The linkers currently used are mainly divided into two categories according to different mechanisms, the first cleavable linker and the second non-cleavable linkers.There are three different types of release mechanisms for cleavable linkers: 1. Lysosomal protease-sensitive linkers.Using lysosomal proteases, such as cathepsin B, we identify and cleave a dipeptide bond to release free drugs from the conjuder.The 2. acid-sensitive linker.The advantage of this class of linkers is stimulating the hydrolysis of an acid unstable group within the linker in a low pH environment in lysosomes to release the drug.The 3. glutathione-sensitive linker.This strategy makes advantage of higher concentrations of thiols in the cellular blood, such as glutathione, where the linker disulfide bonds are relatively stable in the blood circulation but glutathione is reduced to release the free drug.Cleavable connectors can be divided into small and macromolecular linkers according to the molecular size of the linker.ADCs coupled with small molecule linkers, which have poor water-soluble connections and good water-soluble antibodies, can lead to large toxic side effects of protein aggregation.
Conjugated molecules
作者:超级管理员发布时间:2021-10-27 08:54:20
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