| abstract |
[PROBLEMS] To prevent the detachment of a low-molecular-weight drug, it has sufficient stability outside the cell, and after being taken into the cell, a cleavable linker is ruptured under appropriate conditions to release an active low-molecular-weight drug. On the other hand, in the case of a non-cleavable linker, an antibody-drug conjugate linker is provided in which the active ingredient is composed of a small molecule, a linker, and an amino acid residue obtained by enzymatic degradation. A novel linker having a binding function (linker, also known as a coupling agent), a method for producing a linker-payload intermediate and a ring-opening reaction and a method for converting a linker-payload intermediate into a protein in a site-specific manner, Disclosed are a method for stably connecting to the C-terminus of a peptide, a method for producing a complex product thereof, and a complex formed between the complex product and a drug. [Selection diagram] None |