Peptide-drug conjugates
    75.
    发明授权
    Peptide-drug conjugates 有权
    肽 - 药物共轭物

    公开(公告)号:US09579317B2

    公开(公告)日:2017-02-28

    申请号:US14726897

    申请日:2015-06-01

    Inventor: Shaosong Chu

    Abstract: Peptide-drug conjugates comprising p-aminobenzyl carbamoyl or p-aminobenzolyl carbonate self-immolating linkers are disclosed. The peptide-drug conjugates comprise a peptide moiety that can be cleaved by cellular proteases, bound to the self-immolating linker, which linker is bound to a cytotoxic drug moiety. Upon cleavage of the peptide moiety, the linker self-immolates, releasing the cytotoxic drug in active form. Dimeric structures of the peptide drug conjugates comprising two molecules of cytotoxic drug per conjugate are also disclosed.

    Abstract translation: 公开了包含对氨基苄基氨基甲酰基或对氨基苯甲酰碳酸酯自脱胶接头的肽 - 药物共轭物。 肽 - 药物缀合物包含能够被细胞蛋白酶切割的肽部分,其结合到自蜕膜接头上,该接头与细胞毒性药物部分结合。 在肽部分切割时,连接体自身脱粘,释放活性形式的细胞毒性药物。 还公开了包含每个缀合物的两分子细胞毒性药物的肽药物缀合物的二聚体结构。

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