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    • 2. 发明公开
    • ANTIBODY LOCKER FOR THE INACTIVATION OF PROTEIN DRUG
    • ANTIKÖRPERSPERRERZUR INAKTIVIERUNG VON PROTEINARZNEIMITTEL
    • EP3003370A2
    • 2016-04-13
    • EP14803825.0
    • 2014-05-28
    • DCB-USA LLCKaohsiung Medical University
    • CHENG, Tian-LuCHUANG, Chih-HungKO, Hsiu-FenLU, Yun-Chi
    • A61K39/395A61K39/00C12P21/08
    • Disclosed herein is a hinge antibody capable of being selectively activated in a target cell or tissue to treat a condition therein. The hinge antibody includes a functional antibody, two inhibitory domains and four cleavable linkers. The functional antibody is capable of treating the condition in an activated state, and has two light chains and two heavy chains. Each inhibitory domain includes a hinge domain of an immunoglobulin and consists of two peptide arms. Each cleavable linker includes a peptide substrate cleavable by an enzyme specifically or highly expressed in the target cell or tissue, and connects one of the peptide arms of the inhibitory domains to the N-terminal of one of the light chains and heavy chains of the functional antibody. Also disclosed herein are methods for preparing and using this hinge antibody.
    • 本文公开了能够在靶细胞或组织中选择性活化以治疗其中的病症的铰链抗体。 铰链抗体包括功能性抗体,两个抑制结构域和四个可切割接头。 功能性抗体能够处于活化状态,具有两条轻链和两条重链。 每个抑制结构域包括免疫球蛋白的铰链结构域并由两个肽臂组成。 每个可切割接头包括可由靶细胞或组织中特异性或高度表达的酶切割的肽底物,并将抑制结构域的一个肽臂与功能性的轻链和重链之一的N-末端连接 抗体。 本文还公开了制备和使用该铰链抗体的方法。