Modified cellular substrates are used as linking groups that are recognized as cellular substrates by intracellular metabolic enzymes. The linking groups function to attach a ligand, such as a drug or radionuclide, to a targeting protein, such as an antibody or antibody fragment. The false substrate structure of the linking groups causes increased cellular retention of the linking group/ligand conjugate because the enzymes used for catabolism of the substrate are inhibited by the false substrate structure of the linking group.
经修饰的细胞底物可用作连接基团,被细胞内代谢酶识别为细胞底物。连接基团的作用是将
配体(如药物或放射性核素)连接到靶向蛋白(如
抗体或
抗体片段)上。连接基团的假底物结构可增加细胞对连接基团/
配体共轭物的保留,因为用于分解底物的酶受到连接基团假底物结构的抑制。