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    SPECIFIC ACTIVE SITE INHIBITORS OF ENZYMES OR SUBSTRATE BINDING PARTNERS AND METHODS OF PRODUCING SAME
    1.
    发明申请
    SPECIFIC ACTIVE SITE INHIBITORS OF ENZYMES OR SUBSTRATE BINDING PARTNERS AND METHODS OF PRODUCING SAME 审中-公开
    酶或底物结合的特定活性位点抑制剂及其生产方法

    公开(公告)号：WO2012020289A3

    公开(公告)日：2012-05-18

    申请号：PCT/IB2011001663

    申请日：2011-06-08

    Applicant: UNIV TORONTO ,  SIDHU SACHDEV ,  BEATTY LINDA ,  ERNST ANDREAS

    Inventor： SIDHU SACHDEV ,  BEATTY LINDA ,  ERNST ANDREAS

    IPC: C07K14/47

    CPC classification number: C07K14/435 ,  A61K38/17 ,  C07K14/47

    Abstract: The present disclosure provides a method of producing enzyme- specific inhibitors or substrate binding partners comprising: identifying active site residues of the substrate in the enzyme substrate complex or in substrate binding partner-substrate complex; randomizing the active site residues to produce a combinatorial library of substrate variants; and selecting substrate variants that inhibit enzyme activity or bind substrate as substrate-specific binding partners. The present disclosure also provides ubiquitin enzyme specific inhibitors and ubiquitin variants that bind ubiquitin interaction motifs.

    Abstract translation: 本公开提供了生产酶特异性抑制剂或底物结合配偶体的方法，包括：鉴定酶底物复合物或底物结合配偶体 - 底物复合物中底物的活性位点残基; 使活性位点残基随机化以产生底物变体的组合文库; 并选择抑制酶活性或结合底物作为底物特异性结合配偶体的底物变体。 本公开还提供了结合遍在蛋白相互作用基序的遍在蛋白酶特异性抑制剂和泛素变体。

    SPECIFIC ACTIVE SITE INHIBITORS OF ENZYMES OR SUBSTRATE BINDING PARTNERS AND METHODS OF PRODUCING SAME
    2.
    发明申请
    SPECIFIC ACTIVE SITE INHIBITORS OF ENZYMES OR SUBSTRATE BINDING PARTNERS AND METHODS OF PRODUCING SAME 审中-公开
    酶或底物结合剂的特定活性位点抑制剂及其生产方法

    公开(公告)号：WO2012020289A2

    公开(公告)日：2012-02-16

    申请号：PCT/IB2011/001663

    申请日：2011-06-08

    Applicant: THE GOVERNING COUNCIL OF THE UNIVERSITY OF TORONTO ,  SIDHU, Sachdev ,  BEATTY, Linda ,  ERNST, Andreas

    Inventor： SIDHU, Sachdev ,  BEATTY, Linda ,  ERNST, Andreas

    IPC: C07K14/47

    CPC classification number: C07K14/435 ,  A61K38/17 ,  C07K14/47

    Abstract: The present disclosure provides a method of producing enzyme- specific inhibitors or substrate binding partners comprising: identifying active site residues of the substrate in the enzyme substrate complex or in substrate binding partner-substrate complex; randomizing the active site residues to produce a combinatorial library of substrate variants; and selecting substrate variants that inhibit enzyme activity or bind substrate as substrate-specific binding partners. The present disclosure also provides ubiquitin enzyme specific inhibitors and ubiquitin variants that bind ubiquitin interaction motifs.

    Abstract translation: 本公开提供了生产酶特异性抑制剂或底物结合配偶体的方法，包括：鉴定酶底物复合物或底物结合配偶体 - 底物复合物中底物的活性位点残基; 使活性位点残基随机化以产生底物变体的组合文库; 并选择抑制酶活性或结合底物作为底物特异性结合配偶体的底物变体。 本公开还提供泛素酶特异性抑制剂和结合泛素相互作用基序的泛素变体。

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