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    COMPOUNDS THAT PARTICIPATE IN COOPERATIVE BINDING AND USES THEREOF
    4.
    发明申请
    COMPOUNDS THAT PARTICIPATE IN COOPERATIVE BINDING AND USES THEREOF 审中-公开
    参与合作结合的化合物及其用途

    公开(公告)号：WO2016112279A1

    公开(公告)日：2016-07-14

    申请号：PCT/US2016/012631

    申请日：2016-01-08

    申请人： WARP DRIVE BIO, INC.

    发明人： VERDINE, Gregory, Lawrence ,  NICHOLS, Matthew, Square ,  STILES, Dylan, Talbot ,  ANTHONY, Neville, John ,  BOWMAN, Brian, Roger ,  SOWA, Mathew, Edward ,  TOWNSON, Sharon, Ann

    IPC分类号： A61K38/12 ,  A61K47/48 ,  C07K7/64

    CPC分类号： A61K47/48346 ,  A61K38/00 ,  C07D405/06 ,  C07D498/18 ,  C07D498/22 ,  C07K7/56 ,  C07K7/64 ,  C07K7/645

    摘要： The invention features compounds (e.g., macrocyclic compounds) capable of modulating biological processes, for example through binding to a presenter protein (e.g., a member of the FKBP family, a member of the cyclophilin family, or PIN1) and a target protein (e.g., a eukaryotic target protein such as a mammalian target protein or a fungal target protein or a prokaryotic target protein such as a bacterial target protein). These compounds bind endogenous intracellular presenter proteins, such as the FKBPs or cyclophilins, and the resulting binary complexes selectively bind and modulate the activity of intracellular target proteins. Formation of a tripartite complex among the presenter protein, the compound, and the target protein is driven by both protein-compound and protein-protein interactions, and both are required for modulation of the targeted protein's activity. In some embodiments, the compounds of the invention "re-program" the binding of the presenter proteins to protein targets that either do not normally bind to the presenter protein (e.g., do not show detectable binding in mammalian cells absent the compound). In some embodiments, provided compounds "re-program" presenter protein binding to greatly enhance interaction with a particular target with which it may have some interaction absent the compound. Interactions achieved through such reprogramming result in an ability to modulate the activity of these new targets.

    摘要翻译： 本发明的特征在于能够调节生物学过程的化合物（例如大环化合物），例如通过与呈递蛋白（例如，FKBP家族的成员，亲环蛋白家族成员或 PIN1）和靶蛋白（例如，真核靶蛋白如哺乳动物靶蛋白或真菌靶蛋白或原核靶蛋白如细菌靶蛋白）。 这些化合物结合内源性细胞内呈递蛋白，如FKBPs或亲环蛋白，并且所得到的二元复合物选择性结合并调节细胞内靶蛋白的活性。 表达蛋白，化合物和靶蛋白之间的三重复合物的形成受到蛋白质 - 化合物和蛋白质 - 蛋白质相互作用的驱动，并且二者都是调节靶蛋白质活性所需的。 在一些实施方案中，本发明的化合物“重新编程” 表达蛋白与蛋白质靶标的结合，所述蛋白质靶标或者通常不与表达蛋白结合（例如，在不存在所述化合物的哺乳动物细胞中不显示可检测的结合）。 在一些实施方案中，提供的化合物“重新编程” 呈递者蛋白质结合以极大地增强与特定靶标的相互作用，与特定靶标可能具有一些缺乏该化合物的相互作用。 通过这种重新编程实现的相互作用导致调节这些新目标的活性的能力。

    COMPOUNDS THAT PARTICIPATE IN COOPERATIVE BINDING AND USES THEREOF
    8.
    发明申请
    COMPOUNDS THAT PARTICIPATE IN COOPERATIVE BINDING AND USES THEREOF 审中-公开
    参与合作结合的化合物及其用途

    公开(公告)号：WO2016112295A1

    公开(公告)日：2016-07-14

    申请号：PCT/US2016/012656

    申请日：2016-01-08

    申请人： WARP DRIVE BIO, INC.

    发明人： VERDINE, Gregory, Lawrence ,  BOWMAN, Brian, Roger ,  SOWA, Mathew, Edward ,  BLODGETT, Joshua Alan, Van Dyke ,  ROBISON, Keith, Earl ,  STILES, Dylan, Talbot ,  MORGENSTERN, Jay, Paul ,  TOWNSON, Sharon, Ann ,  SHIGDEL, Uddhav, Kumar

    IPC分类号： A61K38/12 ,  A61K47/48 ,  C07K7/64

    CPC分类号： C07D498/18 ,  A61K38/00 ,  A61K47/62 ,  A61P35/00

    摘要： The invention features compounds (e.g., macrocyclic compounds) capable of modulating biological processes, for example through binding to a presenter protein (e.g., a member of the FKBP family, a member of the cyclophilin family, or PIN1 ) and a target protein such as CEP250. These compounds bind endogenous intracellular presenter proteins, such as the FKBPs or cyclophilins, and the resulting binary complexes selectively bind and modulate the activity of the target protein. Formation of a tripartite complex among the presenter protein, the compound, and the target protein is driven by both protein-compound and protein-protein interactions, and both are required for modulation of target protein activity.

    摘要翻译： 本发明具有能够调节生物过程的化合物（例如，大环化合物），例如通过结合呈递者蛋白（例如，FKBP家族的成员，亲环蛋白家族的成员或PIN1）和靶蛋白如 CEP250。 这些化合物结合内源性细胞内呈递者蛋白质，例如FKBPs或亲环蛋白，所得二元复合物选择性结合并调节靶蛋白的活性。 主要蛋白质，化合物和靶蛋白之间的三方复合物的形成由蛋白质 - 化合物和蛋白质 - 蛋白质相互作用驱动，并且都需要调节靶蛋白活性。

    COMPOUNDS THAT PARTICIPATE IN COOPERATIVE BINDING AND USES THEREOF
    9.
    发明申请
    COMPOUNDS THAT PARTICIPATE IN COOPERATIVE BINDING AND USES THEREOF 审中-公开

    公开(公告)号：WO2018187401A1

    公开(公告)日：2018-10-11

    申请号：PCT/US2018/025991

    申请日：2018-04-04

    申请人： WARP DRIVE BIO, INC.

    发明人： MULVIHILL, Mark, Joseph ,  JIN, Meizhong

    IPC分类号： A61K47/48

    摘要： The invention features compounds (e.g., macrocyclic compounds) capable of modulating biological processes, for example through binding to a presenter protein (e.g., a member of the FKBP family, a member of the cyclophilin family, or PIN1) and a target protein (e.g., a eukaryotic target protein such as a mammalian target protein or a fungal target protein or a prokaryotic target protein such as a bacterial target protein). These compounds bind endogenous intracellular presenter proteins, such as the FKBPs or cyclophilins, and the resulting binary complexes selectively bind and modulate the activity of intracellular target proteins. Formation of a tripartite complex among the presenter protein, the compound, and the target protein is driven by both protein-compound and protein-protein interactions, and both are required for modulation of the targeted protein's activity.

    METHODS AND REAGENTS FOR ANALYZING PROTEIN-PROTEIN INTERFACES
    10.
    发明申请
    METHODS AND REAGENTS FOR ANALYZING PROTEIN-PROTEIN INTERFACES 审中-公开
    用于分析蛋白质 - 蛋白质界面的方法和试剂

    公开(公告)号：WO2017059207A8

    公开(公告)日：2017-04-06

    申请号：PCT/US2016/054691

    申请日：2016-09-30

    申请人： WARP DRIVE BIO, INC.

    发明人： VERDINE, Gregory, L. ,  NICHOLS, M., James ,  TOWNSON, Sharon, A. ,  SHIGDEL, Uddhav, Kumar ,  LEE, Seung-Joo ,  STILES, Dylan, T. ,  ANTHONY, Neville, J.

    IPC分类号： A61K47/42 ,  A61K38/12 ,  A61K38/13 ,  A61K38/17 ,  C12N9/90

    摘要： The present disclosure provides methods and reagents useful for analyzing protein-protein interfaces such as interfaces between a presenter protein (e.g., a member of the FKBP family, a member of the cyclophilin family, or PIN1 ) and a target protein. In some embodiments, the target and/or presenter proteins are intracellular proteins. In some embodiments, the target and/or presenter proteins are mammalian proteins.

    摘要翻译： 本公开内容提供了用于分析蛋白质 - 蛋白质界面的方法和试剂，所述蛋白质 - 界面蛋白质例如呈递蛋白质（例如，FKBP家族的成员，亲环蛋白家族成员或PIN1）和 一个目标蛋白质。 在一些实施方案中，靶和/或呈递者蛋白质是细胞内蛋白质。 在一些实施方案中，靶和/或呈递者蛋白质是哺乳动物蛋白质。