya ,  Wei Cheng ,  James J. Donegan

发明人： Elazar Rabbani ,  Xiaofeng Li ,  Dakai Liu ,  Yazhou Zhang ,  Richard Jin ,  Riddhi Bhattacharyya ,  Wei Cheng ,  James J. Donegan

IPC分类号： A61K31/235 ,  A61P3/06 ,  A61P29/00 ,  A61P37/02 ,  A61P3/08 ,  A61P17/14 ,  A61K31/192 ,  A61K31/185 ,  C40B30/06 ,  C40B30/02 ,  C40B30/04

CPC分类号： A61K31/538 ,  A61K31/015 ,  A61K31/185 ,  A61K31/192 ,  A61K31/235 ,  A61K31/395 ,  A61K31/535 ,  A61K38/00 ,  G01N33/5011 ,  G01N33/5041 ,  G01N33/564 ,  G01N33/92 ,  G01N2333/705 ,  G01N2800/24

摘要： The present invention relates to the field of therapeutic methods, compositions and uses thereof, that affect, directly or indirectly, the behavior of LRP receptors. These compositions and methods result in the treatment of inflammatory, immunological and metabolic conditions. More particularly, the methods and compositions of the invention are directed to the identification of small molecules, drugs and/or pharmacological agents that affect the Wnt pathway by affecting normal complex formation among various signaling receptors, the LRP5 and LRP6 receptor, and related ligands.

摘要翻译： 本发明涉及直接或间接影响LRP受体的行为的治疗方法，组合物和用途领域。 这些组合物和方法导致治疗炎症，免疫和代谢疾病。 更具体地，本发明的方法和组合物涉及通过影响各种信号传导受体（LRP5和LRP6受体）和相关配体之间的正常复合物形成来鉴定影响Wnt途径的小分子，药物和/或药理学试剂。

公开(公告)号：US09046537B2

公开(公告)日：2015-06-02

申请号：US12221863

申请日：2008-08-07

申请人： Elazar Rabbani ,  Xiaofeng Li ,  Dakai Liu ,  Yazhou Zhang ,  Richard Jin ,  Riddhi Bhattacharyya ,  Wei Cheng ,  James J. Donegan

发明人： Elazar Rabbani ,  Xiaofeng Li ,  Dakai Liu ,  Yazhou Zhang ,  Richard Jin ,  Riddhi Bhattacharyya ,  Wei Cheng ,  James J. Donegan

IPC分类号： A01N43/00 ,  A61K31/33 ,  A01N61/00 ,  A61K31/00 ,  A61K31/535 ,  A01N43/02 ,  A61K31/335 ,  A01N43/16 ,  A61K31/35 ,  G01N33/92 ,  A61K31/015 ,  A61K31/395 ,  G01N33/50 ,  G01N33/564 ,  A61K38/00

CPC分类号： A61K31/538 ,  A61K31/015 ,  A61K31/185 ,  A61K31/192 ,  A61K31/235 ,  A61K31/395 ,  A61K31/535 ,  A61K38/00 ,  G01N33/5011 ,  G01N33/5041 ,  G01N33/564 ,  G01N33/92 ,  G01N2333/705 ,  G01N2800/24

摘要： The present invention relates to the field of therapeutic methods, compositions and uses thereof, that affect, directly or indirectly, the behavior of LRP receptors. These compositions and methods result in the treatment of inflammatory, immunological and metabolic conditions. More particularly, the methods and compositions of the invention are directed to the identification of small molecules, drugs and/or pharmacological agents that affect the Wnt pathway by affecting normal complex formation among various signaling receptors, the LRP5 and LRP6 receptor, and related ligands.

摘要翻译： 本发明涉及直接或间接影响LRP受体的行为的治疗方法，组合物和用途领域。 这些组合物和方法导致治疗炎症，免疫和代谢疾病。 更具体地，本发明的方法和组合物涉及通过影响各种信号传导受体（LRP5和LRP6受体）和相关配体之间的正常复合物形成来鉴定影响Wnt途径的小分子，药物和/或药理学试剂。

公开(公告)号：US20100041599A1

公开(公告)日：2010-02-18

申请号：US12228757

申请日：2008-08-15

申请人： Dakai Liu ,  Richard Jin ,  Xiaofeng Li ,  Yazhou Zhang ,  Wei Cheng ,  Riddhi Bhattacharyya

发明人： Dakai Liu ,  Richard Jin ,  Xiaofeng Li ,  Yazhou Zhang ,  Wei Cheng ,  Riddhi Bhattacharyya

IPC分类号： A61K38/22 ,  C12Q1/68 ,  A61P19/08

CPC分类号： A61K31/538 ,  G01N33/5041 ,  G01N33/6803 ,  G01N2333/51

摘要： The present invention identifies compounds that disrupt the interaction between anthrax proteins and LRP5/6 receptors, resulting in a reduction in anthrax toxicity. The compounds act to disrupt the intracellular transport of toxin complexes into a target cell. The present invention also provides methods for testing the effect of compounds on Wnt activity, through the use of in vitro experiments involving cells that have in at least one gene mutation involved in the Wnt pathway.

摘要翻译： 本发明鉴定了破坏炭疽蛋白与LRP5 / 6受体之间相互作用的化合物，导致炭疽毒性降低。 这些化合物起着破坏细胞内毒素复合物进入靶细胞的作用。 本发明还提供了通过使用涉及在Wnt途径中涉及至少一个基因突变的细胞的体外实验来测试化合物对Wnt活性的影响的方法。

公开(公告)号：US20120184616A9

公开(公告)日：2012-07-19

申请号：US12221863

申请日：2008-08-07

申请人： Elazar Rabbani ,  Xiaofeng Li ,  Dakai Liu ,  Yazhou Zhang ,  Richard Jin ,  Riddhi Bhattacharyya ,  Wei Cheng ,  James J. Donegan

发明人： Elazar Rabbani ,  Xiaofeng Li ,  Dakai Liu ,  Yazhou Zhang ,  Richard Jin ,  Riddhi Bhattacharyya ,  Wei Cheng ,  James J. Donegan

IPC分类号： A61K31/235 ,  A61P29/00 ,  A61P37/02 ,  A61P3/08 ,  C40B30/04 ,  A61K31/192 ,  A61K31/185 ,  C40B30/06 ,  C40B30/02 ,  A61P3/06 ,  A61P17/14

CPC分类号： A61K31/538 ,  A61K31/015 ,  A61K31/185 ,  A61K31/192 ,  A61K31/235 ,  A61K31/395 ,  A61K31/535 ,  A61K38/00 ,  G01N33/5011 ,  G01N33/5041 ,  G01N33/564 ,  G01N33/92 ,  G01N2333/705 ,  G01N2800/24

摘要： The present invention relates to the field of therapeutic methods, compositions and uses thereof, that affect, directly or indirectly, the behavior of LRP receptors. These compositions and methods result in the treatment of inflammatory, immunological and metabolic conditions. More particularly, the methods and compositions of the invention are directed to the identification of small molecules, drugs and/or pharmacological agents that affect the Wnt pathway by affecting normal complex formation among various signaling receptors, the LRP5 and LRP6 receptor, and related ligands.

摘要翻译： 本发明涉及直接或间接影响LRP受体的行为的治疗方法，组合物和用途领域。 这些组合物和方法导致治疗炎症，免疫和代谢疾病。 更具体地，本发明的方法和组合物涉及通过影响各种信号传导受体（LRP5和LRP6受体）和相关配体之间的正常复合物形成来鉴定影响Wnt途径的小分子，药物和/或药理学试剂。

公开(公告)号：US10060910B2

公开(公告)日：2018-08-28

申请号：US13556304

申请日：2012-07-24

申请人： Jack Coleman ,  Maciej Szczepanik ,  Richard Jin

发明人： Jack Coleman ,  Maciej Szczepanik ,  Richard Jin

IPC分类号： C12Q1/68 ,  G01N33/543 ,  G01N33/58

CPC分类号： G01N33/54306 ,  C12Q1/68 ,  G01N33/58

摘要： Provided is a composition comprising an analyte bound to a polymer where the analyte is less than about 2000 MW and the polymer further comprises more than one signal or first member of a second binding pair. Also provided is an assay for an analyte comprising combining a sample suspected of containing the analyte with the above-described composition and a binding agent that binds to the analyte; and detecting the signal or the first member of the second binding pair that is bound to the binding agent. Additionally provided is a multisignal labeling reagent comprising a first polymer covalently bound to (a) a reactive group or a first member of a first binding pair, and (b) more than one digoxigenin molecule.

公开(公告)号：US09696298B2

公开(公告)日：2017-07-04

申请号：US13556425

申请日：2012-07-24

申请人： Jack Coleman ,  Maciej Szczepanik ,  Richard Jin

发明人： Jack Coleman ,  Maciej Szczepanik ,  Richard Jin

IPC分类号： G01N33/53 ,  G01N33/557 ,  G01N33/549 ,  C07H21/00 ,  C07H21/04 ,  C09B11/08 ,  C09B11/24 ,  C12Q1/68 ,  G01N33/58 ,  G01N33/82 ,  G01N33/94 ,  C07H19/04

CPC分类号： G01N33/53 ,  C07H21/00 ,  C07H21/04 ,  C09B11/08 ,  C09B11/24 ,  C12Q1/6818 ,  G01N33/581 ,  G01N33/82 ,  G01N33/94

摘要： Provided is a composition comprising an analyte bound covalently or through a first binding pair to a polymer. In this composition, the analyte is less than about 2000 MW; the polymer further comprises more than one signal or first member of a second binding pair; and the analyte is not a member of the first binding pair or the second binding pair. Also provided is an assay for an analyte. The assay comprises: combining a sample suspected of containing the analyte with the above-described composition and a binding agent that binds to the analyte; and detecting the signal or the first member of the second binding pair that is bound to the binding agent. Additionally provided is a multisignal labeling reagent comprising a first polymer covalently bound to (a) a reactive group or a first member of a first binding pair, and (b) more than one digoxigenin molecule.