The present invention relates to biomolecule conjugates which comprise a biomolecule wherein at least one non-natural amino acid (NNAA) is integral to the structure of the biomolecule and wherein the NNAA is a point of attachment of a linker to which a payload, particularly a cytotoxic agent, is attached. More specifically, this invention relates to conjugates of cell-binding agents and active release products comprising cytotoxic agents wherein the conjugates are produced by means of a cycloaddition reaction. Methods of production, pharmaceutical compositions and methods of use are provided.
本发明涉及
生物分子共轭物,其包括一种
生物分子,其中至少有一种非天然
氨基酸(NNAA)构成
生物分子的结构,并且NNAA是连接物的附着点,连接物上附着有一种荷载物,特别是细胞毒性药剂。更具体地说,本发明涉及细胞结合剂和活性释放产物的共轭物,其中共轭物是通过环加成反应制备的。提供了生产方法、药物组合物和使用方法。