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1. 发明授权

US5395924A Blocked lectins; methods and affinity support for making the same using affinity ligands; and method of killing selected cell populations having reduced non-selective cytotoxicity 失效
标题翻译：阻断凝集素; 方法和亲和力支持使用亲和配体进行相同; 以及杀死所选择的具有降低的非选择性细胞毒性的细胞群的方法
公开(公告)号：US5395924A
公开(公告)日：1995-03-07
申请号：US19831
申请日：1993-02-19
申请人： Walter A. Blattler , John M. Lambert , Victor S. Goldmacher , Ravi V. J. Chari , Charles F. Scott, Jr. , Linda J. Kostuba , Simon E. Moroney , Albert R. Collison
发明人： Walter A. Blattler , John M. Lambert , Victor S. Goldmacher , Ravi V. J. Chari , Charles F. Scott, Jr. , Linda J. Kostuba , Simon E. Moroney , Albert R. Collison
IPC分类号： A61K47/48 , C07H21/00 , C07K3/00 , A61K39/00
CPC分类号： C07H21/00 , A61K47/48438
摘要： An activated affinity ligand is described comprising: a ligand having (a) a region with affinity for binding sites of a lectin; and (b) a reactive group capable of covalently linking the ligand to the lectin to thereby block one or more of the binding sites of the lectin. A blocked lectin is described comprising one or more affinity ligands covalently linked by means of a reactive group present on each of the ligands to a lectin such that one or more binding sites of the lectin is blocked. A cell-binding agent-blocked lectin conjugate is described comprising the above-described blocked lectin and a cell-binding agent covalently linked to: (a) one of the covalently linked affinity ligands; or (b) the lectin. A method of preparing the cell-binding agent-blocked lectin conjugate is described. An affinity support capable of binding to a lectin to form a blocked lectin is described comprising an activated affinity ligand covalently linked to a solid support. A method of preparing the affinity support capable of binding to a lectin to form a blocked lectin is described. A method of killing selected cell populations having reduced cytotoxicity to non-selected cell populations is described comprising contacting a cell population or tissue suspected of containing cells from said selected cell population with the above-described cell-binding agent-blocked lectin conjugate, wherein the lectin is a cytotoxic lectin. Medicaments and methods of treatment using the above-described cell-binding agent-blocked lectin conjugate also are described.
摘要翻译：描述了活化的亲和配体，其包括：具有（a）对凝集素的结合位点具有亲和力的区域的配体; 和（b）能够将配体与凝集素共价连接从而阻断凝集素的一个或多个结合位点的反应性基团。描述了封闭的凝集素，其包含通过存在于每个配体上的反应性基团与凝集素共价连接的一个或多个亲和配体，使得凝集素的一个或多个结合位点被阻断。描述了包含上述封闭凝集素和共价连接的细胞结合剂的细胞结合剂阻断的凝集素缀合物：（a）共价连接的亲和配体之一; 或（b）凝集素。描述了制备细胞结合剂阻断的凝集素缀合物的方法。描述了能够结合凝集素以形成封闭的凝集素的亲和载体，其包含与固体支持物共价连接的活化的亲和配体。描述了制备能够结合凝集素形成封闭的凝集素的亲和载体的方法。描述了杀死对未选择的细胞群体具有降低的细胞毒性的选定细胞群的方法，其包括使来自所述选择的细胞群的怀疑含有细胞的细胞群体或组织与上述细胞结合剂阻断的凝集素缀合物接触，其中凝集素是一种细胞毒素凝集素。还描述了使用上述细胞结合剂阻断的凝集素缀合物的药物和治疗方法。

2. 发明授权

US5239062A Blocked lectins, methods and affinity support for making same using affinity ligands, and method of killing selected cell populations having reduced nonselective cytotoxicity 失效
标题翻译：阻断凝集素，方法和亲和力支持使用亲和配体进行相同的操作，以及杀死选择性细胞群降低非选择性细胞毒性的方法
公开(公告)号：US5239062A
公开(公告)日：1993-08-24
申请号：US560948
申请日：1990-07-31
申请人： Walter A. Blattler , John M. Lambert , Victor S. Goldmacher , Ravi V. J. Chari , Charles F. Scott, Jr. , Linda J. Kostuba , Simon E. Moroney , Albert R. Collinson
发明人： Walter A. Blattler , John M. Lambert , Victor S. Goldmacher , Ravi V. J. Chari , Charles F. Scott, Jr. , Linda J. Kostuba , Simon E. Moroney , Albert R. Collinson
IPC分类号： A61K47/48 , C07H21/00
CPC分类号： C07H21/00 , A61K47/48438
摘要： An activated affinity ligand is described comprising: a ligand having (a) a region with affinity for binding sites of a lectin; and (b) a reactive group capable of covalently linking the ligand to the lectin to thereby block one or more of the binding sites of the lectin. A blocked lectin is described comprising one or more affinity ligands covalently linked by means of a reactive group present on each of the ligands to a lectin such that one or more binding sites of the lectin is blocked. A cell-binding agent-blocked lectin conjugate is described comprising the above-described blocked lectin and a cell-binding agent covalently linked to: (a) one of the covalently linked affinity ligands; or (b) the lectin. A method of preparing a blocked lectin is described. A method of preparing the cell-binding agent-blocked lectin conjugate is described. An affinity support capable of binding to a lectin to form a blocked lectin is described comprising an activated affinity ligand covalently linked to a solid support. A method of preparing the affinity support capable of binding to a lectin to form a blocked lectin is described. A method of killing selected cell populations having reduced cytotoxicity to non-selected cell populations is described comprising contacting a cell population or tissue suspected of containing cells from said selected cell population with the above-described cell-binding agent-blocked lectin conjugate, wherein the lectin is a cytotoxic lectin. Medicaments and methods of treatment using the above-described cell-binding agent-blocked lectin conjugate also are described.
摘要翻译：描述了活化的亲和配体，其包括：具有（a）对凝集素的结合位点具有亲和力的区域的配体; 和（b）能够将配体与凝集素共价连接从而阻断凝集素的一个或多个结合位点的反应性基团。描述了封闭的凝集素，其包含通过存在于每个配体上的反应性基团与凝集素共价连接的一个或多个亲和配体，使得凝集素的一个或多个结合位点被阻断。描述了包含上述封闭凝集素和共价连接的细胞结合剂的细胞结合剂阻断的凝集素缀合物：（a）共价连接的亲和配体之一; 或（b）凝集素。描述了一种制备阻塞凝集素的方法。描述了制备细胞粘附剂阻断的凝集素缀合物的方法。描述了能够结合凝集素以形成封闭的凝集素的亲和载体，其包含与固体支持物共价连接的活化的亲和配体。描述了制备能够结合凝集素形成封闭的凝集素的亲和载体的方法。描述了杀死对未选择的细胞群体具有降低的细胞毒性的选定细胞群的方法，其包括使来自所述选择的细胞群的怀疑含有细胞的细胞群体或组织与上述细胞结合剂阻断的凝集素缀合物接触，其中凝集素是一种细胞毒素凝集素。还描述了使用上述细胞结合剂阻断的凝集素缀合物的药物和治疗方法。

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