Synthetic method and application of modified Fc-III peptide, antibody-lipid conjugate and bispecific antibody compound

The invention discloses a synthetic method and application of a modified Fc-III peptide, an antibody-lipid conjugate and a bispecific antibody compound, and relates to a method for acetylating an Fc region of immune globulin, especially Lys248 of a heavy chain of human immune globulin G (IgG) by usi...

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Hauptverfasser: YUAN DINGDONG, XIA JIANG, ZHANG YU
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention discloses a synthetic method and application of a modified Fc-III peptide, an antibody-lipid conjugate and a bispecific antibody compound, and relates to a method for acetylating an Fc region of immune globulin, especially Lys248 of a heavy chain of human immune globulin G (IgG) by using a novel Fc-III derived peptide. The Lys248 site having bio-orthogonal reactive groups for further derivatization can be selectively functionalized by acetylation reaction with a phenolic ester having an azide or an alkyne. Further provided are methods of synthesizing antibody-lipid conjugates and bispecific antibody complexes (BsAbC) connecting two different antibodies, the conjugates being capable of constructing immunoliposomes that can target cells expressing oncogenes, including HER2 + cells. The BsAbC can induce the cytotoxicity mediated by effector cells under the nanomolar concentration. 本发明公开一种经修饰的Fc-III肽及抗体-脂质偶联物、双特异性抗体复合物的合成方法及应用,涉及使用新型Fc-III衍生肽对免疫球蛋白的Fc区域、特别是人免疫球蛋白G(IgG)重链的Lys248乙酰化的方法。通过与具有叠氮化物或炔烃的酚酯